WO2006042625A2 - Compositions with inhibitors of the synthesis of prostaglandin and/or of leukotriene in conjunction with stimulators of the release of cutaneous neuromediators - Google Patents

Compositions with inhibitors of the synthesis of prostaglandin and/or of leukotriene in conjunction with stimulators of the release of cutaneous neuromediators Download PDF

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WO2006042625A2
WO2006042625A2 PCT/EP2005/010524 EP2005010524W WO2006042625A2 WO 2006042625 A2 WO2006042625 A2 WO 2006042625A2 EP 2005010524 W EP2005010524 W EP 2005010524W WO 2006042625 A2 WO2006042625 A2 WO 2006042625A2
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acid
skin
extracts
synthesis
composition according
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PCT/EP2005/010524
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German (de)
French (fr)
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WO2006042625A3 (en
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Thomas Döring
Anemone TRÄGER
Bernd Anderheggen
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Henkel Kommanditgesellschaft Auf Aktien
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Priority to EP05790088A priority Critical patent/EP1799311A2/en
Publication of WO2006042625A2 publication Critical patent/WO2006042625A2/en
Publication of WO2006042625A3 publication Critical patent/WO2006042625A3/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/007Preparations for dry skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0208Tissues; Wipes; Patches
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4986Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with sulfur as the only hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/58Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
    • A61K8/585Organosilicon compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • A61K8/733Alginic acid; Salts thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9706Algae
    • A61K8/9711Phaeophycota or Phaeophyta [brown algae], e.g. Fucus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9728Fungi, e.g. yeasts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9755Gymnosperms [Coniferophyta]
    • A61K8/9761Cupressaceae [Cypress family], e.g. juniper or cypress
    • AHUMAN NECESSITIES
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    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9794Liliopsida [monocotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/14Preparations for removing make-up
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/004Aftersun preparations
    • AHUMAN NECESSITIES
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    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
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    • A61Q19/005Preparations for sensitive skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
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    • A61Q19/08Anti-ageing preparations
    • AHUMAN NECESSITIES
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    • A61Q19/00Preparations for care of the skin
    • A61Q19/10Washing or bathing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74Biological properties of particular ingredients
    • A61K2800/78Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782Enzyme inhibitors; Enzyme antagonists

Definitions

  • compositions with inhibitors of prostaglandin and / or leukotriene synthesis in combination with stimulants of the release of cutaneous neuromediators Compositions with inhibitors of prostaglandin and / or leukotriene synthesis in combination with stimulants of the release of cutaneous neuromediators
  • the present invention relates to topical cosmetic and / or dermatological compositions for the treatment of sensitive and / or dry skin, for the treatment of atopic dermatitis and / or for the treatment of sensory irritations and skin inflammations of the aging skin.
  • the object of the present invention was to develop compositions for the treatment of sensitive and / or dry skin with improved effectiveness compared to the prior art, which both inhibit inflammatory mechanisms and sensory irritations, such as, for example. As itching, reduce.
  • Another task of the present The invention was to develop compositions for the treatment of atopic dermatitis with respect to the prior art improved efficacy, which inhibit both inflammatory mechanisms and sensory irritations, such as. As itching, reduce.
  • a further object of the present invention was to develop compositions for the treatment of sensory irritations and skin inflammations of the aging skin with improved efficacy compared with the prior art, which inhibit both inflammatory mechanisms and sensory irritations, such as, for example, As itching, reduce.
  • compositions which contain at least one active substance which inhibits inflammatory mechanisms and at least one active substance which minimizes sensory irritations.
  • active substance which inhibits inflammatory mechanisms
  • active substance which minimizes sensory irritations.
  • the present invention for the first time combines anti-irritative effects with a simultaneous, lasting alleviation of sensory irritations.
  • the different types of drugs can complement each other in a synergistic manner.
  • the present invention relates to cosmetic and / or dermatological topical compositions which, in a suitable carrier, contain at least one active substance which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active substance which stimulates the cutaneous synthesis of neuromediators. contain.
  • a suitable carrier contains at least one active substance which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active substance which stimulates the cutaneous synthesis of neuromediators. contain.
  • this specific combination of active substances is particularly suitable for the care and treatment of the skin, in particular the sensitive skin, the dry skin and / or the atopic skin as well as the aged skin.
  • the active ingredient inhibiting the prostaglandin synthesis is selected from active substances which inhibit the enzyme cyclooxygenase.
  • the inhibition of cyclooxygenase can be understood as meaning both a reduction in the amount of this enzyme and a reduction in its activity, as well as both.
  • the active ingredient which inhibits prostaglandin synthesis is selected from active compounds which inhibit the secretion of interleukins, in particular of interleukin-1-alpha.
  • the active substance inhibiting leukotriene synthesis is selected from active substances which inhibit the enzyme 5-lipoxygenase.
  • the inhibition of 5-lipoxygenase can be understood as meaning both a reduction in the amount of this enzyme and a reduction in its activity, as well as both.
  • the active substance stimulating the cutaneous synthesis of neuromediators is selected from active substances which stimulate ⁇ -endorphin synthesis in keratinocytes.
  • Inhibitors of prostaglandin synthesis which are preferred according to the invention, in particular inhibitors of cyclooxygenase and / or interleukin secretion, are selected from silymarin, which is particularly preferably used in liposome-encapsulated form (obtainable, for example, under the trade name silymarin phytosome (INCI: Silybum Marianum Extract and phospholipids) from the company Indena SpA.
  • silymarin represents an active substance concentrate from the fruits of the milk thistle (Silybum marianum) which was formerly regarded as a uniform substance.
  • silybin silybin I
  • silychristin silymarin II
  • silydianin Other preferred inhibitors of prostagladin synthesis according to the invention, in particular inhibitors of cyclooxygenase and / or interleukin secretion, are selected from extracts of Centella asiatica, for example available under the name Madecassicoside from DSM, glycyrrethine acid, which is particularly preferably encapsulated in liposomes and in this form z.
  • compositions according to the invention are characterized in that the concentration of the inhibitor (s) of the prostaglandin synthesis in total 0.0001-10.0% by weight, preferably 0.001-2.0% by weight, particularly preferably 0.05%. 1, 0 wt .-% and most preferably 0.1 to 0.5 wt .-%, each based on the total composition is.
  • Inhibitors of leukotriene synthesis which are preferred according to the invention, in particular inhibitors of 5-lipoxygenase, are selected from algin hydrolyzates, amino dicarboxylic acids having a C chain length of 3 to 6 carbon atoms and their physiologically tolerated salts, N-alkylated C 2 -C 10 amino acids C 1 -C 22 -alkyl radicals and their physiologically tolerated salts, N-acylated C 2 -C i i-amino acids with C 2 -C 22 acyl radicals and their physiologically tolerated salts, yeast extracts, ⁇ -bisabolol, ⁇ -lipoic acid, and any desired mixtures of these agents.
  • the algin hydrolyzates according to the invention are selected from the products which, for. B. under the trade name phycosaccharides, in particular phycosaccharides Al, are available from Codif.
  • compositions according to the invention are characterized in that at least one amino dicarboxylic acid having a C chain length of 3 to 6 carbon atoms or at least one physiologically acceptable salt of an amino dicarboxylic acid having a C chain length of 3 to 6 carbon atoms in a total amount of 0.01 to 5 wt .-%, preferably 0.1 to 2 wt .-% and particularly preferably 0.5 to 1 wt .-%, each based on the total topical composition is included.
  • the preferred N-alkylated C 2 -C 11 -amino acids with a C 1 -C 22 -alkyl radical selected from alanine, glutamic acid, pyroglutamic acid, lysine, arginine, histidine, valine, leucine, isoleucine, Pro ⁇ lin, tryptophan, phenylalanine, methionine, glycine, serine, tyrosine, threonine, cysteine, asparagin and glutamine and their physiologically tolerated salts which on the nitrogen atom of the amino group are a C r C 22 -alkyl radical selected from a group of methyl, Ethyl, propyl, butyl, pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl (lauryl), tridecyl, tetrade
  • compositions of the invention are characterized in that at least one N-alkylated C ⁇ C ⁇ amino acid having a C r C 22 -alkyl radical or at least one physiologically acceptable salt of an N-alkylated Cz-Cn-amino acid having a C 1 -C 22 -alkyl radical in a total amount of 0.01 to 10 wt .-%, preferably 0.1 to 5 wt .-% and particularly preferably 0.5 to 2 wt .-%, each based on the total topical composition is included.
  • the inventively preferred N-acylated C 2 -C 1 r are amino acids having a C 2 -C 22 acyl radical selected from glutamic acid, pyroglutamic acid, lysine, arginine, histidine, valine, leucine, isoleucine, proline, Tryp ⁇ tophan, phenylalanine, methionine, glycine, serine, tyrosine, threonine, cysteine, asparagine and glutamine and their physiologically acceptable salts.
  • the amino acids can be used individually or in a mixture. More particularly suitable according to the invention are amino acid mixtures which have been obtained from plants, in particular cereal plants.
  • the C 2 -C 22 -acyl radical with which the amino acids mentioned are derivatized at the amino group is selected from an acetyl, propanoyl, butanoyl, pentanoyl, hexanoyl, heptanoyl, octanoyl, nonanoyl -, decanoyl, undecanoyl, lauroyl, tridecanoyl, myristoyl, pentadecanoyl, cetoyl, palmitoyl, stearoyl, arachidoyl or behenoyl radical.
  • Mixtures of C 8 -C 8 -acyl radicals are also referred to as cocoyl radical and are likewise preferred substituents.
  • the cereal plants from which the amino acids suitable according to the invention are obtained are subject to no restriction.
  • oats, wheat, barley and rye are suitable; oat is particularly suitable.
  • a particularly preferred 5-lipoxygenase inhibitor is a mixture of the sodium salts of amino acids acylated with coconut fatty acid residues, the potassium and magnesium salts of aspartic acid and sarcosine, as described for example as Sepiealm S by Seppic with the INCI name "Sodium Cocoyl Amino Acids, Sarcosine, Potassium Aspartate, Magnesium Aspartate" is available.
  • compositions according to the invention are characterized in that at least one N-acylated C 2 -C 1 r amino acids having a C 2 -C 22 acyl residue or at least one physiologically acceptable salt of an N-acylated C 1 -C 5 amino acid having a C 2 - C 22 - Acy I rest in a total amount of 0.01 to 10 wt .-%, preferably 0.1 to 5 wt .-% and particularly preferably 0.5 to 2 wt .-%, each based on the total topical composition , is included.
  • the yeast extracts preferred according to the invention as 5-lipoxygenase inhibitors are in amounts of from 0.001 to 5% by weight, preferably from 0.01 to 2% by weight and particularly preferably from 0.1 to 1% by weight, in each case based on the total topical composition used.
  • a particularly preferred commercial product used is Drieline (INCI name "sorbitol, Yeast Extract”), available from Lanatech.
  • the preferred 5-lipoxygenase inhibitor according to the invention is ⁇ -bisabolol in amounts of 0.001 to 5% by weight, preferably 0.01 to 2% by weight and particularly preferably 0.1 to 1% by weight. , in each case based on the total topical composition used.
  • the 5-lipoxygenase inhibitor preferred according to the invention is ⁇ -lipoic acid in amounts of 0.001 to 5% by weight, preferably 0.01 to 2% by weight and more preferably 0.1 to 1% by weight. , in each case based on the total topical composition used.
  • the sterol sulphate salts can be used both individually and in any desired mixtures.
  • compositions according to the invention are characterized in that at least one physiologically acceptable sterolsulfate salt in a total amount of 0.001 to 5 wt .-%, preferably 0.01 to 2 wt .-% and particularly preferably 0.1 to 1 wt .-%, each based on the total topical composition, is included.
  • physiologically tolerated salts of the abovementioned 5-lipoxygenase inhibitors are preferably selected from the ammonium, alkali metal, magnesium, calcium, aluminum, zinc and manganese salts. Particular preference is given to the sodium, potassium, magnesium, aluminum, zinc and manganese salts.
  • compositions according to the invention are characterized in that at least one inhibitor of leukotriene synthesis is present in a total amount of 0.0001-10.0% by weight, preferably 0.001-2.0% by weight, particularly preferably 0.05-1. 0 wt .-% and most preferably 0.1 to 0.5 wt .-%, each based on the total composition is included.
  • Particularly preferred modulators according to the invention of the release of cutaneous neurotransmitters are selected from mixtures of at least one extract from the leaves of Mentha piperita and at least one extract from cocoa beans (Theobroma cacao) aqueous, glycolic or aqueous-glycolic preparations of these extract mixtures, in particular those which are obtainable under the trade name Caomint from the company Solabia, are particularly preferred.
  • Another particularly preferred modulator of the release of cutaneous neuromediators is the dipeptide derivative N-acetyl-Tyr-Arg-hexyldecyl ester with the INCI name Acetyl Dipeptide-1 Cetyl Ester, which, for. B.
  • cutaneous release Neuromediators in particular stimulators of ⁇ -endorphin secretion in keratinocytes, are extracts from the shells of cocoa beans (Theobroma cacao), for example obtainable as raw material caobromines, cao-orange, caospice and caophenol from Solabia.
  • Further inventively preferred modulators of the release kuta ⁇ ner neuromediators, in particular stimulators of ß-endorphin secretion in keratinocytes are selected from extracts of Helichrysum italicum, z. B.
  • ArEAUmat Perpetua (INCI: Water, Helichrysum italicum extract) and ArEAUmat Perpetua Glycerine (INCI: Glycerol, Water, Helichrysum italicum extract) from Codif, extracts from Crithmum Maritimum, z.
  • ArEAUmat Samphira (Sea Fennel, INCI: Water, Crithmum Maritimum Extract) and Aroleat Samphira (INCI: Caprylic / Capric Triglyceride, Hydroge- nated Vegetable Oil, Crithmum Maritimum Extract) from Codif, extracts from Lavandula stoechas , z.
  • ArEAUmat Samphira Sea Fennel, INCI: Water, Crithmum Maritimum Extract
  • Aroleat Samphira (INCI: Caprylic / Capric Triglyceride, Hydroge- nated Vegetable Oil, Crithmum Maritimum Extract) from Codif, extracts
  • ArEAUmat Lavanda (INCI: Water, Lavandula stoechas extract) and ArEAUmat Lavanda (INCI: Glycerol, Water, Lavandula stoechas extract) from Codif, extracts from Mentha piperita, z. Available under the tradenames Authenticals of Peppermint (Solabia) and Calmi- ska (Silab), glutamylamidoethyl indole, eg. B.
  • Tephroline (INCI: Water, Propylene Glycol, Tephrosia purpurea extract) from the company Vincience, mixtures of the oil of Mentha arvensis leaves, lime skin oil, cypress oil, lavender oil and Cistus Ladeniferus oil with the INCI Name Mentha Arvensis Leaf OiI and Citrus Medica Limonium (Lemon) Peel OiI and Cupressus Sempervirens OiI and Lavandula Hybrida OiI and Cistus Ladaniferus OiI, z. B. available under the trade name V-Tonic (Gattefosse), hexasaccharides according to FR 2842201, as well as any mixtures of vor ⁇ named active ingredients.
  • Preferred cosmetic compositions according to the invention are characterized in that at least one active substance for modulating the release of cutaneous neurotransmitters, in particular at least one stimulator of the ⁇ -endorphin secretion in keratinocytes, in a total amount of 0.000001-10% by weight, preferably 0 , 00001 - From 5 to 10% by weight, more preferably from 0.0001 to 1 to 2 to 3% by weight and, most preferably, from 0.001 to 0.005 to 0.01 to 0.1 to 0.5% by weight, based in each case on the content of active substance in the entire cosmetic composition, is included.
  • further cosmetic active ingredients are contained.
  • Preferred further active ingredients are humectants, in particular selected from the water-soluble polyhydric C 2 -C 9 -alkanols having 2 to 6 hydroxyl groups and / or the water-soluble polyethylene glycols, consisting of 3 to 20 ethylene oxide units, and mixtures thereof.
  • These components are preferably selected from 1,2-propylene glycol, 2-methyl-1,3-propanediol, glycerol, butylene glycols such as 1,2-butylene glycol, 1,3-butylene glycol and 1,4-butylene glycol, pentylene glycols, hexane diols, such as 1, 6-hexanediol, hexanetriols such as 1, 2,6-hexanetriol, 1, 8-octanediol, dipropylene glycol, tripropylene glycol, diglycerol, triglycerol, erythritol, sorbitol and mixtures of the aforementioned substances.
  • Suitable water-soluble polyethylene glycols consisting of 3 to 20 ethylene oxide units, are selected from PEG-3, PEG-4, PEG-6, PEG-7, PEG-8, PEG-9, PEG-10, PEG-12, PEG- 14, PEG-16, PEG-18 and PEG-20, and mixtures thereof, with PEG-3 to PEG-8 being preferred.
  • Sugar and certain sugar derivatives such as fructose, glucose, maltose, maltitol, mannitol, inositol, sucrose, trehalose, xylose, rhamnose and fucose may also be preferred according to the invention.
  • humectants are taurine, allantoin, (2-hydroxyethyl) urea, biosaccharide Gum-1 and glycosaminoglycans and their salts and / or esters, especially hyaluronic acid, its salts and its silanol derivatives.
  • Preferred cosmetic compositions according to the invention are characterized in that they contain at least one humectant in a total amount of 0.1-25% by weight, preferably 1.0-15% by weight, particularly preferably 5-10% by weight. based on the total composition.
  • active substances are selected from oligomers and polymers of amino acids, NC 2 -C 24 -acylamino acids, the esters and / or the physiologically tolerable salts of these substances, DNA or RNA oligonucleotides, natural betaine compounds, vitamins, Provitamins and vitamin precursors of groups A, B, C, E, H and K and the esters of the aforementioned substances, ⁇ -hydroxycarboxylic acids, ⁇ -ketocarboxylic acids, ⁇ -hydroxycarboxylic acids and their ester, lactone or salt form, flavonoids and flavonoid-rich plant extracts , Isoflavonoids and isoflavonoid rich plant extracts, polyphenols and polyphenol-rich plant extracts, ubiquinone and ubiquinol and derivatives thereof, naturally occurring xanthine derivatives, selected from caffeine, theophylline, theobromine and aminophylline, ectoine, anor ⁇ ganic and organic UV filter substances, self-t
  • amino acid oligomers are peptides having 2 to 30, preferably 2 to 15, amino acids.
  • the oligomers of the amino acids and / or the NC 2 -C 24 acylamino acids are preferably selected from di-, tri-, tetra-, penta-, hexa- or pentadecapeptides which may be acylated and / or esterified.
  • amino acid oligomers stimulate collagen synthesis or are able to recruit cells of the immune system, such as mast cells and macrophages, which then induce, or are capable of, repair processes in the tissue via the release of growth factors, eg collagen synthesis to bind the sequence Arg-Phe-Lys into thrombospondin I (TSP-1) and thus to release active TGF-ß (tissue growth factor), which induces the synthesis of collagen in dermal fibroblasts.
  • growth factors eg collagen synthesis to bind the sequence Arg-Phe-Lys into thrombospondin I (TSP-1) and thus to release active TGF-ß (tissue growth factor), which induces the synthesis of collagen in dermal fibroblasts.
  • TGF-ß tissue growth factor
  • N-acylated and / or esterified dipeptides are acetyl-citrullyl-arginine (eg Exsy-algins of exsymol with the INCI name Acetyl Citrull Amido Arginine), Tyr-Arg (dipeptide-1), Val- Trp (dipeptide-2), Asn-Phe, Asp-Phe, N-palmitoyl-.beta.-Ala-His, N-acetyl-Tyr-Arg-hexyldecylester (eg, calmosensins from Sederma), carnosine (.beta.-A!
  • acetyl-citrullyl-arginine eg Exsy-algins of exsymol with the INCI name Acetyl Citrull Amido Arginine
  • Tyr-Arg dipeptide-1
  • Val- Trp dipeptide-2
  • Asn-Phe Asp-Phe
  • N-acylated and / or esterified tripeptides are Gly-His-Lys, the z. B. under the name "Omega-CH activator" by the company GfN or in acylated form (N-palmitoyl-Gly-His-Lys) under the name Biopeptide CL of Sederma er ⁇ is available, but (in acylated form) also is a component of the product Matrixyl 3000 from Sederma
  • the tripeptide Gly-His-Lys can also be used as the copper salt (Cu 2+ ) and can be obtained as such from ProCyte Corporation.
  • Gly in accordance with the invention is suitable for Ala, Leu and He
  • the preferred amino acids according to the invention which can replace His or Lys include a side chain having a nitrogen atom which is predominantly charged at pH 6, eg Pro, Lys, Arg, His, desmosine and isodesmosine, more preferably Lys is replaced by Arg, Orn or citrulline.
  • a further preferred tripeptide according to the invention is Gly-His-Arg (INCI name: tripeptide-3) and its derivative N-myristoyl-Gly-His-Arg, which, for. B. under the designation Collasyn 314-GR of Therapeutic Peptide Inc.
  • N-acylated and / or esterified tetrapeptides are selected from Rigin and Rigin-based tetrapeptides and ALAMCAT tetrapeptides.
  • Rigin has the sequence Gly-Gln-Pro-Arg.
  • Rigin-based tetrapeptides include the Rigin analogs and Rigin derivatives, in particular the invention particularly preferred N-palmitoyl-Gly-Gln-Pro-Arg, z. B. is available under the name Eyeliss of Sederma, but also forms part of the product Matrixyl 3000 of Sederma.
  • the Rigin analogs include those in which the four amino acids are rearranged and / or in which a maximum of two amino acids are substituted by Rigin, z. For example, the sequence Ala-Gln-Thr-Arg.
  • At least one of the amino acids of the sequence has a Pro or Arg, and more preferably the tetrapeptide includes both Pro and Arg, and their order and position may vary.
  • the substituting amino acids can be selected from any amino acid which is defined below.
  • Particularly preferred rigin-based tetrapeptides include: Xaa-Xbb-Arg-Xcc, Xaa-Xbb-Xcc-Pro, Xaa-Xbb-Pro-Arg, Xaa-Xbb-Pro-Xcc, Xaa-Xbb-Xcc-Arg, wherein Xaa, Xbb and Xcc may be the same or different amino acids and wherein Xaa is selected from Gly and the amino acids which can substitute Gly, Xbb is selected from GIn and the amino acids which can substitute for GIn, Xcc is selected from Pro or Arg and the amino acids that can substitute Pro and Arg.
  • the preferred amino acids that can replace GIy include an aliphatic side chain, e.g. B. ⁇ -Ala, Ala, VaI, Leu, Pro, Sarcosine (Sar) and Isoleucine (He).
  • the preferred amino acids that can replace GIn include a side chain having an amino group predominantly uncharged at neutral pH (pH 6-7), eg, Asn, Lys, Om, 5-hydroxyproline, citrulline, and canavanine.
  • the preferred amino acids that can replace Arg include a side chain with a nitrogen atom predominantly charged at pH 6, such as Pro, Lys, His, desmosine, and isodesmosine.
  • Gly-Gln-Arg-Pro and Val-Val-Arg-Pro are preferred as Rigin analogues.
  • ALAMCAT tetrapeptides are tetrapeptides containing at least one amino acid with an aliphatic side chain, e.g. B. ⁇ -Ala, Ala, VaI, Leu, Pro, Sarcosine (Sar) and Isoleucine (He). Furthermore, ALAMCAT tetrapeptides contain at least one amino acid having a side chain with an amino group which is predominantly uncharged at neutral pH (pH 6-7), for example GIn, Asn, Lys, Om, 5-hydroxyproline, citrulline and canals. vanin. Furthermore, ALAMCAT tetrapeptides include at least one amino acid having a side chain with a nitrogen atom predominantly charged at pH 6, e.g.
  • ALAMCAT tetrapeptides may contain any amino acid; however, preferably the fourth amino acid is also selected from the three abovementioned groups.
  • N-acylated and / or esterified pentapep tides which are preferred according to the invention are selected from Lys-Thr-Thr-Lys-Ser and its N-acylated derivatives, more preferably N-palmitoyl-Lys-Thr-Thr-Lys-Ser which is available under the name Matrixyl from the company Sederma, furthermore N-palmitoyl-Tyr-Gly-Gly-Phe-Met, Val-Va-Arg-Pro-Pro, N-palmitoyl-Tyr-Gly-Gly-Phe- Leu, Gly-Pro-Phe-Pro-Leu and N-Benzyl-oxycarbonyl-Gly-Pro-Phe-Pro-Leu (the latter two are serine proteinase inhibitors for the inhibition of desquamation).
  • N-acylated and / or esterified hexapeptides are Val-Gly-Val-Ala-Pro-Gly and its N-acylated derivatives, particularly preferably N-palmitoyl-Val-Gly-Val-Ala-Pro-Gly Acetyl-Hexapeptide-3 (Argireline from Lipotec), Hexapeptide-4 (eg Collasyn 6KS from Therapeutic Peptide Inc.
  • Hexapeptide-5 also referred to as Biopeptide EL from Sederma, eg Collasyn 6VY from TPI
  • myristoyl hexapeptide-5 eg Collasyn 614VY from TPI
  • myristoyl hexapeptide-6 eg Collasyn 614VG from TPI
  • hexapeptide-8 eg Collasyn 6KS from TPI
  • myristoyl hexapeptide-8 eg Collasyn Lipo-6KS from TPI
  • hexapeptide-9 eg Collaxyl from Vincience
  • hexapeptide-10 eg Collaxyl from Vincience or Seriseline from Lipotec
  • Ala-Arg-His-Leu-Phe-Trp hexapeptide-1
  • acetyl hexapeptide-1 e.g., modulene from Vincience
  • hexapeptide-4 eg Collasyn 6KS of Therapeutic Peptide Inc. (TPI)
  • hexapeptide-5 e.g., Collasyn 6VY from TPI
  • myristoyl hexapeptide-5 e.g., Collasyn 614VY from TPI
  • myristoyl hexapeptide-6 e.g., Collasyn 614VG from TPI
  • Ala-Arg-His-methylnorleucine-homophenylalanine-Trp hexapeptide-7
  • hexapeptide-8 eg Collasyn 6KS from TPI
  • myristoyl hexapeptide-8 eg Collasyn Lipo-6KS from TPI
  • Hexapeptide-9 eg, Collaxyl from Vincience
  • Hexapeptide-10 eg, Collaxyl from Vincience
  • An inventively preferred pentadecapeptide is z.
  • Vinci 01 by Vincience Pentadecapeptide-1).
  • Particularly preferred according to the invention is the combination of N-palmitoyl-Gly-His-Lys and N-palmitoyl-Gly-Gln-Pro-Arg, as obtainable, for example, in the raw material Matrixyl 3000 from Sederma.
  • physiologically acceptable salts of the inventively preferred active ingredients containing acid groups and can form salts are selected from the ammonium, alkali metal, magnesium, calcium, aluminum, zinc and manganese salts. Preferred are the sodium, potassium, magnesium, aluminum, zinc and manganese salts.
  • the polymers of the amino acids and / or the NC 2 -C 24 -acylamino acids are selected from plant and animal protein hydrolysates and / or proteins.
  • Animal protein hydrolysates are z.
  • Vegetable protein hydrolysates eg. Soy, wheat, almonds, peas, potato and rice protein hydrolysates.
  • Corresponding commercial products are z. B. DiaMin® ® (Diamalt) Gluadin ® (Cognis), Lexein ® (Inolex) and Crotein ® (Croda).
  • soy protein hydrolysates e.g.
  • protein hydrolysates may also contain monomeric amino acids and oligopeptides; their composition is usually undefined. Also possible is the use of acyl derivatives of protein hydrolysates, z. In the form of their fatty acid condensation products. Corresponding commercial products are z. B. Lamepon ® (Cognis), Gluadin ® (Cognis), Lexein ® (Inolex), Crolastin ® ® or Crotein (Croda).
  • Cationized protein hydrolysates can also be used according to the invention. Preference is given to cationic protein hydrolysates whose protein content on which they are based has a molecular weight of from 100 to 25,000 daltons, preferably from 250 to 5,000 daltons. Farther are cationic protein hydrolyzates quaternized amino acids and their Gemi ⁇ cal understand. Furthermore, the cationic protein hydrolysates may also be further derivatized.
  • Typical examples of cationic protein hydrolyzates and derivatives used in accordance with the invention are some of those listed under the INCI names in the International Cosmetic Ingredient Dictionary and Handbook, (seventh edition 1997, The Cosmetic, Toiletry, and Fragrance Association 1101 17 th Street, NW Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Steardimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Hydroxypropyl Hydrolyzed Rice Protein, Cocodimium Hydroxypropyl Hydrolyzed Silicon, Cocodimonium Hydroxypropyl Hydrolyzed Soy Protein, Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Cocodimonium Hydroxypropyl Hydrolyzed Wheat Protein, Cocodimonium Hydroxypropyl SiCl Amino Acids, Hydroxypropyl Arginine Lauryl
  • the polymers of the amino acids are selected from DNA repair enzymes.
  • DNA repair enzymes preferred according to the invention are photolyase and T4 endonuclease V, the latter being abbreviated to "T4N5" below. These two enzymes are already known in the art as so-called DNA repair enzymes. DNA repair is defined as the cleavage or removal of UV-induced pyrimidine dimers from the DNA.
  • Photolyase is the abbreviation for deoxyribodipyrimidine photolyase or DNA photolyase, an enzyme with the classification number EC 4.1.99.3.
  • a particularly effi ⁇ tient photolyase comes from Anacystis nidulans, a phototrophic marine microorganism.
  • the photolyase from A. nidulans is now obtained in technically relevant quantities from E. coli.
  • Photolyase relies on light for activation.
  • the enzyme T4 endonuclease V is produced by the denV gene of bacteriophage T4 and belongs to the phosphodiesterases which hydrolytically cleave the nucleic acids at the (5 " -3 " ) bond.
  • T4N5 is also active without the influence of light.
  • compositions according to the invention are characterized in that they contain at least one of the raw materials Photosome TM or Ultrasome TM in a total amount of 0.1-10% by weight, preferably 0.5-5.0% by weight and more preferably 1 , 0 -4.0 wt .-%, each based on the total composition.
  • compositions according to the invention are characterized in that they contain at least one oligomer or polymer of amino acids, NC 2 -C 24 -acylamino acids and / or the esters and / or the physiologically tolerable salts of these substances in a total amount of 0.000001-5 Wt .-%, preferably 0.00001 - 2 wt .-%, particularly preferably 0.0001 - 1 wt .-% and most preferably 0.005 - 0.5 wt .-%, each based on the content of active substance in the whole Composition, included.
  • the monomers, oligomers and polymers of amino acids, NC 2 -C 24 -acylamino acids, the esters and / or the physiologically tolerable salts of these substances are present in supported form, in particular applied to finely divided, pulverulent substrates such as silica gel , in particular Aerosil types, talc, microsponges, modified starches and starch derivatives, crystalline cellulose, cellulose powders, lactoglobulin derivatives, polymer particles of nylon, polyolefins, polycarbonates, polyurethanes, polyacrylates, (meth) acrylate or (meth) acrylate-vinylidene copolymers may be crosslinked, polyesters, polyamides, polystyrenes, Teflon and silicones.
  • a particularly preferred raw material of this type are the Vegetal Filling Spheres of Coletica.
  • compositions according to the invention contain at least one DNA oligonucleotide or an RNA oligonucleotide in addition to the extract of the beans of cocoa (Theobroma cacao) and the extract of the leaves of peppermint (Mentha piperita).
  • an oligonucleotide is understood as meaning polymers of from 2 to 20, preferably from 2 to 10, mononucleotides which, like polynucleotides and nucleic acids, are linked by phosphoric diester bridges.
  • the nucleotides be ⁇ from nucleobases (usually pyrimidine or purine derivatives), pentoses (usually D-ribofuranose or 2-deoxy-D-ribofuranose in ß-N-glycosidic bond to the nucleobase) and phosphoric acid.
  • the mononucleotides are, for example, adenosine phosphates, cytidine phosphates, guanosine phosphates, uridine phosphates and thymidine phosphates, in particular CMP (cytidine 5'-monophosphate), UDP (uridine 5'-diphosphate), ATP (adenosine 5'-triphosphate) and GTP (guanosine 5'-triphosphate).
  • An oligonucleotide particularly preferred according to the invention is the thymidine dinucleotide.
  • compositions according to the invention are characterized in that they contain at least one DNA oligonucleotide or RNA oligonucleotide in a total amount of 0.0001-5 wt.%, Preferably 0.001-1.0 wt.% And particularly preferably 0.01 - 0.5 wt .-%, based on the total composition.
  • compositions according to the invention are characterized in that they contain at least one natural betaine compound in a total amount of 0.05 to 5 wt.%, Preferably 0.1 to 3 wt.%, Particularly preferably 0.5 to 2 wt. in each case based on the total composition.
  • compositions according to the invention comprise at least one vitamin, provitamin or a compound designated as vitamin precursor from the vitamin groups A, B, C, E, H and K and the esters of the abovementioned substances.
  • the group of substances called vitamin A includes retinol (vitamin A 1 ) and 3,4-didehydroretinol (vitamin A 2 ).
  • the ß-carotene is the provitamin of retinol.
  • vitamin A component according to the invention for example, vitamin A acid and its esters, vitamin A aldehyde and vitamin A alcohol and its esters, such as retinyl palmitate and retinyl acetate into consideration.
  • the compositions according to the invention preferably contain the vitamin A component in quantities of 0.05-1% by weight, based on the total composition.
  • the vitamin B group or the vitamin B complex include, among others Vitamin B 1, thiamine trivial name, chemical designation 3 - [(4 '-amino-2'-methyl-5' -pyrimidinyl) methyl] -5- (2-hydroxyethyl) -4-methylthiazolium chloride.
  • Thiamine hydrochloride is preferably used in amounts of from 0.05 to 1% by weight, based on the total composition.
  • Vitamin B 2 common name riboflavin, chemical name 7,8-dimethyl-10- (1-D-ribityl) -benzo [g] pteridine-2,4 (3 / - /, 10 / - /) - dione.
  • Riboflavin or its derivatives are preferably used in amounts of from 0.05 to 1% by weight, based on the total composition.
  • Vitamin B 3 the compounds nicotinic acid and nicotinamide (niacinamide) are performed.
  • Preferred according to the invention is the nicotinic acid amide, which is preferably present in the agents according to the invention in amounts of from 0.05 to 1% by weight, based on the total composition.
  • Vitamin B 5 pantothenic acid and panthenol.
  • Panthenol is preferably used.
  • Derivatives of panthenol which can be used according to the invention are, in particular, the esters and ethers of panthenol and also cationically derivatized panthenols.
  • derivatives of 2-furanone instead of and in addition to pantothenic acid or panthenol, it is also possible to use derivatives of 2-furanone having the general structural formula (I).
  • the substituents R 1 to R 6 independently of one another are a hydrogen atom, a hydroxyl radical, a methyl, methoxy, aminomethyl or hydroxymethyl radical, a saturated or one or two unsaturated, linear or branched C 2 -C 4 -hydrocarbon radical, a saturated or mono- or diunsaturated, branched or linear mono-, di- or trihydroxy-C 2 -C 4 -hydrocarbon radical or a saturated or mono- or diunsaturated one , branched or linear mono-, di- or triamino- Represent C 2 -C 4 hydrocarbon radical.
  • Particularly preferred derivatives are the commercially available substances dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone with the trivial name pantolactone (Merck), 4-hydroxymethyl- ⁇ -butyrolactone (Merck), 3 , 3-dimethyl-2-hydroxy- ⁇ -butyrolactone (Aldrich) and 2,5-dihydro-5-methoxy-2-furanone (Merck), expressly including all stereoisomers.
  • the inventively extraordinarily preferred 2-furanone derivative is pantolactone (dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone), wherein in formula (I) R 1 is a hydroxyl group, R 2 represents a hydrogen atom, R 3 and R 4 represent a methyl group, and R 5 and R 6 represent a hydrogen atom.
  • R 1 is a hydroxyl group
  • R 2 represents a hydrogen atom
  • R 3 and R 4 represent a methyl group
  • R 5 and R 6 represent a hydrogen atom.
  • the stereoisomer (R) -pantolactone is formed during the degradation of pantothenic acid.
  • the said compounds of the vitamin B 5 type and the 2-furanone derivatives are present in the compositions according to the invention in a total amount of 0.05 to 5 wt.%, Preferably 0.1 to 3 wt.%, Particularly preferably 0.5 to 2% by weight, in each case based on the total composition.
  • Vitamin B 6 which is understood hereunder not a uniform substance, but the known under the common names pyridoxine, pyridoxamine and pyridoxal derivatives of 5-hydroxymethyl-2-methylpyridin-3-ol. Vitamin B 6 is preferably present in the compositions according to the invention in amounts of 0.0001 to 1.0% by weight, in particular in amounts of 0.001 to 0.01% by weight.
  • Vitamin B 7 also known as vitamin H or "skin vitamin”.
  • Biotin is (3aS, 4S, 6aR) -2-oxohexahydrothienol [3,4-c / i-imidazole-4-valeric acid.
  • Biotin is preferably present in the compositions according to the invention in amounts of from 0.0001 to 1.0% by weight, in particular in amounts of from 0.001 to 0.01% by weight.
  • the vitamin C group includes vitamin C (ascorbic acid) and its derivatives, in particular the esters of ascorbic acid with organic and inorganic acids and their salts, and also the acetals with glucose or other sugars, in particular ascorbyl glucoside. Vitamin C and / or at least one of its derivatives is preferably used in a total amount of from 0.1 to 3% by weight, based on the total composition.
  • the use of the derivatives ascorbyl palmitate, stearate, dipalmitate, acetate, Mg ascorbyl phosphate, Na ascorbyl phosphate, sodium and magnesium ascorbate, disodium ascorbyl phosphate and sulfate, potassium ascorbyl tocopheryl phosphate, chitosan ascorbate or ascorbyl glucoside may be preferred.
  • the use of at least one member of the vitamin C group in combination with tocopherols and / or other members of the vitamin E group may also be preferred.
  • the vitamin E group includes tocopherol, in particular ⁇ -tocopherol, and its derivatives Deri.
  • Preferred derivatives are in particular the esters, such as tocopheryl acetate, nicotinate, phosphate, succinate, linoleate, oleate, tocophereth-5, tocophereth-10, tocophereth-12, tocophereth-18, tocophereth-50 and tocopherol.
  • Tocopherol and its derivatives are preferably contained in a total amount of 0.05 - 1 wt .-%, based on the total composition.
  • Vitamin F is usually understood as meaning essential fatty acids, in particular linoleic acid, linolenic acid and arachidonic acid.
  • Vitamin H is another name for biotin or vitamin B 7 (see above).
  • the fat-soluble vitamins of the vitamin K group which the backbone of 2-methyl-1, is 4-naphthoquinone based belong phylloquinone (vitamin Ki), quinone Farno- or menaquinone-7 (vitamin K2) and menadione (vitamin K 3 ).
  • Vitamin K is preferably present in amounts of from 0.0001 to 1.0% by weight, in particular from 0.01 to 0.5% by weight, in each case based on the total composition.
  • Vitamin A palmitate (retinyl palmitate), panthenol, pantolactone, nicotinamide, pyridoxine, pyridoxamine, pyridoxal, biotin, ascorbyl palmitate, acetate, Mg ascorbyl phosphate, Na ascorbyl phosphate, sodium and magnesium ascorbate and the tocopherol esters, especially tocopheryl acetate, are particularly preferred according to the invention.
  • compositions according to the invention contain at least one ⁇ -hydroxycarboxylic acid, ⁇ -ketocarboxylic acid or ⁇ -hydroxycarboxylic acid or their ester, lactone or salt form.
  • Preferred ⁇ -hydroxycarboxylic acids or ⁇ -ketocarboxylic acids according to the invention are glycolic acid, lactic acid, tartaric acid, citric acid, 2-hydroxybutanoic acid, 2,3-dihydroxypropanoic acid, 2-hydroxypentanoic acid, 2-hydroxyhexanoic acid, 2-hydroxyheptanoic acid, 2-hydroxyoctanoic acid, 2-hydroxydecanoic acid, 2-hydroxydodecanoic acid, 2-hydroxytetradecanoic acid, 2-hydroxyhexadecanoic acid, 2-hydroxyoctadecanoic acid, mandelic acid, 4-hydroxymandelic acid, malic acid, erythraric acid, threaric acid, glucaric acid, galactaric acid, mann
  • Particularly preferred ⁇ -hydroxycarboxylic acids are lactic acid, citric acid, glycolic acid and gluconic acid.
  • a particularly preferred ⁇ -hydroxycarboxylic acid is salicylic acid.
  • the esters of said acids are preferably selected from the methyl, ethyl, propyl, isopropyl, butyl, amyl, pentyl, hexyl, 2-ethylhexyl, octyl, decyl, dodecyl and hexadecyl esters.
  • compositions according to the invention are characterized in that at least one ⁇ -hydroxycarboxylic acid, ⁇ -ketocarboxylic acid and / or ⁇ -hydroxycarboxylic acid and / or at least one derivative thereof are present in a total amount of 0.1-10% by weight. , Preferably 0.5 to 5 wt .-%, in each case based on the total composition, is contained.
  • compositions according to the invention contain at least one flavonoid or at least one flavonoid-rich plant extract.
  • the flavonoids preferred according to the invention include the glycosides of the flavones, the flavanones, the 3-hydroxyflavones (flavonols), the aurones and the isoflavones.
  • Particularly preferred flavonoids are selected from naringin (aurantiin, Na ⁇ ngenin-7-rhamnoglucosid), ⁇ -glucosylrutin, ⁇ -glucosylmyricetin, ⁇ -glucosylisoquercetin, ⁇ -glucosyl-cerecetin, isoquercitrin (quercetin-3-O- ⁇ -D-glucofuranoside ), Hesperidin (3 ', 5,7-trihydroxy-4'-methoxyflavanone-7-rhamnoglucoside, hesperetin-7-O-rhamnoglucoside), neohesperidin, rutin (S.S'''. ⁇ J-pentahydroxyflavone-S
  • Vitexin isovitexin, vicenin-2, shankoside, isoschaftoside and luteolin.
  • Extremely preferred flavonoids according to the invention are ⁇ -glucosylrutin, naringin, apigenin-7-glucoside, ⁇ -glucosylquercetin, isoquercitrin and orientin.
  • the constructed from two flavonoid biflavonoids, z. B. occur in gingko species.
  • Other preferred flavonoids are the chalcones, especially phloricin, neohesperidin dihydrochalcone, aspalathin and nothofagin.
  • compositions according to the invention are characterized in that at least one flavonoid and / or at least one flavonoid-rich plant extract in a total amount of 0.0001 to 1 wt .-%, preferably 0.0005 to 0.5 wt .-% and particularly preferably 0.001 to 0.1 wt .-%, each based on the flavonoid active substance in the total composition is included.
  • the compositions according to the invention contain at least one isoflavonoid or at least one isoflavonoid-rich plant extract. The isoflavones and the isoflavone glycosides are counted at this point as isoflavonoids.
  • isoflavones are to be understood as meaning substances which are hydrogenation, oxidation or substitution products of 3-phenyl-4H-1-benzopyran, hydrogenation of which may be in the 2,3-position of the carbon skeleton, oxidation under Formation of a carbonyl group in the 4-position may be present, and by substitution of the replacement of one or more hydrogen atoms by hydroxy or methoxy groups to understand.
  • the isoflavones preferred according to the invention include, for example, daidzein, genistein, prunetin, biochanin, orobol, santal, pratense, irigenin, glycitein, biochanin A and formononetin.
  • isoflavones are daidzein, genistein, glycitein and formononetin.
  • the isoflavones are glycosidically linked to at least one sugar via at least one hydroxy group.
  • Suitable sugars are mono- or oligosaccharides, in particular D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and rutinose.
  • Particularly preferred isoflavone glycosides according to the invention are daidzin and genistin.
  • the isoflavones and / or their glycosides are contained in the preparations as constituents of a substance mixture obtained from a plant, in particular a vegetable extract.
  • a vegetable substance mixtures can be obtained, for example, by pressing or extracting from plants such as soy, in particular from the soybean seeds, red clover or chickpeas, in a manner familiar to the person skilled in the art.
  • Particular preference is given to using isoflavones or isoflavone glycosides in the form of soya-derived extracts in the preparations according to the invention, as described, for example, under the product name Soy Protein Isolate SPI (Protein Technology International, St.
  • apple seed extract contains phytohormones, isoflavonoids, phytosterols, triterpenoids, tocopherols and natural waxes.
  • compositions according to the invention are characterized in that at least one isoflavonoid and / or at least one isoflavonoid richer Plant extract in a total amount of 0.00001 to 1 wt .-%, preferably 0.0005 to 0.5 wt .-% and particularly preferably 0.001 to 0.1 wt .-%, each based on the Isoflavonoiditsubstanz in the total composition, is included.
  • compositions according to the invention additionally comprise at least one polyphenol or a polyphenol-rich plant extract.
  • polyphenols are aromatic compounds which contain at least two phenolic hydroxyl groups in the molecule. These include the three dihydroxybenzenes catechol, resorcinol and hydroquinone, as well as phloroglucin, pyrogallol and hexahydroxybenzene.
  • free and etherified polyphenols occur, for example, in floral dyes (anthocyanidins, flavones), in tannins (catechins, tannins), as lichen or fern ingredients (usnic acid, acyl polyphenols), in lignins and as gallic acid derivatives , Preferred polyphenols are flavones, catechols, usnic acid, and tannins are the derivatives of gallic acid, digallic acid and digalloylgallic acid.
  • Particularly preferred polyphenols are the monomeric catechins, that is, the derivatives of flavan-3-ols, and leucoanthocyanidins, that is, the derivatives of leucoanthocyanidins which preferably carry phenolic hydroxyl groups in the ⁇ , ⁇ '' position, preferably epicatechin and epigallocatechin, and the resulting by self-condensation tannins.
  • Such tannins are preferably not used in isolated pure substance but as extracts of tannin-rich plant parts, eg. Extracts of catechu, quebracho, oak bark and pine bark, as well as other tree bark, leaves of green tea (camellia sinensis) and mate. Also particularly preferred are the tannins.
  • a particularly preferred polyphenol-rich cosmetic active ingredient is the commercial product Sepivinol R, an extract of red wine, available from Seppic.
  • Another particularly preferred polyphenol-rich cosmetic active ingredient is the commercial product Crodarom Chardonnay, an extract from the kernels of the Chardonnay grape, obtainable from Croda.
  • compositions according to the invention are characterized in that at least one polyphenol and / or at least one polyphenol-rich plant extract are present in a total amount of 0.001 to 10% by weight, preferably 0.005 to 5% by weight and more preferably 0.01 to 3 wt .-%, in each case based on the Polyphe- noleptsubstanz in the entire composition.
  • the compositions according to the invention comprise at least one ubiquinone or a ubiquinol or derivatives thereof.
  • Ubiquinols are the reduced form of ubiquinones.
  • the preferred ubiquinones according to the invention have the formula (II):
  • ubiquinone of formula (II) with n 10, also known as coenzyme Q10.
  • compositions according to the invention are characterized in that at least one ubiquinone and / or at least one ubiquinol and / or at least one derivative of these substances in a total amount of 0.0001 to 1 wt .-%, preferably 0.001 to 0.5 wt. % and more preferably 0.005 to 0.1% by weight, in each case based on the total composition.
  • compositions according to the invention contain at least one naturally occurring xanthine derivative, in particular a naturally occurring di- or trialkylxanthine, preferably selected from caffeine, theophylline, theobromine and aminophylline.
  • compositions according to the invention are characterized in that they contain at least one naturally occurring xanthine derivative in a total amount of 0.0001 to 1% by weight, preferably 0.001 to 0.5% by weight and more preferably 0.005 to 0.1% by weight. %, in each case based on the total composition.
  • compositions according to the invention contain ectoine.
  • Ectoin is the common name for 2-methyl-1, 4,5,6-tetrahydro- pyrimidin-4-carboxylate.
  • Particularly preferred compositions according to the invention are characterized in that ectoine is used in amounts of from 0.0001 to 1% by weight, preferably from 0.001 to 0.5% by weight and particularly preferably from 0.005 to 0.01% by weight, in each case on the entire composition, is included.
  • compositions according to the invention contain at least one inorganic and / or at least one organic UV filter substance.
  • the UV filter substances are liquids which are liquid or crystalline at room temperature and are capable of absorbing ultraviolet rays and of absorbing the absorbed energy in the form of longer-wave radiation, eg. B. to give off heat again.
  • the UVA and UVB filters can be used individually or in mixtures. The use of filter mixtures is preferred according to the invention.
  • the organic UV filters used according to the invention are selected from the derivatives of dibenzoylmethane, cinnamic acid esters, diphenylacrylic acid esters, benzophenone, camphor, p-aminobenzoic acid esters, o-aminobenzoic acid esters, salicylic acid esters, benzimidazoles, symmetrically or asymmetrically substituted 1,3,5-triazines, mono ⁇ mers and oligomeric 4,4-Diarylbutadiencarbonklareestern and -carbonklareamiden, Ketotricyclo (5.2.1.0) decane, Benzalmalonklaestern, benzoxazole and any mixtures of the above components.
  • the organic UV filters can be oil-soluble or water-soluble.
  • the benzoxazole derivatives are advantageously present in dissolved form in the cosmetic preparations according to the invention. However, it may also be advantageous if the benzoxazole derivatives are present in a pigmentary, ie undissolved form, for example in particle sizes of 10 nm to 300 nm.
  • oil-soluble UV filters are 1- (4-tert-butylphenyl) -3- (4'-methoxyphe- nyl) propane-1, 3-dione (Parsol ® 1789), 1-phenyl-3- (4 '-isopropylphenyl) propane-1, 3-dione, 3- (4 * methylbenzylidene) -D, L-camphor, 4- (dimethylamino) benzoic acid 2-ethylhexyl ester, 4- (dimethylamino) benzoic acid 2-octyl ester Ethyl 4- (dimethylamino) benzoate, 2-ethylhexyl 4-methoxycinnamate, propyl 4-methoxycinnamate, isopentyl 4-methoxycinnamate, 2-ethylhexyl 2-cyano-3,3-phenylcinnamate (octocrylene), salicylic acid-2 ethylhexyl
  • Preferred water-soluble UV filters are 2-phenylbenzimidazole-5-sulfonic acid, phenylene-1, 4-bis (2-benzimidazyl) -3,3'-5,5'-tetrasulfonic acid and its alkali metal, alkaline earth metal, Ammonium, alkylammonium, alkanolammonium and glucammonium salts, in particular the sulfonic acid itself with the INCI name phenylbenzimidazole sulfonic acid (CAS No.
  • Neo Heliopan AP sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts, sulfonic acid derivatives of Benzylidencamphers, such as.
  • UV-A filter 1- (4-tert-butylphenyl) -3- (4'methoxyphenyl) propane-1, 3-dione (z. B. Parsol ® 1789) can for example be different in ver ⁇ UV Make -B filters.
  • compositions according to the invention contain 1- (4-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1,3-dione in combination with at least one UV-B filter of 4-methoxycinnamic acid 2-ethylhexyl ester, 2-cyano-3,3-phenylcinnamic acid 2-ethylhexyl ester, 2-ethylhexyl salicylate and 3,3,5-trimethylcyclohexylsalicylate.
  • the weight ratio of UV-B filter to 1- (4-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1,3-dione is between 1: 1 and 10: 1, preferably between 2: 1 and 8: 1, the molar ratio being between 0.3 and 3.8, preferably between 0.7 and 3.0.
  • the inventively preferred inorganic photoprotective pigments are finely dispersed or colloidally disperse metal oxides and metal salts, for example titanium dioxide, zinc oxide, iron oxide, aluminum oxide, cerium oxide, zirconium oxide, silicates (talc) and barium sulfate.
  • the particles should have an average diameter of less than 100 nm, preferably between 5 and 50 nm and in particular between 15 and 30 nm, so-called nanopigments. They may have a spherical shape, but it is also possible to use those particles which have an ellipsoidal or otherwise deviating shape from the spherical shape.
  • the pigments can also be surface-treated, ie hydrophilized or hydrophobized.
  • Typical examples are coated titanium dioxides, such as. Example, titanium dioxide T 805 (Degussa) or Eusolex ® T2000 (Merck).
  • Suitable hydrophobic coating agents are in particular silicones and in particular trialkoxyoctylsilanes or simethicones. Particularly preferred are titanium dioxide and zinc oxide.
  • compositions according to the invention are characterized in that they contain at least one organic UV filter substance in a total amount of 0.1-30% by weight, preferably 0.5-20% by weight, more preferably 1.0-0.0% by weight. % and most preferably 2 or 3 - 7 wt .-%, each based on the total composition.
  • compositions according to the invention are characterized in that they comprise at least one inorganic UV filter substance in a total amount of 0.1-15% by weight, preferably 0.5-10% by weight, more preferably 1-5% by weight and extraordinarily preferably 2 to 4% by weight, based in each case on the total composition.
  • compositions according to the invention contain at least one self-tanning active ingredient.
  • Self-tanning active ingredients preferred according to the invention are selected from dihydroxyacetone and erythrulose.
  • Preferred compositions according to the invention are characterized in that they contain at least one self-tanning active ingredient in a total amount of 0.1-15% by weight, preferably 0.5-10% by weight, more preferably 1.0-0.5% by weight. % and most preferably 2.0 to 4.0 wt .-%, each based on the total composition.
  • compositions according to the invention comprise at least one skin-lightening active ingredient.
  • preferred skin lightening agents are selected from ascorbic acid, the esters of ascorbic acid with phosphoric acid and / or organic C 2 -C 2 o-carboxylic acids and their alkali and alkaline earth metal salts, kojic acid, hydroquinone, arbutin, Maulbeerbaum ⁇ thereof extract and licorice extract and mixtures thereof. Both as a single substance and as a mixture, the ascorbic acid derivatives and kojic acid are preferred.
  • the invention exceptionally preferred ascorbic acid derivatives are sodium ascorbyl phosphate and magnesium ascorbyl phosphate.
  • compositions according to the invention are characterized in that they contain at least one skin-lightening active ingredient in a total amount of from 0.05 to 5% by weight, preferably from 0.1 to 2% by weight, in each case based on the total composition.
  • a further subject matter of the present invention is the use of a cosmetic and / or dermatological topical composition which, in a suitable carrier, comprises at least one active ingredient which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active ingredient which which stimulates cutaneous synthesis of neuromediators, for the non-therapeutic, cosmetic treatment of sensitive skin, dry skin, atopic dermatitis, aging skin, UV-damaged skin and / or irritated skin.
  • a further subject matter of the present invention is the use of a cosmetic and / or dermatological topical composition which, in a suitable carrier, comprises at least one active ingredient which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active ingredient which which stimulates the cutaneous synthesis of neuromediators, for the preparation of an agent for the therapeutic treatment of sensitive skin, dry skin, atopic dermatitis, aging skin, UV-damaged skin and / or irritated skin.
  • a further subject matter of the present invention is a process for the non-therapeutic cosmetic skin treatment, in which a cosmetic or dermatological topical composition comprising at least one active ingredient in a suitable carrier, the prostaglandin synthesis and / or the leukotriene synthesis inhibited and at least one drug that stimulates the cutaneous synthesis of neuromediators, is applied to the skin, especially the facial skin.
  • compositions according to the invention contain, in addition to at least one active ingredient which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active substance which stimulates the cutaneous synthesis of neuromediators, furthermore at least one conditioning agent.
  • conditioning active ingredients is understood to mean those substances which are applied to keratinic materials, in particular to the skin, and which improve physical and sensory properties. Conditioners smooth the top layer of the skin and make it soft and supple.
  • Conditioning agents which are preferred according to the invention are selected from fatty substances, in particular vegetable oils, such as sunflower oil, olive oil, soybean oil, rapeseed oil, almond oil, jojoba oil, orange oil, wheat germ oil, peach kernel oil and the liquid portions of coconut oil, lanolin and its derivatives, liquid paraffin oils, isoparaffin oils and synthetic hydrocarbons, di-n-alkyl ethers having a total of 12 to 36 carbon atoms, z. B.
  • vegetable oils such as sunflower oil, olive oil, soybean oil, rapeseed oil, almond oil, jojoba oil, orange oil, wheat germ oil, peach kernel oil and the liquid portions of coconut oil, lanolin and its derivatives, liquid paraffin oils, isoparaffin oils and synthetic hydrocarbons, di-n-alkyl ethers having a total of 12 to 36 carbon atoms, z.
  • fatty acids especially linear and / or branched, saturated and / or unsaturated C 8-3 o fatty acids
  • fatty alcohols especially saturated, mono- or polyunsaturated , branched or unbranched fatty alcohols having 4 to 30 carbon atoms, which may be ethoxylated with 1 to 75, preferably 5 to 20 ethylene oxide units and / or propoxylated with 3 to 30, preferably 9 to 14 propylene oxide units
  • ester oils ie esters of C 6 - 30 fatty acids with C 2-3 pick o-fatty alcohol, Hydroxycarbonklarealkylestem, dicarboxylic acid esters of di-n-butyl adipate and diol esters such as Ethylenglykoldioleat or propylene glycol di (2-ethylhexanoate), symmetri ⁇ rule, asymmetrical or
  • glycerol carbonate or dicaprylyl As glycerol carbonate or dicaprylyl (Cetiol ® CC), mono, - di- and Trifettkla- esters of saturated and / or unsaturated linear and / or branched fatty acids with glycerol, which are ethoxylated with 1-10, preferably 7-9 ethylene oxide units kön ⁇ nen, z.
  • phospholipids for example, soybean lecithin, egg lecithin and cephalins, silicone compounds selected from decamethylcyclopentasiloxane, Dodecamethylcyclohexasiloxan and silicone polymers, which can be cross-linked if desired, z. B.
  • the amount of fatty substances used is preferably 0.1-50% by weight, more preferably 0.1-20% by weight, and most preferably 0.1-15% by weight, based in each case on the entire composition.
  • the cosmetic or dermatological compositions according to the invention are in the form of a liquid, flowable or solid oil-in-water emulsion, water-in-oil emulsion, multiple emulsion, in particular an oil-in-water-in-oil.
  • the agents may also be presented in anhydrous form, such as, for example, an oil or a balm.
  • the carrier may be a vegetable or animal oil, a mineral oil, a synthetic oil or a mixture of such oils.
  • the compositions are present as a microemulsion.
  • microemulsions are understood as meaning not only the thermodynamically stable microemulsions but also the so-called "PIT" emulsions.
  • PIT phase inversion temperature
  • These emulsions are systems with the 3 components water, oil and emulsifier which are present at room temperature as an oil-in-water emulsion. Upon heating of these systems, they form in a specific temperature range (as phase inversion temperature or " PIT ”) denotes microemulsions which, on further heating, convert to water-in-oil emulsions.
  • O / W emulsions are again formed, but they are also present at room temperature as microemulsions or as very finely divided emulsions having an average particle diameter of less than 400 nm and in particular of about 100-300 nm. According to the invention, those micro- or "PIT" emulsions may be preferred which have an average particle diameter of about 200 nm.
  • the compositions according to the invention contain at least one surface-active substance as emulsifier or dispersant.
  • Suitable emulsifiers are for example adducts of from 4 to 30 mol ethylene oxide and / or 0 to 5 mol propylene oxide onto linear C 8 -C 22 fatty alcohols, on C 12 - C 22 fatty acids and C 8 -C 15 alkylphenols, C 12 - C 22 -fatty acid mono- and diesters of addition products of 1 to 30 moles of ethylene oxide onto C 3 -C 6 -polyols, in particular to glycerol, ethylene oxide and polyglycerol addition products of methylglucoside fatty acid esters, fatty acid alkanolamides and fatty acid glucamides, C 8 -C 22 alkyl mono- and - oligoglycosides and their ethoxylated analogues, wherein degrees of oligomerization of 1, 1 to 5, in particular 1, 2 to 2.0, and glucose are preferred as the sugar component, mixtures of alkyl (oligo) -glucosiden and fatty
  • the agents according to the invention preferably contain the emulsifiers in amounts of 0.1 to 25% by weight, in particular 0.5 to 15% by weight, based on the total agent.
  • at least one nonionic emulsifier having an HLB value of 8 and below is included.
  • Behenyl alcohol and arachidyl alcohol which preferably form lamellar oil-in-water emulsions
  • emulsifiers with an HLB value of 8 and below are the adducts of 1 or 2 moles of ethylene oxide or propylene oxide with behenyl alcohol, erucyl alcohol, arachidyl alcohol or behenic acid or erucic acid.
  • the monoesters of C 16 -C 30 fatty acids with polyols such as.
  • pentaerythritol trimethylolpropane, diglycerol, sorbitol, glucose or methyl glucose. Examples of such products are z. Sorbitan mono- behenate or pentaerythritol monoerucate.
  • thickeners for.
  • B. natural and synthetic clays and phyllosilicates such as bentonite, hectorite, montmorillonite or Laponite ® , or anionic polymers of acrylic acid, methacrylic acid, crotonic acid, maleic anhydride and 2-acrylamido-2-methylpropanesulfonic acid, wherein the acidic groups wholly or partly as sodium , Potassium, ammonium, mono- or triethanolammonium salt, and wherein at least one nonionic monomer may be contained.
  • Preferred nonionic monomers are acrylamide, methacrylamide, acrylates, methacrylates, vinylpyrrolidone, vinyl ethers and vinyl esters.
  • Preferred anionic copolymers are acrylic acid-acrylamide copolymers and in particular polyacrylamide copolymers with monomers containing sulfonic acid groups. These copolymers can also be networked. Suitable commercial products are Sepigel ® 305 Simulgel® ® 600, Simulgel® ® NS and Simulgel® ® EC SEPPIC. More particularly Brad ⁇ ferred anionic homo- and copolymers are uncrosslinked and crosslinked polyacrylic ren. Such compounds are for example the commercial products Carbopol ®.
  • a particularly preferred anionic copolymer contains 80 to 98% of an unsaturated, optionally substituted C 3-6 -carboxylic acid or its anhydride as well as 2 to 20%, if desired, substituted acrylic acid esters of saturated C 10 -3 o-carboxylic acid. acids, wherein the copolymer may be crosslinked with the aforementioned crosslinking agents.
  • Corresponding commercial products are Pemulen ® and Carbopol ® grades 954, 980, 1342 and ETD 2020 (ex BF Goodrich).
  • Suitable nonionic polymers include polyvinyl alcohols, which may be partially saponified, for.
  • polyvinyl alcohols which may be partially saponified, for.
  • Mowiol ® and Vinylpyrrolidon ⁇ / inylester copolymers and polyvinylpyrrolidones the z. B. under the trademark Luviskol ® (BASF) ver ⁇ be driven.
  • antioxidants are antioxidants, preservatives, solvents such as ethanol, isopropanol, ethylene glycol, propylene glycol, propylene glycol, glycerol and diethylene glycol, adsorbents and fillers such as talc and Veegum ®, perfume oils, pigments and dyes for coloring the composition, substances position suitability for adjusting the pH, complexing agents such as EDTA, NTA, ⁇ -alaninediacetic acid and phosphonic acids, propellants such as propane-butane mixtures, pentane, isopentane, isobutane, N 2 O, dimethyl ether, CO 2 and air.
  • solvents such as ethanol, isopropanol, ethylene glycol, propylene glycol, propylene glycol, glycerol and diethylene glycol
  • adsorbents and fillers such as talc and Veegum ®
  • perfume oils pigments and dyes for coloring the composition
  • keratinocyte cultures were each mixed with an aqueous solution of 1% by weight or 5% by weight of the raw material source to be investigated for 24 hours.
  • the produced ⁇ -endorphin content was determined with the aid of an enzyme immunoassay kit ( ⁇ -endorphin human, EIA kit from Phoenix Pharmaceuticals) in the culture medium.
  • the enzyme 5-lipoxygenase catalyses the conversion of arachidonic acid into the leucotrienes LTB 4 , LTC 4 , LTD 4 and LTE 4 .
  • Leukotrienes are mediators in inflammatory and allergic reactions of granulocytes, mast cells, monocytes and macrophages. Also in the keratinocytes of the skin leukotrienes are formed in inflammatory reactions. Accordingly, inhibitors of leukotriene synthesis can have an antiinflammatory or skin-calming effect.
  • the 5-lipoxygenase was differentiated from human leukemia cell lines by addition of dimethylsulfoxide (DMSO), TGF- ⁇ 1 (transforming growth factor ⁇ 1) and dihydroxyvitamin D3 and simultaneously induced 5-lipoxygenase. After 4 days in the differentiation medium, the cells were harvested, taken up in a glucose-containing PBS buffer and disrupted by sonication. Larger Zell rave ⁇ parts were centrifuged off at 100 000 g, with 5-lipoxigenase remaining in the supernatant.
  • DMSO dimethylsulfoxide
  • TGF- ⁇ 1 transforming growth factor ⁇ 1
  • dihydroxyvitamin D3 dihydroxyvitamin D3
  • the determination of the 5-üpoxygenase inhibitory activity was carried out according to Werz et al., Naunyn-Schmiedeberg's Arch. Pharmacol., 1997, Vol. 456, 441-445.
  • the supernatant from the 5-lipoxygenase production were adenosine triphosphate (ATP) and the added to testing raw materials. In the present case, 100 ⁇ g of raw material was used as it is per milliliter of supernatant.
  • the solvents used were, depending on the substance, water, ethanol, DMSO or chloroform.
  • the batches were preincubated for 30 seconds at 37 ° C. Subsequently, the 5-lipoxygenase reaction was started by addition of arachidonic acid. After 10 minutes reaction time, the reaction was stopped by addition of methanol. The leukotrienes produced by the action of 5-lipoxygenase on arachidonic acid were quantified by HPLC.
  • Oil-in-water emulsions 1. Skin creams
  • compositions for soaking wipes are examples of compositions for soaking wipes.
  • Example 1 illustrates a lotion composition for a lotion and make-up remover cloth.
  • Example 2 illustrates a soak composition for a self-tanner cloth.
  • Example 3 illustrates a soak composition for a sunscreen cloth.
  • Example 4 illustrates a soak composition for a facial cleansing wipe.

Abstract

The invention relates to topical compositions containing, in a suitable carrier, at least one active substance, which inhibits the synthesis of prostaglandin and/or of leukotriene, and at least one active substance that stimulates the cutaneous synthesis of neuromediators.

Description

Zusammensetzungen mit Inhibitoren der Prostaglandin- und/oder Leukotrien-Synthese in Kombination mit Stimulatoren der Freisetzung kutaner NeuromediatorenCompositions with inhibitors of prostaglandin and / or leukotriene synthesis in combination with stimulants of the release of cutaneous neuromediators
Gegenstand der vorliegenden Erfindung sind topische kosmetische und/oder dermatologische Zusammensetzungen zur Behandlung empfindlicher und/oder trockener Haut, zur Behandlung der atopischen Dermatitis und/oder zur Behandlung sensorischer Irritationen und Hautentzündungen der Altershaut.The present invention relates to topical cosmetic and / or dermatological compositions for the treatment of sensitive and / or dry skin, for the treatment of atopic dermatitis and / or for the treatment of sensory irritations and skin inflammations of the aging skin.
Als Reaktion auf Umweltreize können in der menschlichen Haut nicht nur Entzündungs¬ mechanismen (Bildung von Erythemen), sondern gleichzeitig auch sensorische Irritatio¬ nen, wie z. B. Juckreiz, Brennen oder Stechen, ausgelöst werden. Diese Hautreaktionen basieren auf unterschiedlichen molekularen Mechanismen. Die gleichzeitige Linderung des (entzündeten) Hautzustandes und sensorischer Irritationen bei empfindlicher Haut, trockener Haut oder bei atopischer Dermatitis stellt ein derzeit nur ungenügend gelöstes Problem dar. Die Tendenz zu sensorischen Irritationen und Hautentzündungen ist im Alter verstärkt vorhanden. Auch bei der trockenen Haut treten häufig sensorische Irritati¬ onen wie Spannungsgefühle und Juckreiz in Verbindung mit entzündlichen Hautirritatio¬ nen auf. Die Behandlung dieser Erscheinungsformen der Altershaut und der trockenen Haut ist ein bislang ebenfalls nur ungenügend gelöstes Problem. Die im Stand der Technik bekannten Mittel zur Behandlung empfindlicher Haut, trocke¬ ner Haut, atopischer Dermatitis oder sensorischer Irritationen und Hautentzündungen der Altershaut zielen bislang entweder nur auf eine Entzündungshemmung oder aber nur auf eine Juckreizminderung beziehungsweise allgemein nur auf eine Minderung sensori¬ scher Irritationen ab. Zusammensetzungen zur gleichzeitigen Entzündungshemmung und Minderung sensorischer Irritationen sind im Stand der Technik bisher nicht bekannt.In response to environmental stimuli, not only inflammatory mechanisms (formation of erythema) in the human skin, but at the same time also sensory irritations, such as, for example, As itching, burning or stinging, are triggered. These skin reactions are based on different molecular mechanisms. The simultaneous alleviation of the (inflamed) skin condition and sensory irritations in sensitive skin, dry skin or in atopic dermatitis represents a currently insufficiently solved problem. The tendency to sensory irritation and dermatitis is increasingly present in old age. Also in the case of dry skin, sensory irritations such as feelings of tension and itching often occur in connection with inflammatory skin irritations. The treatment of these manifestations of aging skin and dry skin is a hitherto also insufficiently solved problem. The means known in the state of the art for the treatment of sensitive skin, dry skin, atopic dermatitis or sensory irritations and skin inflammations of the aging skin have hitherto either aimed only at inhibiting the inflammation or else only at reducing itching or generally only at reducing sensory irritations , Compositions for the simultaneous inflammation inhibition and reduction of sensory irritations are not known in the prior art.
Aufgabe der vorliegenden Erfindung war es, Zusammensetzungen zur Behandlung emp¬ findlicher und/oder trockener Haut mit gegenüber dem Stand der Technik verbesserter Wirksamkeit zu entwickeln, die sowohl Entzündungsmechanismen hemmen als auch sensorische Irritationen, wie z. B. Juckreiz, mindern. Eine weitere Aufgabe der vorliegen- den Erfindung war es, Zusammensetzungen zur Behandlung der atopischen Dermatitis mit gegenüber dem Stand der Technik verbesserter Wirksamkeit zu entwickeln, die so¬ wohl Entzündungsmechanismen hemmen als auch sensorische Irritationen, wie z. B. Juckreiz, mindern. Eine weitere Aufgabe der vorliegenden Erfindung war es, Zusam¬ mensetzungen zur Behandlung sensorischer Irritationen und Hautentzündungen der Altershaut mit gegenüber dem Stand der Technik verbesserter Wirksamkeit zu entwic¬ keln, die sowohl Entzündungsmechanismen hemmen als auch sensorische Irritationen, wie z. B. Juckreiz, mindern.The object of the present invention was to develop compositions for the treatment of sensitive and / or dry skin with improved effectiveness compared to the prior art, which both inhibit inflammatory mechanisms and sensory irritations, such as, for example. As itching, reduce. Another task of the present The invention was to develop compositions for the treatment of atopic dermatitis with respect to the prior art improved efficacy, which inhibit both inflammatory mechanisms and sensory irritations, such as. As itching, reduce. A further object of the present invention was to develop compositions for the treatment of sensory irritations and skin inflammations of the aging skin with improved efficacy compared with the prior art, which inhibit both inflammatory mechanisms and sensory irritations, such as, for example, As itching, reduce.
Überraschend wurde nun gefunden, dass die vorgenannten Aufgaben durch Zusammen¬ setzungen gelöst werden können, die mindestens einen Wirkstoff, der Entzündungs¬ mechanismen hemmt, und mindestens einen Wirkstoff, der sensorische Irritationen min¬ dert, enthalten. Im Stand der Technik bekannte Mittel zeigen nur partielle Effekte auf ein¬ zelne Hautreaktionen. Dagegen vereint die vorliegende Erfindung erstmals antiirritative Wirkungen mit einer gleichzeitigen nachhaltigen Linderung sensorischer Irritationen. Weiterhin wurde überraschend gefunden, dass sich die unterschiedlichen Wirkstofftypen in synergistischer Weise ergänzen können.Surprisingly, it has now been found that the abovementioned objects can be achieved by compositions which contain at least one active substance which inhibits inflammatory mechanisms and at least one active substance which minimizes sensory irritations. Known in the prior art agents show only partial effects on ein¬ individual skin reactions. By contrast, the present invention for the first time combines anti-irritative effects with a simultaneous, lasting alleviation of sensory irritations. Furthermore, it was surprisingly found that the different types of drugs can complement each other in a synergistic manner.
Gegenstand der vorliegenden Erfindung sind kosmetische und/oder dermatologische topische Zusammensetzungen, die in einem geeigneten Träger mindestens einen Wirk¬ stoff, der die Prostaglandin-Synthese und/oder die Leukotrien-Synthese inhibiert und mindestens einen Wirkstoff, der die kutane Synthese von Neuromediatoren stimuliert, enthalten. Überraschenderweise hat sich gezeigt, dass diese spezifische Wirkstoffkom¬ bination in besonderer Weise zur Pflege und Behandlung der Haut, insbesondere der empfindlichen Haut, der trockenen Haut und/oder der atopischen Haut sowie der Alters¬ haut, geeignet ist.The present invention relates to cosmetic and / or dermatological topical compositions which, in a suitable carrier, contain at least one active substance which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active substance which stimulates the cutaneous synthesis of neuromediators. contain. Surprisingly, it has been found that this specific combination of active substances is particularly suitable for the care and treatment of the skin, in particular the sensitive skin, the dry skin and / or the atopic skin as well as the aged skin.
In einer bevorzugten Ausführungsform der vorliegenden Erfindung ist der die Prostaglan¬ din-Synthese inhibierende Wirkstoff ausgewählt aus Wirkstoffen, die das Enzym Cyclo- oxygenase inhibieren. Im Sinne der vorliegenden Erfindung kann unter der Inhibierung der Cyclooxygenase sowohl eine Senkung der Menge dieses Enzyms als auch eine Minderung seiner Aktivität sowie beides hiervon verstanden werden. In einer weiteren bevorzugten Ausführungsform der vorliegenden Erfindung ist der die Prostaglandin-Synthese inhibierende Wirkstoff ausgewählt aus Wirkstoffen, die die Aus¬ schüttung von Interleukinen, insbesondere von lnterleukin-1-alpha, inhibieren. In einer bevorzugten Ausführungsform der vorliegenden Erfindung ist der die Leukotrien- Synthese inhibierende Wirkstoff ausgewählt aus Wirkstoffen, die das Enzym 5-Lipoxyge- nase inhibieren. Im Sinne der vorliegenden Erfindung kann unter der Inhibierung der 5- Lipoxygenase sowohl eine Senkung der Menge dieses Enzyms als auch eine Minderung seiner Aktivität sowie beides hiervon verstanden werden.In a preferred embodiment of the present invention, the active ingredient inhibiting the prostaglandin synthesis is selected from active substances which inhibit the enzyme cyclooxygenase. For the purposes of the present invention, the inhibition of cyclooxygenase can be understood as meaning both a reduction in the amount of this enzyme and a reduction in its activity, as well as both. In a further preferred embodiment of the present invention, the active ingredient which inhibits prostaglandin synthesis is selected from active compounds which inhibit the secretion of interleukins, in particular of interleukin-1-alpha. In a preferred embodiment of the present invention, the active substance inhibiting leukotriene synthesis is selected from active substances which inhibit the enzyme 5-lipoxygenase. For the purposes of the present invention, the inhibition of 5-lipoxygenase can be understood as meaning both a reduction in the amount of this enzyme and a reduction in its activity, as well as both.
In einer weiteren bevorzugten Ausführungsform der vorliegenden Erfindung ist der die kutane Synthese von Neuromediatoren stimulierende Wirkstoff ausgewählt aus Wirkstof¬ fen, die die ß-Endorphin-Synthese in Keratinozyten stimulieren.In a further preferred embodiment of the present invention, the active substance stimulating the cutaneous synthesis of neuromediators is selected from active substances which stimulate β-endorphin synthesis in keratinocytes.
Erfindungsgemäß bevorzugte Inhibitoren der Prostaglandin-Synthese, insbesondere Inhibitoren der Cyclooxygenase und/oder der Interleukin-Ausschüttung, sind ausgewählt aus Silymarin, das besonders bevorzugt in liposomenverkapselter Form eingesetzt wird (erhältlich z. B. unter der Handelsbezeichnung Silymarin Phytosome (INCI: Silybum Marianum Extract and Phospholipids) von der Firma lndena SpA. Silymarin stellt ein früher als einheitliche Substanz angesehenes Wirkstoff-Konzentrat aus den Früchten der Mariendistel (Silybum marianum) dar. Die Hauptbestandteile des Silymarins sind Silybin (Silymarin I), Silychristin (Silymarin II) und Silydianin, die zur Gruppe der Flavanolignane gehören. Weitere erfindungsgemäß bevorzugte Inhibitoren der Prostagladin-Synthese, insbesondere Inhibitoren der Cyclooxygenase und/oder der Interleukin-Ausschüttung, sind ausgewählt aus Extrakten aus Centella asiatica, beispielsweise erhältlich unter der Bezeichnung Madecassicoside von DSM, Glycyrrethinsäure, die besonders bevorzugt in Liposomen verkapselt vorliegt und in dieser Form z. B. unter der Handelsbezeichnung Calmsphere von Soliance erhältlich ist, Mischungen aus Getreidewachsen, Extrakten aus Schibutter und Argania Spinosa-Öl mit der INCI-Bezeichnung „Spent grain wax and butyrospermum parkii (shea butter) extract and Argania Spinosa Kernel OiI", wie sie z. B. unter der Handelsbezeichnung Stimu-Tex AS von der Firma Pentapharm erhältlich sind, Extrakten aus Vanilla Tahitensis, wie sie z. B. unter der Handelsbezeichnung Vanirea (INCI : Vanilla Tahitensis Fruit Extract) von der Firma Solabia erhältlich sind, Extrakten aus Olivenblättern (INCI: Olea Europaea (Olive) Leaf Extract), wie sie insbesondere unter der Handelsbezeichnung Oleanoline DPG von der Firma Vincience erhältlich sind, weiterhin Alginhydrolysaten, wie sie z. B. unter der Handelsbezeichnung Phycosaccha- ride, insbesondere Phycosaccharide AI, von der Firma Codif erhältlich sind, Extrakten aus Bacopa Monniera, wie sie z. B. unter der Handelsbezeichnung Bacocalmine von der Firma Sederma erhältlich sind, Extrakten aus der Rooibos-Pflanze, wie sie z. B. unter der Handelsbezeichnung Rooibos Herbasec MPE von der Firma Cosmetochem erhält¬ lich sind, den physiologisch verträglichen Salzen von Sterolsulfaten, wie sie z. B. unter der Handelsbezeichnung Phytocohesine (INCI: Sodium Beta-Sitosterylsulfate) von der Firma Vincience erhältlich sind, sowie beliebigen Mischungen dieser Wirkstoffe.Inhibitors of prostaglandin synthesis which are preferred according to the invention, in particular inhibitors of cyclooxygenase and / or interleukin secretion, are selected from silymarin, which is particularly preferably used in liposome-encapsulated form (obtainable, for example, under the trade name silymarin phytosome (INCI: Silybum Marianum Extract and phospholipids) from the company Indena SpA. Silymarin represents an active substance concentrate from the fruits of the milk thistle (Silybum marianum) which was formerly regarded as a uniform substance. The main constituents of the silymarin are silybin (silymarin I), silychristin (silymarin II) and silydianin, Other preferred inhibitors of prostagladin synthesis according to the invention, in particular inhibitors of cyclooxygenase and / or interleukin secretion, are selected from extracts of Centella asiatica, for example available under the name Madecassicoside from DSM, glycyrrethine acid, which is particularly preferably encapsulated in liposomes and in this form z. Sold under the trade name Calmsphere by Soliance, mixtures of cereal waxes, extracts of shea butter and Argania spinosa oil with the INCI name "Spent grain wax and butyrospermum parkii (shea butter) extract and Argania spinosa kernel OiI", as described, for example, in US Pat B. under the trade name Stimu-Tex AS available from the company Pentapharm, extracts of vanilla Tahitensis, as they are available, for example, under the trade name Vanirea (INCI: Vanilla Tahitensis Fruit Extract) from the company Solabia, extracts of olive leaves (INCI: Olea Europaea (Olive) Leaf Extract), as they are in particular under the trade name Oleanoline DPG available from the company Vincience, continue Alginhydrolysaten, as for example under the trade name Phycosacchancer, especially Phycosaccharide AI, from the company Codif, extracts of Bacopa Monniera, as described, for example, under the trade name Bacocalmine by the Company Sederma are available, extracts from the Rooibos plant, as z. B. under the trade name Rooibos Herbasec MPE of the company Cosmetochem Lich, the physiologically acceptable salts of sterol sulfates, as z. B. under the trade name Phytocohesins (INCI: Sodium Beta Sitosterylsulfate) are available from the company Vincience, and any mixtures of these agents.
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass die Konzentration des/der Inhibitors/en der Prostaglandin-Synthese insgesamt 0,0001 - 10,0 Gew.-%, bevorzugt 0,001 - 2,0 Gew.-%, besonders bevorzugt 0,05 - 1 ,0 Gew.-% und außerordentlich bevorzugt 0,1 - 0,5 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, beträgt.Preferred compositions according to the invention are characterized in that the concentration of the inhibitor (s) of the prostaglandin synthesis in total 0.0001-10.0% by weight, preferably 0.001-2.0% by weight, particularly preferably 0.05%. 1, 0 wt .-% and most preferably 0.1 to 0.5 wt .-%, each based on the total composition is.
Erfindungsgemäß bevorzugte Inhibitoren der Leukotrien-Synthese, insbesondere Inhibi¬ toren der 5-Lipoxygenase, sind ausgewählt aus Alginhydrolysaten, Aminodicarbonsäuren mit einer C-Kettenlänge von 3 - 6 Kohlenstoffatomen sowie deren physiologisch verträglichen Salzen, N-alkylierten C2-Ci i-Aminosäuren mit C1-C22-Alkylresten sowie deren physiologisch verträglichen Salzen, N-acylierten C2-Ci i-Aminosäuren mit C2-C22- Acylresten sowie deren physiologisch verträglichen Salzen, Hefeextrakten, α-Bisabolol, α-Liponsäure, sowie beliebigen Mischungen dieser Wirkstoffe.Inhibitors of leukotriene synthesis which are preferred according to the invention, in particular inhibitors of 5-lipoxygenase, are selected from algin hydrolyzates, amino dicarboxylic acids having a C chain length of 3 to 6 carbon atoms and their physiologically tolerated salts, N-alkylated C 2 -C 10 amino acids C 1 -C 22 -alkyl radicals and their physiologically tolerated salts, N-acylated C 2 -C i i-amino acids with C 2 -C 22 acyl radicals and their physiologically tolerated salts, yeast extracts, α-bisabolol, α-lipoic acid, and any desired mixtures of these agents.
In einer bevorzugten Ausführungsform sind die erfindungsgemäßen Alginhydrolysate ausgewählt aus den Produkten, die z. B. unter der Handelsbezeichnung Phycosacchari- de, insbesondere Phycosaccharide Al, von der Firma Codif erhältlich sind.In a preferred embodiment, the algin hydrolyzates according to the invention are selected from the products which, for. B. under the trade name phycosaccharides, in particular phycosaccharides Al, are available from Codif.
In einer weiteren bevorzugten Ausführungsform sind die erfindungsgemäß bevorzugten Aminodicarbonsäuren mit einer C-Kettenlänge von 3 - 6 Kohlenstoffatomen ausgewählt aus Aminomalonsäure, Aminobemsteinsäure (= Asparaginsäure), Aminoglutarsäure und Aminoadipinsäure sowie deren physiologisch verträglichen Salzen. Besonders bevorzugt sind Asparaginsäure und ihre physiologisch verträglichen Salze, insbesondere Kalium- aspartat und Magnesiumaspartat.In a further preferred embodiment, the inventively preferred aminodicarboxylic acids having a C chain length of 3 to 6 carbon atoms are selected from aminomalonic acid, aminobemic acid (= aspartic acid), aminoglutaric acid and aminoadipic acid and their physiologically tolerated salts. Particular preference is given to aspartic acid and its physiologically tolerated salts, in particular potassium aspartate and magnesium aspartate.
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass mindestens eine Aminodicarbonsäure mit einer C-Kettenlänge von 3 - 6 Kohlen¬ stoffatomen oder mindestens ein physiologisch verträgliches Salz einer Aminodicarbon¬ säure mit einer C-Kettenlänge von 3 - 6 Kohlenstoffatomen in einer Gesamtmenge von 0,01 bis 5 Gew.-%, bevorzugt 0,1 bis 2 Gew.-% und besonders bevorzugt 0,5 bis 1 Gew.-%, jeweils bezogen auf die gesamte topische Zusammensetzung, enthalten ist.Preferred compositions according to the invention are characterized in that at least one amino dicarboxylic acid having a C chain length of 3 to 6 carbon atoms or at least one physiologically acceptable salt of an amino dicarboxylic acid having a C chain length of 3 to 6 carbon atoms in a total amount of 0.01 to 5 wt .-%, preferably 0.1 to 2 wt .-% and particularly preferably 0.5 to 1 wt .-%, each based on the total topical composition is included.
In einer weiteren bevorzugten Ausführungsform sind die erfindungsgemäß bevorzugten N-alkylierten C2-C11 -Aminosäuren mit einem C1-C22-Alkylrest ausgewählt aus Alanin, Glutaminsäure, Pyroglutaminsäure, Lysin, Arginin, Histidin, Valin, Leucin, Isoleucin, Pro¬ lin, Tryptophan, Phenylalanin, Methionin, Glycin, Serin, Tyrosin, Threonin, Cystein, Aspa- ragin und Glutamin sowie deren physiologisch verträglichen Salzen, die am Stickstoff¬ atom der Aminogruppe einen CrC22-Alkylrest, ausgewählt aus einer Gruppe Methyl, Ethyl, Propyl, Butyl, Pentyl, Hexyl, Heptyl, Octyl, Nonyl, Decyl, Undecyl, Dodecyl (Lau- ryl), Tridecyl, Tetradecyl (Myristyl), Pentadecyl, Hexadecyl (Palmityl, Cetyl), Heptadecyl, Octadecyl (Stearyl), Nonadecyl, Eicosanyl (Arachidyl) und Behenyl, aufweisen. Beson¬ ders bevorzugt ist N-Methylglycin (= Sarcosin).In a further preferred embodiment, the preferred N-alkylated C 2 -C 11 -amino acids with a C 1 -C 22 -alkyl radical selected from alanine, glutamic acid, pyroglutamic acid, lysine, arginine, histidine, valine, leucine, isoleucine, Pro¬ lin, tryptophan, phenylalanine, methionine, glycine, serine, tyrosine, threonine, cysteine, asparagin and glutamine and their physiologically tolerated salts which on the nitrogen atom of the amino group are a C r C 22 -alkyl radical selected from a group of methyl, Ethyl, propyl, butyl, pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl (lauryl), tridecyl, tetradecyl (myristyl), pentadecyl, hexadecyl (palmityl, cetyl), heptadecyl, octadecyl (stearyl), Nonadecyl, eicosanyl (arachidyl) and behenyl. Particularly preferred is N-methylglycine (= sarcosine).
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass mindestens eine N-alkylierte C^C^-Aminosäure mit einem CrC22-Alkylrest oder mindestens ein physiologisch verträgliches Salz einer N-alkylierten Cz-Cn-Aminosäure mit einem Ci-C22-Alkylrest in einer Gesamtmenge von 0,01 bis 10 Gew.-%, bevorzugt 0,1 bis 5 Gew.-% und besonders bevorzugt 0,5 bis 2 Gew.-%, jeweils bezogen auf die gesamte topische Zusammensetzung, enthalten ist.Preferred compositions of the invention are characterized in that at least one N-alkylated C ^ C ^ amino acid having a C r C 22 -alkyl radical or at least one physiologically acceptable salt of an N-alkylated Cz-Cn-amino acid having a C 1 -C 22 -alkyl radical in a total amount of 0.01 to 10 wt .-%, preferably 0.1 to 5 wt .-% and particularly preferably 0.5 to 2 wt .-%, each based on the total topical composition is included.
In einer weiteren bevorzugten Ausführungsform sind die erfindungsgemäß bevorzugten N-acylierten C2-C1 rAminosäuren mit einem C2-C22-Acylrest ausgewählt aus Glutamin¬ säure, Pyroglutaminsäure, Lysin, Arginin, Histidin, Valin, Leucin, Isoleucin, Prolin, Tryp¬ tophan, Phenylalanin, Methionin, Glycin, Serin, Tyrosin, Threonin, Cystein, Asparagin und Glutamin sowie deren physiologisch verträglichen Salzen. Die Aminosäuren können einzeln oder im Gemisch eingesetzt werden. Erfindungsgemäß geeignet sind insbeson¬ dere Aminosäuregemische, die aus Pflanzen, insbesondere Getreidepflanzen, gewon¬ nen wurden. Der C2 - C22-Acylrest, mit dem die genannten Aminosäuren an der Amino¬ gruppe derivatisiert sind, ist ausgewählt aus einem Acetyl-, Propanoyl-, Butanoyl-, Pen- tanoyl-, Hexanoyl-, Heptanoyl-, Octanoyl-, Nonanoyl-, Decanoyl-, Undecanoyl-, Lauroyl-, Tridecanoyl-, Myristoyl-, Pentadecanoyl-, Cetoyl-, Palmitoyl-, Stearoyl-, Arachidoyl- oder Behenoyl-Rest. Mischungen von C8-C-, 8-Acylresten werden auch als Cocoyl-Rest be¬ zeichnet und sind ebenfalls bevorzugte Substituenten. Besonders bevorzugt sind Natri- umcocoylaminosäuren, Natriumoctanoylglutamat, Natriumdecanoylglutamat, Natriumlau- roylglutamat, Natriummyristoylglutamat, Natriumcetoylglutamat und Natriumstearoylglu- tamat und die Lauroyl-Derivate von aus Getreidepflanzen gewonnenen Aminosäuren. Die Getreidepflanzen, aus denen die erfindungsgemäß geeigneten Aminosäuren gewon¬ nen werden, unterliegen keiner Einschränkung. Geeignet sind beispielsweise Hafer, Wei¬ zen, Gerste und Roggen; besonders geeignet ist Hafer.In a further preferred embodiment, the inventively preferred N-acylated C 2 -C 1 r are amino acids having a C 2 -C 22 acyl radical selected from glutamic acid, pyroglutamic acid, lysine, arginine, histidine, valine, leucine, isoleucine, proline, Tryp¬ tophan, phenylalanine, methionine, glycine, serine, tyrosine, threonine, cysteine, asparagine and glutamine and their physiologically acceptable salts. The amino acids can be used individually or in a mixture. More particularly suitable according to the invention are amino acid mixtures which have been obtained from plants, in particular cereal plants. The C 2 -C 22 -acyl radical with which the amino acids mentioned are derivatized at the amino group is selected from an acetyl, propanoyl, butanoyl, pentanoyl, hexanoyl, heptanoyl, octanoyl, nonanoyl -, decanoyl, undecanoyl, lauroyl, tridecanoyl, myristoyl, pentadecanoyl, cetoyl, palmitoyl, stearoyl, arachidoyl or behenoyl radical. Mixtures of C 8 -C 8 -acyl radicals are also referred to as cocoyl radical and are likewise preferred substituents. Particular preference is given to sodium cocoyl amino acids, sodium octanoyl glutamate, sodium decanoyl glutamate, sodium roylglutamate, sodium myristoylglutamate, sodium cetoylglutamate and sodium stearoylglutamate, and the lauroyl derivatives of cereal-derived amino acids. The cereal plants from which the amino acids suitable according to the invention are obtained are subject to no restriction. For example, oats, wheat, barley and rye are suitable; oat is particularly suitable.
Ein besonders bevorzugter 5-Lipoxygenase-lnhibitor ist eine Mischung aus den Natrium¬ salzen von mit Kokosfettsäureresten acylierten Aminosäuren, den Kalium- und Magnesi¬ umsalzen der Asparaginsäure und Sarcosin, wie sie beispielsweise als Handelsprodukt Sepiealm S von der Firma Seppic mit der INCI-Bezeichnung "Sodium Cocoyl Amino- aeids, Sarcosine, Potassium Aspartate, Magnesium Aspartate" erhältlich ist. Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass mindestens eine N-acylierte C2-C1 rAminosäuren mit einem C2-C22- Acy I rest oder mindestens ein physiologisch verträgliches Salz einer N-acylierten C^Cn-Aminosäure mit einem C2-C22- Acy I rest in einer Gesamtmenge von 0,01 bis 10 Gew.-%, bevorzugt 0,1 bis 5 Gew.-% und besonders bevorzugt 0,5 bis 2 Gew.-%, jeweils bezogen auf die gesamte topische Zusammensetzung, enthalten ist.A particularly preferred 5-lipoxygenase inhibitor is a mixture of the sodium salts of amino acids acylated with coconut fatty acid residues, the potassium and magnesium salts of aspartic acid and sarcosine, as described for example as Sepiealm S by Seppic with the INCI name "Sodium Cocoyl Amino Acids, Sarcosine, Potassium Aspartate, Magnesium Aspartate" is available. Preferred compositions according to the invention are characterized in that at least one N-acylated C 2 -C 1 r amino acids having a C 2 -C 22 acyl residue or at least one physiologically acceptable salt of an N-acylated C 1 -C 5 amino acid having a C 2 - C 22 - Acy I rest in a total amount of 0.01 to 10 wt .-%, preferably 0.1 to 5 wt .-% and particularly preferably 0.5 to 2 wt .-%, each based on the total topical composition , is included.
In einer weiteren bevorzugten Ausführungsform werden die erfindungsgemäß als 5-Lipoxygenase-lnhibitoren bevorzugten Hefeextrakte in Mengen von 0,001 bis 5 Gew.- %, bevorzugt 0,01 bis 2 Gew.-% und besonders bevorzugt 0,1 bis 1 Gew.-%, jeweils bezogen auf die gesamte topische Zusammensetzung, eingesetzt. Ein besonders bevor¬ zugt verwendetes Handelsprodukt ist Drieline (INCI-Bezeichnung "Sorbitol, Yeast Extract"), erhältlich von der Firma Lanatech.In a further preferred embodiment, the yeast extracts preferred according to the invention as 5-lipoxygenase inhibitors are in amounts of from 0.001 to 5% by weight, preferably from 0.01 to 2% by weight and particularly preferably from 0.1 to 1% by weight, in each case based on the total topical composition used. A particularly preferred commercial product used is Drieline (INCI name "sorbitol, Yeast Extract"), available from Lanatech.
In einer weiteren bevorzugten Ausführungsform wird der erfindungsgemäß bevorzugte 5-Lipoxygenase-lnhibitor α-Bisabolol in Mengen von 0,001 bis 5 Gew.-%, bevorzugt 0,01 bis 2 Gew.-% und besonders bevorzugt 0,1 bis 1 Gew.-%, jeweils bezogen auf die gesamte topische Zusammensetzung, eingesetzt.In a further preferred embodiment, the preferred 5-lipoxygenase inhibitor according to the invention is α-bisabolol in amounts of 0.001 to 5% by weight, preferably 0.01 to 2% by weight and particularly preferably 0.1 to 1% by weight. , in each case based on the total topical composition used.
In einer weiteren bevorzugten Ausführungsform wird der erfindungsgemäß bevorzugte 5-Lipoxygenase-lnhibitor α-Liponsäure in Mengen von 0,001 bis 5 Gew.-%, bevorzugt 0,01 bis 2 Gew.-% und besonders bevorzugt 0,1 bis 1 Gew.-%, jeweils bezogen auf die gesamte topische Zusammensetzung, eingesetzt. In einer weiteren bevorzugten Ausführungsform sind die erfindungsgemäß als 5-Lipoxy- genase-lnhibitoren bevorzugten physiologisch verträglichen Salze der Sterolsulfate aus¬ gewählt aus mindestens einem physiologisch verträglichen Salz von ß-Sitosterolsulfat, Ergosterolsulfat, Stigmasterolsulfat, Cholesterolsulfat und Lanosterolsulfat. Besonders bevorzugt sind die Salze von ß-Sitosterolsulfat. Die Sterolsulfatsalze können dabei so¬ wohl einzeln als auch in beliebigen Mischungen eingesetzt werden. Besonders bevor¬ zugt ist das Natriumsalz von ß-Sitosterolsulfat, z. B. als Handelsprodukt Phytocohesine (INCI-Bezeichnung "Sodium Beta-Sitosteryl Sulfate"), von der Firma Vincience erhältlich. Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass mindestens ein physiologisch verträgliches Sterolsulfatsalz in einer Gesamtmenge von 0,001 bis 5 Gew.-%, bevorzugt 0,01 bis 2 Gew.-% und besonders bevorzugt 0,1 bis 1 Gew.-%, jeweils bezogen auf die gesamte topische Zusammensetzung, enthalten ist.In a further preferred embodiment, the 5-lipoxygenase inhibitor preferred according to the invention is α-lipoic acid in amounts of 0.001 to 5% by weight, preferably 0.01 to 2% by weight and more preferably 0.1 to 1% by weight. , in each case based on the total topical composition used. In a further preferred embodiment, the preferred according to the invention as 5-lipoxygenase inhibitors physiologically acceptable salts of sterol sulfates aus¬ selected from at least one physiologically acceptable salt of ß-sitosterol sulfate, ergosterol sulfate, stigmasterol sulfate, cholesterol sulfate and lanosterol sulfate. Particularly preferred are the salts of β-sitosterol sulfate. The sterol sulphate salts can be used both individually and in any desired mixtures. Particularly preferred is the sodium salt of β-sitosterol sulphate, eg. B. as a commercial product phytocohesins (INCI name "Sodium Beta Sitosteryl Sulfate"), available from the company Vincience. Preferred compositions according to the invention are characterized in that at least one physiologically acceptable sterolsulfate salt in a total amount of 0.001 to 5 wt .-%, preferably 0.01 to 2 wt .-% and particularly preferably 0.1 to 1 wt .-%, each based on the total topical composition, is included.
Die physiologisch verträglichen Salze der vorgenannten 5-Lipoxygenase-lnhibitoren sind bevorzugt ausgewählt aus den Ammonium-, Alkalimetall-, Magnesium-, Calcium-, Alumi¬ nium-, Zink- und Mangan-Salzen. Besonders bevorzugt sind die Natrium-, Kalium-, Mag¬ nesium-, Aluminium-, Zink- und Mangan-Salze.The physiologically tolerated salts of the abovementioned 5-lipoxygenase inhibitors are preferably selected from the ammonium, alkali metal, magnesium, calcium, aluminum, zinc and manganese salts. Particular preference is given to the sodium, potassium, magnesium, aluminum, zinc and manganese salts.
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass mindestens ein Inhibitor der Leukotrien-Synthese in einer Gesamtmenge von 0,0001 - 10,0 Gew.-%, bevorzugt 0,001 - 2,0 Gew.-%, besonders bevorzugt 0,05 - 1,0 Gew.-% und außerordentlich bevorzugt 0,1 - 0,5 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, enthalten ist.Preferred compositions according to the invention are characterized in that at least one inhibitor of leukotriene synthesis is present in a total amount of 0.0001-10.0% by weight, preferably 0.001-2.0% by weight, particularly preferably 0.05-1. 0 wt .-% and most preferably 0.1 to 0.5 wt .-%, each based on the total composition is included.
Erfindungsgemäß besonders bevorzugte Modulatoren der Freisetzung kutaner Neuro- mediatoren, insbesondere besonders bevorzugte Stimulatoren der ß-Endorphin-Synthe- se, sind ausgewählt aus Mischungen aus mindestens einem Extrakt aus den Blättern der Mentha piperita und mindestens einem Extrakt aus Kakaobohnen (Theobroma cacao), wobei wässrige, glycolische oder wässrig-glycolische Zubereitungen dieser Extrakt¬ mischungen, insbesondere solche, die unter der Handelsbezeichnung Caomint von der Firma Solabia erhältlich sind, besonders bevorzugt sind. Ein weiterer besonders bevor¬ zugter Modulator der Freisetzung kutaner Neuromediatoren ist das Dipeptidderivat N- Acetyl-Tyr-Arg-hexyldecylester mit der INCI-Bezeichnung Acetyl Dipeptide-1 Cetyl Ester, das z. B. als wässrige Zubereitung unter der Handelsbezeichnung Calmosensine von der Firma Sederma erhältlich ist. Weitere bevorzugte Modulatoren der Freisetzung kutaner Neuromediatoren, insbesondere Stimulatoren der ß-Endorphinausschüttung in Keratino- zyten, sind Extrakte aus den Schalen von Kakaobohnen (Theobroma cacao), zum Bei¬ spiel erhältlich als Rohstoff Caobromine, Caoorange, Caospice und Caophenol von der Firma Solabia. Weitere erfindungsgemäß bevorzugte Modulatoren der Freisetzung kuta¬ ner Neuromediatoren, insbesondere Stimulatoren der ß-Endorphinausschüttung in Kera- tinozyten, sind ausgewählt aus Extrakten aus Helichrysum italicum, z. B. erhältlich unter den Handelsbezeichnungen ArEAUmat Perpetua (INCI: Water, Helichrysum italicum extract) und ArEAUmat Perpetua Glycerine (INCI: Glycerin, Water, Helichrysum italicum extract) von der Firma Codif, Extrakten aus Crithmum Maritimum, z. B. erhältlich unter den Handelsbezeichnungen ArEAUmat Samphira (Sea Fennel, INCI: Water, Crithmum Maritimum Extract) und Aroleat Samphira (INCI: Caprylic/Capric Triglyceride, Hydroge- nated Vegetable OiI, Crithmum Maritimum Extract) von der Firma Codif, Extrakten aus Lavandula stoechas, z. B. erhältlich unter den Handelsbezeichnungen ArEAUmat Lavan- da (INCI: Water, Lavandula stoechas extract) und ArEAUmat Lavanda (INCI: Glycerin, Water, Lavandula stoechas extract) von der Firma Codif, Extrakten aus Mentha piperita, z. B. unter den Handelsbezeichnungen Authenticals of Peppermint (Solabia) und Calmi- skin (Silab) erhältlich, Glutamylamidoethylindol, z. B. erhältlich unter der Handelsbe¬ zeichnung Glistin von der Firma Exsymol, einem durch mikrobielle Fermentation gewon¬ nenen verzweigten Polysaccharid mit Rhamnose-, Galactose- und Glucuronsäure-Ein- heiten mit der INCI-Bezeichnung Biosaccharide Gum-2, z. B. erhältlich unter der Han¬ delsbezeichnung Rhamnosoft von der Firma Solabia, Extrakten aus den Samen von Tephrosia Purpurea mit der INCI-Bezeichnung Tephrosia Purpurea Seed Extract, z. B. erhältlich unter der Handelsbezeichnung Tephroline (INCI: Water, Propylene Glycol, Tephrosia purpurea extract) von der Firma Vincience, Mischungen aus dem Öl von Mentha arvensis-Blättem, Limonenschalenöl, Zypressenöl, Lavendelöl und Cistus Lada- niferus-ÖI mit der INCI-Bezeichnung Mentha Arvensis Leaf OiI and Citrus Medica Limo- num (Lemon) Peel OiI and Cupressus Sempervirens OiI and Lavandula Hybrida OiI and Cistus Ladaniferus OiI, z. B. erhältlich unter der Handelsbezeichnung V-Tonic (Gatte- fosse), Hexasacchariden gemäß FR 2842201 , sowie beliebigen Mischungen der vorge¬ nannten Wirkstoffe.Particularly preferred modulators according to the invention of the release of cutaneous neurotransmitters, in particular particularly preferred stimulators of the β-endorphin synthesis, are selected from mixtures of at least one extract from the leaves of Mentha piperita and at least one extract from cocoa beans (Theobroma cacao) aqueous, glycolic or aqueous-glycolic preparations of these extract mixtures, in particular those which are obtainable under the trade name Caomint from the company Solabia, are particularly preferred. Another particularly preferred modulator of the release of cutaneous neuromediators is the dipeptide derivative N-acetyl-Tyr-Arg-hexyldecyl ester with the INCI name Acetyl Dipeptide-1 Cetyl Ester, which, for. B. as an aqueous preparation under the trade name Calmosensine from the company Sederma is available. Other preferred modulators of cutaneous release Neuromediators, in particular stimulators of β-endorphin secretion in keratinocytes, are extracts from the shells of cocoa beans (Theobroma cacao), for example obtainable as raw material caobromines, cao-orange, caospice and caophenol from Solabia. Further inventively preferred modulators of the release kuta¬ ner neuromediators, in particular stimulators of ß-endorphin secretion in keratinocytes, are selected from extracts of Helichrysum italicum, z. B. available under the trade names ArEAUmat Perpetua (INCI: Water, Helichrysum italicum extract) and ArEAUmat Perpetua Glycerine (INCI: Glycerol, Water, Helichrysum italicum extract) from Codif, extracts from Crithmum Maritimum, z. Available under the trade names ArEAUmat Samphira (Sea Fennel, INCI: Water, Crithmum Maritimum Extract) and Aroleat Samphira (INCI: Caprylic / Capric Triglyceride, Hydroge- nated Vegetable Oil, Crithmum Maritimum Extract) from Codif, extracts from Lavandula stoechas , z. B. available under the trade names ArEAUmat Lavanda (INCI: Water, Lavandula stoechas extract) and ArEAUmat Lavanda (INCI: Glycerol, Water, Lavandula stoechas extract) from Codif, extracts from Mentha piperita, z. Available under the tradenames Authenticals of Peppermint (Solabia) and Calmi- ska (Silab), glutamylamidoethyl indole, eg. B. available under the trade name Glistin from the company exsymol, a gewon¬ by microbial fermentation branched polysaccharide with rhamnose, galactose and glucuronic acid units with the INCI name Biosaccharide Gum-2, z. B. available under the trade name Rhamnosoft from the company Solabia, extracts from the seeds of Tephrosia Purpurea with the INCI name Tephrosia Purpurea Seed Extract, z. B. available under the trade name Tephroline (INCI: Water, Propylene Glycol, Tephrosia purpurea extract) from the company Vincience, mixtures of the oil of Mentha arvensis leaves, lime skin oil, cypress oil, lavender oil and Cistus Ladeniferus oil with the INCI Name Mentha Arvensis Leaf OiI and Citrus Medica Limonium (Lemon) Peel OiI and Cupressus Sempervirens OiI and Lavandula Hybrida OiI and Cistus Ladaniferus OiI, z. B. available under the trade name V-Tonic (Gattefosse), hexasaccharides according to FR 2842201, as well as any mixtures of vor¬ named active ingredients.
Bevorzugte erfindungsgemäße kosmetische Zusammensetzungen sind dadurch gekenn¬ zeichnet, dass mindestens ein Wirkstoff zur Modulation der Freisetzung kutaner Neuro¬ mediatoren, insbesondere mindestens ein Stimulator der ß-Endorphinausschüttung in Keratinozyten, in einer Gesamtmenge von 0,000001 - 10 Gew.-%, bevorzugt 0,00001 - 5 bis 10 Gew.-%, besonders bevorzugt 0,0001 - 1 bis 2 bis 3 Gew.-% und außerordent¬ lich bevorzugt 0,001 - 0,005 - 0,01- 0,1 bis 0,5 Gew.-%, jeweils bezogen auf den Gehalt an Aktivsubstanz in der gesamten kosmetischen Zusammensetzung, enthalten ist.Preferred cosmetic compositions according to the invention are characterized in that at least one active substance for modulating the release of cutaneous neurotransmitters, in particular at least one stimulator of the β-endorphin secretion in keratinocytes, in a total amount of 0.000001-10% by weight, preferably 0 , 00001 - From 5 to 10% by weight, more preferably from 0.0001 to 1 to 2 to 3% by weight and, most preferably, from 0.001 to 0.005 to 0.01 to 0.1 to 0.5% by weight, based in each case on the content of active substance in the entire cosmetic composition, is included.
Um die Wirkung der erfindungsgemäßen Zusammensetzungen noch zu erhöhen, sind in einer bevorzugten Ausführungsform der Erfindung weitere kosmetische Wirkstoffe ent¬ halten. Bevorzugte weitere Wirkstoffe sind Feuchthaltemittel, insbesondere ausgewählt aus den wasserlöslichen mehrwertigen C2 - C9-Alkanolen mit 2 - 6 Hydroxylgruppen und/oder den wasserlöslichen Polyethylenglycolen, bestehend aus 3 - 20 Ethylenoxid- Einheiten, sowie Mischungen hiervon. Bevorzugt sind diese Komponenten ausgewählt aus 1 ,2-Propylenglycol, 2-Methyl-1,3-propandiol, Glycerin, Butylenglycolen wie 1 ,2-Butylenglycol, 1 ,3-Butylenglycol und 1 ,4-Butylenglycol, Pentylenglycolen, Hexan- diolen wie 1 ,6-Hexandiol, Hexantriolen wie 1 ,2,6-Hexantriol, 1 ,8-Octandiol, Dipropy- lenglycol, Tripropylenglycol, Diglycerin, Triglycerin, Erythrit, Sorbit sowie Mischungen der vorgenannten Substanzen. Geeignete wasserlösliche Polyethylenglycole, bestehend aus 3 - 20 Ethylenoxid-Einheiten, sind ausgewählt aus PEG-3, PEG-4, PEG-6, PEG-7, PEG- 8, PEG-9, PEG-10, PEG-12, PEG-14, PEG-16, PEG-18 und PEG-20, sowie Mischungen hiervon, wobei PEG-3 bis PEG-8 bevorzugt sind. Auch Zucker und bestimmte Zuckerderivate wie Fructose, Glucose, Maltose, Maltitol, Mannit, Inosit, Sucrose, Treha- lose, Xylose, Rhamnose und Fucose können erfindungsgemäß bevorzugt sein. Weitere bevorzugte Feuchthaltemittel sind Taurin, Allantoin, (2-Hydroxyethyl)harnstoff, Biosac- charide Gum-1 und Glycosaminoglycane und deren Salze und/oder Ester, insbesondere Hyaluronsäure, ihre Salze und ihre Silanolderivate.In order to increase the effect of the compositions according to the invention, in a preferred embodiment of the invention, further cosmetic active ingredients are contained. Preferred further active ingredients are humectants, in particular selected from the water-soluble polyhydric C 2 -C 9 -alkanols having 2 to 6 hydroxyl groups and / or the water-soluble polyethylene glycols, consisting of 3 to 20 ethylene oxide units, and mixtures thereof. These components are preferably selected from 1,2-propylene glycol, 2-methyl-1,3-propanediol, glycerol, butylene glycols such as 1,2-butylene glycol, 1,3-butylene glycol and 1,4-butylene glycol, pentylene glycols, hexane diols, such as 1, 6-hexanediol, hexanetriols such as 1, 2,6-hexanetriol, 1, 8-octanediol, dipropylene glycol, tripropylene glycol, diglycerol, triglycerol, erythritol, sorbitol and mixtures of the aforementioned substances. Suitable water-soluble polyethylene glycols, consisting of 3 to 20 ethylene oxide units, are selected from PEG-3, PEG-4, PEG-6, PEG-7, PEG-8, PEG-9, PEG-10, PEG-12, PEG- 14, PEG-16, PEG-18 and PEG-20, and mixtures thereof, with PEG-3 to PEG-8 being preferred. Sugar and certain sugar derivatives such as fructose, glucose, maltose, maltitol, mannitol, inositol, sucrose, trehalose, xylose, rhamnose and fucose may also be preferred according to the invention. Further preferred humectants are taurine, allantoin, (2-hydroxyethyl) urea, biosaccharide Gum-1 and glycosaminoglycans and their salts and / or esters, especially hyaluronic acid, its salts and its silanol derivatives.
Bevorzugte erfindungsgemäße kosmetische Zusammensetzungen sind dadurch gekenn¬ zeichnet, dass sie mindestens ein Feuchthaltemittel in einer Gesamtmenge von 0,1 - 25 Gew.-%, bevorzugt 1,0 - 15 Gew.-%, besonders bevorzugt 5 - 10 Gew.-%, bezogen auf die Gesamtzusammensetzung, enthalten.Preferred cosmetic compositions according to the invention are characterized in that they contain at least one humectant in a total amount of 0.1-25% by weight, preferably 1.0-15% by weight, particularly preferably 5-10% by weight. based on the total composition.
Weitere bevorzugte Wirkstoffe sind ausgewählt aus Oligomeren und Polymeren von Ami¬ nosäuren, N-C2-C24-Acylaminosäuren, den Estern und/oder den physiologisch verträgli¬ chen Salzen dieser Substanzen, DNA- oder RNA-Oligonucleotiden, natürlichen Betain- verbindungen, Vitaminen, Provitaminen und Vitaminvorstufen der Gruppen A, B, C, E, H und K und den Estern der vorgenannten Substanzen, α-Hydroxycarbonsäuren, α-Ketocarbonsäuren, ß-Hydroxycarbonsäuren und deren Ester-, Lacton- oder Salzform, Flavonoiden und Flavonoid-reichen Pflanzenextrakten, Isoflavonoiden und Isoflavonoid- reichen Pflanzenextrakten, Polyphenolen und Polyphenol-reichen Pflanzenextrakten, Ubichinon und Ubichinol sowie deren Derivaten, natürlich vorkommenden Xanthin-Deri- vaten, ausgewählt aus Coffein, Theophyllin, Theobromin und Aminophyllin, Ectoin, anor¬ ganischen und organischen UV-Filtersubstanzen, selbstbräunenden Wirkstoffen sowie hautaufhellenden Wirkstoffen.Further preferred active substances are selected from oligomers and polymers of amino acids, NC 2 -C 24 -acylamino acids, the esters and / or the physiologically tolerable salts of these substances, DNA or RNA oligonucleotides, natural betaine compounds, vitamins, Provitamins and vitamin precursors of groups A, B, C, E, H and K and the esters of the aforementioned substances, α-hydroxycarboxylic acids, α-ketocarboxylic acids, β-hydroxycarboxylic acids and their ester, lactone or salt form, flavonoids and flavonoid-rich plant extracts , Isoflavonoids and isoflavonoid rich plant extracts, polyphenols and polyphenol-rich plant extracts, ubiquinone and ubiquinol and derivatives thereof, naturally occurring xanthine derivatives, selected from caffeine, theophylline, theobromine and aminophylline, ectoine, anor¬ ganic and organic UV filter substances, self-tanning agents and skin lightening agents.
Unter Aminosäureoligomeren werden erfindungsgemäß Peptide mit 2 - 30, bevorzugt 2 - 15, Aminosäuren, verstanden. Die Oligomere der Aminosäuren und/oder der N-C2-C24- Acylaminosäuren sind bevorzugt ausgewählt aus Di-, Tri-, Tetra-, Penta-, Hexa- oder Pentadecapeptiden, die acyliert und/oder verestert sein können. Zahlreiche dieser Ami- nosäureoligomere stimulieren die Collagensynthese beziehungsweise sind in der Lage, Zellen des Immunsystems, wie Mastzellen und Makrophagen, zu rekrutieren, die dann über die Freisetzung von Wachstumsfaktoren Reparaturprozesse im Gewebe, z.B. die Collagensynthese, induzieren, beziehungsweise sind in der Lage, an die Sequenz Arg- Phe-Lys in Thrombospondin I (TSP-1) zu binden und damit aktives TGF-ß {tissue growth factor), der die Synthese von Collagen in dermalen Fibroblasten induziert, freizusetzen. Derartige Aminosäureoligomere werden bevorzugt als Wirkstoffe gegen die Hautalterung verwendet.According to the invention, amino acid oligomers are peptides having 2 to 30, preferably 2 to 15, amino acids. The oligomers of the amino acids and / or the NC 2 -C 24 acylamino acids are preferably selected from di-, tri-, tetra-, penta-, hexa- or pentadecapeptides which may be acylated and / or esterified. Many of these amino acid oligomers stimulate collagen synthesis or are able to recruit cells of the immune system, such as mast cells and macrophages, which then induce, or are capable of, repair processes in the tissue via the release of growth factors, eg collagen synthesis to bind the sequence Arg-Phe-Lys into thrombospondin I (TSP-1) and thus to release active TGF-ß (tissue growth factor), which induces the synthesis of collagen in dermal fibroblasts. Such amino acid oligomers are preferably used as anti-aging agents.
Erfindungsgemäß bevorzugte, gegebenenfalls N-acylierte und/oder veresterte Dipeptide sind Acetyl-Citrullyl-Arginin (z. B. Exsy-Algine von Exsymol mit der INCI-Bezeichnung Acetyl Citrull Amido Arginine), Tyr-Arg (Dipeptide-1), Val-Trp (Dipeptide-2), Asn-Phe, Asp-Phe, N-Palmitoyl-ß-Ala-His, N-Acetyl-Tyr-Arg-hexyldecylester (z. B. Calmosensine von Sederma), Carnosin (ß-A!a-His) und N-Palmitoyl-Pro-Arg. Erfindungsgemäß bevor¬ zugte, gegebenenfalls N-acylierte und/oder veresterte Tripeptide sind Gly-His-Lys, das z. B. unter der Bezeichnung „Omega-CH-Aktivator" von der Firma GfN oder in acylierter Form (N-Palmitoyl-Gly-His-Lys) unter der Bezeichnung Biopeptide CL von Sederma er¬ hältlich ist, aber (in acylierter Form) auch einen Bestandteil des Produktes Matrixyl 3000 von Sederma darstellt. Das Tripeptid Gly-His-Lys kann auch als Kupfersalz (Cu2+) einge¬ setzt werden und ist als solches über ProCyte Corporation zu beziehen. Weiterhin kön¬ nen Analoga von Gly-His-Lys eingesetzt werden, wobei maximal zwei Aminosäuren durch geeignete andere Aminosäuren substituiert sind. Zur Substitution von GIy sind erfindungsgemäß AIa, Leu und He geeignet. Die erfindungsgemäß bevorzugten Amino¬ säuren, die His oder Lys ersetzen können, beinhalten eine Seitenkette mit einem Stick¬ stoffatom, das bei pH 6 überwiegend geladen vorliegt, z. B. Pro, Lys, Arg, His, Desmosin und Isodesmosin. Besonders bevorzugt wird Lys durch Arg, Orn, oder Citrullin ersetzt. Ein weiteres erfindungsgemäß bevorzugtes Tripeptid ist Gly-His-Arg (INCI-Bezeichnung: Tripeptide-3) sowie dessen Derivat N-Myristoyl-Gly-His-Arg, das z. B. unter der Bezeich¬ nung Collasyn 314-GR von Therapeutic Peptide Inc. erhältlich ist; weitere erfindungs¬ gemäß bevorzugte Tripeptide sind ausgewählt aus Lys-Val-Lys, Lys-Val-Dab (Dab = Diaminobuttersäure), Lys-Phe-Lys, Lys-Ile-Lys, Dab-Val-Lys, Lys-Val-Orn, Lys-Val-Dap (Dap = Diaminopropionsäure), Dap-Val-Lys, Palmitoyl-Lys-Val-Lys, z. B. erhältlich von der Firma Pentapharm unter der Bezeichnung SYN®-COLL, Lys-Pro-Val, Tyr-Tyr-Val, Tyr-Val-Tyr, Val-Tyr-Val (Tripeptide-2), Tripeptide-4 (z. B. ATPeptide, zu beziehen über IMPAG), His-Ala-Om N-Elaidoyl-Lys-Phe-Lys und N-Acetyl-Arg-Lys-Arg-NH2. Erfindungsgemäß bevorzugte, gegebenenfalls N-acylierte und/oder veresterte Tetrapep- tide sind ausgewählt aus Rigin und Rigin-basierten Tetrapeptiden sowie ALAMCAT- Tetrapeptiden. Rigin weist die Sequenz Gly-Gln-Pro-Arg auf. Rigin-basierte Tetrapeptide umfassen die Rigin-Analoga und Rigin-Derivate, insbesondere das erfindungsgemäß besonders bevorzugte N-Palmitoyl-Gly-Gln-Pro-Arg, das z. B. unter der Bezeichnung Eyeliss von Sederma erhältlich ist, aber auch einen Bestandteil des Produktes Matrixyl 3000 von Sederma darstellt. Zu den Rigin-Analoga zählen solche, bei denen die vier Aminosäuren umarrangiert sind und/oder bei denen gegenüber Rigin maximal zwei Ami¬ nosäuren substituiert sind, z. B. die Sequenz Ala-Gln-Thr-Arg. Bevorzugt hat mindestens eine der Aminosäuren der Sequenz ein Pro oder Arg und besonders bevorzugt beinhal¬ tet das Tetrapeptid sowohl Pro als auch Arg, wobei ihre Reihenfolge und Position variie¬ ren können. Die substituierenden Aminosäuren können aus jeder Aminosäure, die im fol¬ genden definiert ist, ausgewählt werden. Besonders bevorzugte Rigin-basierte Tetrapep¬ tide umfassen: Xaa-Xbb-Arg-Xcc, Xaa-Xbb-Xcc-Pro, Xaa-Xbb-Pro-Arg, Xaa-Xbb-Pro- Xcc, Xaa-Xbb-Xcc-Arg, wobei Xaa, Xbb und Xcc gleiche oder voneinander verschiedene Aminosäuren sein können und wobei Xaa ausgewählt ist aus GIy und den Aminosäuren, die GIy substituieren können, Xbb ausgewählt ist aus GIn und den Aminosäuren, die GIn substituieren können, Xcc ausgewählt ist aus Pro oder Arg und den Aminosäuren, die Pro und Arg substituieren können.According to preferred, optionally N-acylated and / or esterified dipeptides are acetyl-citrullyl-arginine (eg Exsy-algins of exsymol with the INCI name Acetyl Citrull Amido Arginine), Tyr-Arg (dipeptide-1), Val- Trp (dipeptide-2), Asn-Phe, Asp-Phe, N-palmitoyl-.beta.-Ala-His, N-acetyl-Tyr-Arg-hexyldecylester (eg, calmosensins from Sederma), carnosine (.beta.-A! a-His) and N-palmitoyl-Pro-Arg. Preference according to the invention, optionally N-acylated and / or esterified tripeptides are Gly-His-Lys, the z. B. under the name "Omega-CH activator" by the company GfN or in acylated form (N-palmitoyl-Gly-His-Lys) under the name Biopeptide CL of Sederma er¬ is available, but (in acylated form) also is a component of the product Matrixyl 3000 from Sederma The tripeptide Gly-His-Lys can also be used as the copper salt (Cu 2+ ) and can be obtained as such from ProCyte Corporation. The substitution of Gly in accordance with the invention is suitable for Ala, Leu and He The preferred amino acids according to the invention which can replace His or Lys include a side chain having a nitrogen atom which is predominantly charged at pH 6, eg Pro, Lys, Arg, His, desmosine and isodesmosine, more preferably Lys is replaced by Arg, Orn or citrulline. A further preferred tripeptide according to the invention is Gly-His-Arg (INCI name: tripeptide-3) and its derivative N-myristoyl-Gly-His-Arg, which, for. B. under the designation Collasyn 314-GR of Therapeutic Peptide Inc. is available; further preferred tripeptides according to the invention are selected from Lys-Val-Lys, Lys-Val-Dab (Dab = diaminobutyric acid), Lys-Phe-Lys, Lys-Ile-Lys, Dab-Val-Lys, Lys-Val-Orn, Lys-Val-Dap (Dap = diaminopropionic acid), Dap-Val-Lys, palmitoyl-Lys-Val-Lys, e.g. As sold by the company Pentapharm under the name ® SYN -COLL, Lys-Pro-Val, Tyr-Tyr-Val, Tyr-Val-Tyr, Val-Tyr-Val (Tripeptide-2), Tripeptide-4 (z. ATPeptides via IMPAG), His-Ala-Om N-elaidoyl-Lys-Phe-Lys and N-acetyl-Arg-Lys-Arg-NH 2 . According to preferred, optionally N-acylated and / or esterified tetrapeptides are selected from Rigin and Rigin-based tetrapeptides and ALAMCAT tetrapeptides. Rigin has the sequence Gly-Gln-Pro-Arg. Rigin-based tetrapeptides include the Rigin analogs and Rigin derivatives, in particular the invention particularly preferred N-palmitoyl-Gly-Gln-Pro-Arg, z. B. is available under the name Eyeliss of Sederma, but also forms part of the product Matrixyl 3000 of Sederma. The Rigin analogs include those in which the four amino acids are rearranged and / or in which a maximum of two amino acids are substituted by Rigin, z. For example, the sequence Ala-Gln-Thr-Arg. Preferably, at least one of the amino acids of the sequence has a Pro or Arg, and more preferably the tetrapeptide includes both Pro and Arg, and their order and position may vary. The substituting amino acids can be selected from any amino acid which is defined below. Particularly preferred rigin-based tetrapeptides include: Xaa-Xbb-Arg-Xcc, Xaa-Xbb-Xcc-Pro, Xaa-Xbb-Pro-Arg, Xaa-Xbb-Pro-Xcc, Xaa-Xbb-Xcc-Arg, wherein Xaa, Xbb and Xcc may be the same or different amino acids and wherein Xaa is selected from Gly and the amino acids which can substitute Gly, Xbb is selected from GIn and the amino acids which can substitute for GIn, Xcc is selected from Pro or Arg and the amino acids that can substitute Pro and Arg.
Die bevorzugten Aminosäuren, die GIy ersetzen können, beinhalten eine aliphatische Seitenkette, z. B. ß-Ala, AIa, VaI, Leu, Pro, Sarcosin (Sar) und lsoleucin (He). Die bevorzugten Aminosäuren, die GIn ersetzen können, beinhalten eine Seitenkette mit einer Aminogruppe, die bei neutralem pH (pH 6-7) überwiegend ungeladen vorliegt, z.B. Asn, Lys, Om, 5-Hydroxyprolin, Citrullin und Canavanin. Die bevorzugten Aminosäuren, die Arg ersetzen können, beinhalten eine Seitenkette mit einem Stickstoffatom, das bei pH 6 überwiegend geladen vorliegt, z.B. Pro, Lys, His, Desmosin und Isodesmosin.The preferred amino acids that can replace GIy include an aliphatic side chain, e.g. B. β-Ala, Ala, VaI, Leu, Pro, Sarcosine (Sar) and Isoleucine (He). The preferred amino acids that can replace GIn include a side chain having an amino group predominantly uncharged at neutral pH (pH 6-7), eg, Asn, Lys, Om, 5-hydroxyproline, citrulline, and canavanine. The preferred amino acids that can replace Arg include a side chain with a nitrogen atom predominantly charged at pH 6, such as Pro, Lys, His, desmosine, and isodesmosine.
Als Rigin-Analoga sind erfindungsgemäß Gly-Gln-Arg-Pro und Val-Val-Arg-Pro bevor¬ zugt.According to the invention, Gly-Gln-Arg-Pro and Val-Val-Arg-Pro are preferred as Rigin analogues.
ALAMCAT-Tetrapeptide sind Tetrapeptide, die mindestens eine Aminosäure mit einer aliphatischen Seitenkette enthalten, z. B. ß-Ala, AIa, VaI, Leu, Pro, Sarcosin (Sar) und lsoleucin (He). Weiterhin beinhalten ALAMCAT-Tetrapeptide mindestens eine Amino¬ säure mit einer Seitenkette mit einer Aminogruppe, die bei neutralem pH (pH 6-7) über¬ wiegend ungeladen vorliegt, z.B. GIn, Asn, Lys, Om, 5-Hydroxyprolin, Citrullin und Cana- vanin. Weiterhin beinhalten ALAMCAT-Tetrapeptide mindestens eine Aminosäure mit einer Seitenkette mit einem Stickstoffatom, das bei pH 6 überwiegend geladen vorliegt, z. B. Arg, Pro, Lys, His, Desmosin und Isodesmosin. Als vierte Aminosäure können ALAMCAT-Tetrapeptide jede beliebige Aminosäure enthalten; bevorzugt ist jedoch auch die vierte Aminosäure aus den drei vorstehend genannten Gruppen ausgewählt. Erfindungsgemäß bevorzugte, gegebenenfalls N-acylierte und/oder veresterte Pentapep- tide sind ausgewählt aus Lys-Thr-Thr-Lys-Ser und seinen N-acylierten Derivaten, beson¬ ders bevorzugt N-Palmitoyl-Lys-Thr-Thr-Lys-Ser, das unter der Bezeichnung Matrixyl von der Firma Sederma erhältlich ist, weiterhin N-Palmitoyl-Tyr-Gly-Gly-Phe-Met, VaI- Val-Arg-Pro-Pro, N-Palmitoyl-Tyr-Gly-Gly-Phe-Leu, Gly-Pro-Phe-Pro-Leu und N-Benzyl- oxycarbonyl-Gly-Pro-Phe-Pro-Leu (die beiden letztgenannten stellen Serinproteinase- Inhibitoren zur Inhibition der Desquamation dar). Erfindungsgemäß bevorzugte, gegebe¬ nenfalls N-acylierte und/oder veresterte Hexapeptide sind Val-Gly-Val-Ala-Pro-Gly und seine N-acylierten Derivate, besonders bevorzugt N-Palmitoyl-Val-Gly-Val-Ala-Pro-Gly, das unter der Bezeichnung Biopeptide EL von der Firma Sederma erhältlich ist, weiterhin Acetyl-Hexapeptide-3 (Argireline von Lipotec), Hexapeptide-4 (z. B. Collasyn 6KS von Therapeutic Peptide Inc. (TPI)), Hexapeptide-5 (z. B. Collasyn 6VY von TPI), Myristoyl Hexapeptide-5 (z. B. Collasyn 614VY von TPI), Myristoyl Hexapeptide-6 (z. B. Collasyn 614VG von TPI), Hexapeptide-8 (z. B. Collasyn 6KS von TPI), Myristoyl Hexapeptide-8 (z. B. Collasyn Lipo-6KS von TPI), Hexapeptide-9 (z. B. Collaxyl von Vincience) und Hexapeptide-10 (z. B. Collaxyl von Vincience oder Seriseline von Lipotec), Ala-Arg-His- Leu-Phe-Trp (Hexapeptide-1), Acetyl Hexapeptide-1 (z. B. Modulene von Vincience), Acetyl Glutamyl Hexapeptide-1 (z. B. SNAP-7 von Centerchem), Hexapeptide-2 (z. B. Melanostatine-DM von Vincience), Ala-Asp-Leu-Lys-Pro-Thr (Hexapeptide-3, z. B. Pep¬ tide 02 von Vincience), Val-Val-Arg-Pro-Pro-Pro, Hexapeptide-4 (z. B. Collasyn 6KS von Therapeutic Peptide Inc. (TPl)), Hexapeptide-5 (z. B. Collasyn 6VY von TPI), Myristoyl Hexapeptide-5 (z. B. Collasyn 614VY von TPI), Myristoyl Hexapeptide-6 (z. B. Collasyn 614VG von TPI), Ala-Arg-His-Methylnorleucin-Homophenylalanin-Trp (Hexapeptide-7), Hexapeptide-8 (z. B. Collasyn 6KS von TPI), Myristoyl Hexapeptide-8 (z. B. Collasyn Lipo-6KS von TPI), Hexapeptide-9 (z. B. Collaxyl von Vincience), Hexapeptide-10 (z. B. Collaxyl von Vincience oder Seriseline von Lipotec) und Hexapeptide-11 (z. B. Pept- amide-6 von Arch Personal Care). Ein erfindungsgemäß bevorzugtes Pentadecapeptid ist z. B. der Rohstoff Vinci 01 von Vincience (Pentadecapeptide-1). Erfindungsgemäß besonders bevorzugt ist die Kombination aus N-Palmitoyl-Gly-His-Lys und N-Palmitoyl-Gly-Gln-Pro-Arg, wie sie beispielsweise in dem Rohstoff Matrixyl 3000 von der Firma Sederma erhältlich ist.ALAMCAT tetrapeptides are tetrapeptides containing at least one amino acid with an aliphatic side chain, e.g. B. β-Ala, Ala, VaI, Leu, Pro, Sarcosine (Sar) and Isoleucine (He). Furthermore, ALAMCAT tetrapeptides contain at least one amino acid having a side chain with an amino group which is predominantly uncharged at neutral pH (pH 6-7), for example GIn, Asn, Lys, Om, 5-hydroxyproline, citrulline and canals. vanin. Furthermore, ALAMCAT tetrapeptides include at least one amino acid having a side chain with a nitrogen atom predominantly charged at pH 6, e.g. Arg, Pro, Lys, His, Desmosin and Isodesmosin. As the fourth amino acid, ALAMCAT tetrapeptides may contain any amino acid; however, preferably the fourth amino acid is also selected from the three abovementioned groups. Optionally N-acylated and / or esterified pentapep tides which are preferred according to the invention are selected from Lys-Thr-Thr-Lys-Ser and its N-acylated derivatives, more preferably N-palmitoyl-Lys-Thr-Thr-Lys-Ser which is available under the name Matrixyl from the company Sederma, furthermore N-palmitoyl-Tyr-Gly-Gly-Phe-Met, Val-Va-Arg-Pro-Pro, N-palmitoyl-Tyr-Gly-Gly-Phe- Leu, Gly-Pro-Phe-Pro-Leu and N-Benzyl-oxycarbonyl-Gly-Pro-Phe-Pro-Leu (the latter two are serine proteinase inhibitors for the inhibition of desquamation). Preference according to the invention, optionally N-acylated and / or esterified hexapeptides are Val-Gly-Val-Ala-Pro-Gly and its N-acylated derivatives, particularly preferably N-palmitoyl-Val-Gly-Val-Ala-Pro-Gly Acetyl-Hexapeptide-3 (Argireline from Lipotec), Hexapeptide-4 (eg Collasyn 6KS from Therapeutic Peptide Inc. (TPI)), Hexapeptide-5 (also referred to as Biopeptide EL from Sederma, eg Collasyn 6VY from TPI), myristoyl hexapeptide-5 (eg Collasyn 614VY from TPI), myristoyl hexapeptide-6 (eg Collasyn 614VG from TPI), hexapeptide-8 (eg Collasyn 6KS from TPI), myristoyl hexapeptide-8 (eg Collasyn Lipo-6KS from TPI), hexapeptide-9 (eg Collaxyl from Vincience) and hexapeptide-10 (eg Collaxyl from Vincience or Seriseline from Lipotec) , Ala-Arg-His-Leu-Phe-Trp (hexapeptide-1), acetyl hexapeptide-1 (e.g., modulene from Vincience), acetyl glutamyl hexapeptide-1 (e.g., SNAP-7 from Centerchem), hexapeptides -2 (eg melanostatine-DM from V incience), Ala-Asp-Leu-Lys-Pro-Thr (hexapeptide-3, e.g. Peptide 02 from Vincience), Val-Val-Arg-Pro-Pro-Pro, hexapeptide-4 (eg Collasyn 6KS of Therapeutic Peptide Inc. (TPI)), hexapeptide-5 (e.g., Collasyn 6VY from TPI), myristoyl hexapeptide-5 (e.g., Collasyn 614VY from TPI), myristoyl hexapeptide-6 (e.g., Collasyn 614VG from TPI), Ala-Arg-His-methylnorleucine-homophenylalanine-Trp (hexapeptide-7), hexapeptide-8 (eg Collasyn 6KS from TPI), myristoyl hexapeptide-8 (eg Collasyn Lipo-6KS from TPI) Hexapeptide-9 (eg, Collaxyl from Vincience), Hexapeptide-10 (eg, Collaxyl from Vincience, or Seriseline from Lipotec) and Hexapeptide-11 (eg, Peptamide-6 from Arch Personal Care). An inventively preferred pentadecapeptide is z. As the raw material Vinci 01 by Vincience (Pentadecapeptide-1). Particularly preferred according to the invention is the combination of N-palmitoyl-Gly-His-Lys and N-palmitoyl-Gly-Gln-Pro-Arg, as obtainable, for example, in the raw material Matrixyl 3000 from Sederma.
Die physiologisch verträglichen Salze der erfindungsgemäß bevorzugten Wirkstoffe, die Säuregruppen enthalten und Salze bilden können, sind ausgewählt aus den Ammonium- , Alkalimetall-, Magnesium-, Calcium-, Aluminium-, Zink- und Mangan-Salzen. Bevorzugt sind die Natrium-, Kalium-, Magnesium-, Aluminium-, Zink- und Mangan-Salze.The physiologically acceptable salts of the inventively preferred active ingredients containing acid groups and can form salts are selected from the ammonium, alkali metal, magnesium, calcium, aluminum, zinc and manganese salts. Preferred are the sodium, potassium, magnesium, aluminum, zinc and manganese salts.
Die Polymere der Aminosäuren und/oder der N-C2-C24-Acylaminosäuren sind ausge¬ wählt aus pflanzlichen und tierischen Proteinhydrolysaten und/oder Proteinen. Tierische Proteinhydrolysate sind z. B. Elastin-, Collagen-, Keratin-, Seiden- und Milcheiweiß-Pro- teinhydrolysate, die auch in Form von Salzen vorliegen können. Erfindungsgemäß bevorzugt sind pflanzliche Proteinhydrolysate, z. B. Soja-, Weizen-, Mandel-, Erbsen-, Kartoffel- und Reisproteinhydrolysate. Entsprechende Handelsprodukte sind z. B. DiaMin® (Diamalt), Gluadin® (Cognis), Lexein® (Inolex) und Crotein® (Croda). Besonders bevorzugt sind Sojaproteinhydrolysate, z. B. die Handelsprodukte Phytokine von Coletica oder Ridulisse C von Silab.The polymers of the amino acids and / or the NC 2 -C 24 -acylamino acids are selected from plant and animal protein hydrolysates and / or proteins. Animal protein hydrolysates are z. B. elastin, collagen, keratin, silk and milk protein protein hydrolyzates, which may also be present in the form of salts. Vegetable protein hydrolysates, eg. Soy, wheat, almonds, peas, potato and rice protein hydrolysates. Corresponding commercial products are z. B. DiaMin® ® (Diamalt) Gluadin ® (Cognis), Lexein ® (Inolex) and Crotein ® (Croda). Particularly preferred are soy protein hydrolysates, e.g. For example, the commercial products Phytokine from Coletica or Ridulisse C from Silab.
Proteinhydrolysate können naturgemäß auch monomere Aminosäuren und Oligopeptide enthalten; ihre Zusammensetzung ist normalerweise nicht definiert. Ebenfalls möglich ist der Einsatz von Acylderivaten der Proteinhydrolysate, z. B. in Form ihrer Fettsäure-Kondensationsprodukte. Entsprechende Handelsprodukte sind z. B. Lamepon® (Cognis), Gluadin® (Cognis), Lexein® (Inolex), Crolastin® oder Crotein® (Croda).Naturally, protein hydrolysates may also contain monomeric amino acids and oligopeptides; their composition is usually undefined. Also possible is the use of acyl derivatives of protein hydrolysates, z. In the form of their fatty acid condensation products. Corresponding commercial products are z. B. Lamepon ® (Cognis), Gluadin ® (Cognis), Lexein ® (Inolex), Crolastin ® ® or Crotein (Croda).
Erfindungsgemäß einsetzbar sind auch kationisierte Proteinhydrolysate. Bevorzugt sind kationische Proteinhydrolysate, deren zugrunde liegender Proteinanteil ein Molekularge¬ wicht von 100 bis zu 25000 Dalton, bevorzugt 250 bis 5000 Dalton aufweist. Weiterhin sind unter kationischen Proteinhydrolysaten quaternierte Aminosäuren und deren Gemi¬ sche zu verstehen. Weiterhin können die kationischen Proteinhydrolysate auch noch weiter derivatisiert sein. Als typische Beispiele für erfindungsgemäß verwendete kationi¬ sche Proteinhydrolysate und -derivate sind einige der unter den INCI- Bezeichnungen im "International Cosmetic Ingredient Dictionary and Handbook", (seventh edition 1997, The Cosmetic, Toiletry, and Fragrance Association 1101 17th Street, N.W., Suite 300, Washington, DC 20036-4702) genannten und im Handel erhältlichen Produkte aufge¬ führt: Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Steardimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Hydroxypropyl Hydrolyzed Rice Protein, Cocodi¬ monium Hydroxypropyl Hydrolyzed SiIk, Cocodimonium Hydroxypropyl Hydrolyzed Soy Protein, Cocodimonium Hydroxypropyl Hydrolyzed Wheat Protein, Cocodimonium Hydroxypropyl SiIk Amino Acids, Hydroxypropyl Arginine Lauryl/Myristyl Ether HCl. Ganz besonders bevorzugt sind die kationischen Proteinhydrolysate und -derivate auf pflanz¬ licher Basis.Cationized protein hydrolysates can also be used according to the invention. Preference is given to cationic protein hydrolysates whose protein content on which they are based has a molecular weight of from 100 to 25,000 daltons, preferably from 250 to 5,000 daltons. Farther are cationic protein hydrolyzates quaternized amino acids and their Gemi¬ cal understand. Furthermore, the cationic protein hydrolysates may also be further derivatized. Typical examples of cationic protein hydrolyzates and derivatives used in accordance with the invention are some of those listed under the INCI names in the International Cosmetic Ingredient Dictionary and Handbook, (seventh edition 1997, The Cosmetic, Toiletry, and Fragrance Association 1101 17 th Street, NW Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Steardimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Hydroxypropyl Hydrolyzed Rice Protein, Cocodimium Hydroxypropyl Hydrolyzed Silicon, Cocodimonium Hydroxypropyl Hydrolyzed Soy Protein, Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Hydroxypropyl Hydrolyzed Collagen, Cocodimonium Cocodimonium Hydroxypropyl Hydrolyzed Wheat Protein, Cocodimonium Hydroxypropyl SiCl Amino Acids, Hydroxypropyl Arginine Lauryl / Myristyl Ether HCl. Very particular preference is given to the cationic protein hydrolysates and derivatives based on plants.
In einer weiteren bevorzugten Ausführungsform sind die Polymeren der Aminosäuren ausgewählt aus DNA-Reparaturenzymen.In a further preferred embodiment, the polymers of the amino acids are selected from DNA repair enzymes.
Erfindungsgemäß bevorzugte DNA-Reparaturenzyme sind Photolyase und T4 Endonu- clease V, letztere im weiteren mit "T4N5" abgekürzt. Diese beiden Enzyme sind im Stand der Technik bereits als sogenannte DNA-Reparatur-Enzyme bekannt. Unter DNA-Repa¬ ratur ist definitionsgemäß die Spaltung bzw. Entfernung von UV-induzierten Pyrimidin- dimeren aus der DNA zu verstehen.DNA repair enzymes preferred according to the invention are photolyase and T4 endonuclease V, the latter being abbreviated to "T4N5" below. These two enzymes are already known in the art as so-called DNA repair enzymes. DNA repair is defined as the cleavage or removal of UV-induced pyrimidine dimers from the DNA.
Photolyase ist die Kurzbezeichnung für Desoxyribodipyrimidin-Photolyase bzw. DNA- Photolyase, ein Enzym mit der Klassifizierungsnummer EC 4.1.99.3. Eine besonders effi¬ ziente Photolyase stammt aus Anacystis nidulans, einem phototrophen marinen Mikroor¬ ganismus. Die Photolyase aus A. nidulans wird in technisch relevanten Mengen mittler¬ weile aus E. coli gewonnen. Photolyase ist zur Aktivierung auf Licht angewiesen. Das Enzym T4 Endonuclease V wird vom denV-Gen der Bakteriophage T4 produziert und gehört zu den Phosphodiesterasen, die die Nucleinsäuren an der (5"-3")-Bindung hydrolytisch spalten. T4N5 ist auch ohne Lichteinfluss aktiv.Photolyase is the abbreviation for deoxyribodipyrimidine photolyase or DNA photolyase, an enzyme with the classification number EC 4.1.99.3. A particularly effi¬ tient photolyase comes from Anacystis nidulans, a phototrophic marine microorganism. The photolyase from A. nidulans is now obtained in technically relevant quantities from E. coli. Photolyase relies on light for activation. The enzyme T4 endonuclease V is produced by the denV gene of bacteriophage T4 and belongs to the phosphodiesterases which hydrolytically cleave the nucleic acids at the (5 " -3 " ) bond. T4N5 is also active without the influence of light.
Erfindungsgemäß besonders bevorzugt ist der Einsatz von liposomenverkapselten DNA- Reparaturenzymen. Liposomenverkapselte Photolyase ist im Handel z. B. unter der Pro¬ duktbezeichnung Photosome™, liposomenverkapselte T4N5 z. B. unter der Bezeichnung Ultrasome™ von der Firma AGI Dermatics, USA, erhältlich. Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass sie mindestens einen der Rohstoffe Photosome™ oder Ultrasome™ in einer Gesamtmenge von 0,1 - 10 Gew.-%, bevorzugt 0,5 - 5,0 Gew.-% und besonders bevor¬ zugt 1,0 -4,0 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, enthalten. Weitere bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekenn¬ zeichnet, dass sie mindestens ein Oligomer oder Polymer von Aminosäuren, N-C2-C24- Acylaminosäuren und/oder den Estern und/oder den physiologisch verträglichen Salzen dieser Substanzen in einer Gesamtmenge von 0,000001 - 5 Gew.-%, bevorzugt 0,00001 - 2 Gew.-%, besonders bevorzugt 0,0001 - 1 Gew.-% und außerordentlich bevorzugt 0,005 - 0,5 Gew.-%, jeweils bezogen auf den Gehalt an Aktivsubstanz in der gesamten Zusammensetzung, enthalten.Particularly preferred according to the invention is the use of liposome-encapsulated DNA repair enzymes. Liposome-encapsulated photolyase is commercially available for. B. under the Pro¬ duktbezeichnung Photosome ™, liposome-encapsulated T4N5 z. B. under the name Ultrasome ™ from AGI Dermatics, USA, available. Preferred compositions according to the invention are characterized in that they contain at least one of the raw materials Photosome ™ or Ultrasome ™ in a total amount of 0.1-10% by weight, preferably 0.5-5.0% by weight and more preferably 1 , 0 -4.0 wt .-%, each based on the total composition. Further preferred compositions according to the invention are characterized in that they contain at least one oligomer or polymer of amino acids, NC 2 -C 24 -acylamino acids and / or the esters and / or the physiologically tolerable salts of these substances in a total amount of 0.000001-5 Wt .-%, preferably 0.00001 - 2 wt .-%, particularly preferably 0.0001 - 1 wt .-% and most preferably 0.005 - 0.5 wt .-%, each based on the content of active substance in the whole Composition, included.
In einer weiteren bevorzugten Ausführungsform liegen die Monomeren, Oligomeren und Polymeren von Aminosäuren, N-C2-C24-Acylaminosäuren, den Estern und/oder den phy¬ siologisch verträglichen Salzen dieser Substanzen in geträgerter Form vor, insbesondere aufgetragen auf feinteiligen, pulverförmigen Substraten wie Kieselgel, insbesondere Aerosil-Typen, Talkum, Microsponges, modifizierten Stärken und Stärkederivaten, kristalliner Cellulose, Cellulosepulvern, Lactoglobulinderivaten, Polymerpartikeln aus Nylon, Polyolefinen, Polycarbonaten, Polyurethanen, Polyacrylaten, (Meth)acrylat- oder (Meth)acrylat-Vinyliden-Copolymeren, die vernetzt sein können, Polyestern, Polyamiden, Polystyrolen, Teflon und Siliconen. Ein besonders bevorzugter Rohstoff dieser Art sind die Vegetal Filling Spheres von Coletica.In a further preferred embodiment, the monomers, oligomers and polymers of amino acids, NC 2 -C 24 -acylamino acids, the esters and / or the physiologically tolerable salts of these substances are present in supported form, in particular applied to finely divided, pulverulent substrates such as silica gel , in particular Aerosil types, talc, microsponges, modified starches and starch derivatives, crystalline cellulose, cellulose powders, lactoglobulin derivatives, polymer particles of nylon, polyolefins, polycarbonates, polyurethanes, polyacrylates, (meth) acrylate or (meth) acrylate-vinylidene copolymers may be crosslinked, polyesters, polyamides, polystyrenes, Teflon and silicones. A particularly preferred raw material of this type are the Vegetal Filling Spheres of Coletica.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen neben dem Extrakt aus den Bohnen von Kakao (Theobroma cacao) und dem Extrakt aus den Blättern der Pfefferminze (Mentha piperita) mindestens ein DNA-Oligonucleotid oder ein RNA-Oligonucleotid.In a further preferred embodiment, the compositions according to the invention contain at least one DNA oligonucleotide or an RNA oligonucleotide in addition to the extract of the beans of cocoa (Theobroma cacao) and the extract of the leaves of peppermint (Mentha piperita).
Erfindungsgemäß werden unter einem Oligonucleotid Polymerisate aus 2 bis 20, bevor¬ zugt 2 bis 10 Mononucleotiden verstanden, die ebenso wie bei Polynucleotiden und Nucleinsäuren durch Phosphorsäurediester-Brücken verknüpft sind. Die Nucleotide be¬ stehen aus Nucleobasen (meist Pyrimidin- oder Purin-Derivaten), Pentosen (meist D-Ribofuranose oder 2-Desoxy-D-ribofuranose in ß-N-glykosidischer Bindung an die Nucleobase) und Phosphorsäure. Die Mononucleotide sind zum Beispiel Adenosinphos- phate, Cytidinphosphate, Guanosinphosphate, Uridinphosphate und Thymidinphospha- te, insbesondere CMP (Cytidin-5'-monophosphat), UDP (Uridin-5'-diphosphat), ATP (Adenosin-5 '-triphosphat) und GTP (Guanosin-5'-triphosphat). Ein erfindungsgemäß besonders bevorzugtes Oligonucleotid ist das Thymidin-Dinucleo- tid.According to the invention, an oligonucleotide is understood as meaning polymers of from 2 to 20, preferably from 2 to 10, mononucleotides which, like polynucleotides and nucleic acids, are linked by phosphoric diester bridges. The nucleotides be¬ from nucleobases (usually pyrimidine or purine derivatives), pentoses (usually D-ribofuranose or 2-deoxy-D-ribofuranose in ß-N-glycosidic bond to the nucleobase) and phosphoric acid. The mononucleotides are, for example, adenosine phosphates, cytidine phosphates, guanosine phosphates, uridine phosphates and thymidine phosphates, in particular CMP (cytidine 5'-monophosphate), UDP (uridine 5'-diphosphate), ATP (adenosine 5'-triphosphate) and GTP (guanosine 5'-triphosphate). An oligonucleotide particularly preferred according to the invention is the thymidine dinucleotide.
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass sie mindestens ein DNA-Oligonucleotid oder RNA-Oligonucleotid in einer Gesamt¬ menge von 0,0001 - 5 Gew.-%, bevorzugt 0,001 - 1,0 Gew.-% und besonders bevorzugt 0,01 - 0,5 Gew.-%, bezogen auf die gesamte Zusammensetzung, enthalten.Preferred compositions according to the invention are characterized in that they contain at least one DNA oligonucleotide or RNA oligonucleotide in a total amount of 0.0001-5 wt.%, Preferably 0.001-1.0 wt.% And particularly preferably 0.01 - 0.5 wt .-%, based on the total composition.
Erfindungsgemäß bevorzugte natürliche Betainverbindungen sind natürlich vorkommen¬ de Verbindungen mit der Atomgruppierung R3N+-CH2-X-COO"" gemäß lUPAC-Regel C- 816.1. Sogenannte Betaintenside (synthetisch) fallen nicht unter die erfindungsgemäß verwendeten Betainverbindungen, ebenso wenig andere zwitterionische Verbindungen, in denen sich die positive Ladung an N oder P und die negative Ladung formal an O, S, B oder C befindet, die aber nicht der lUPAC-Regel C-816.1 entsprechen. Erfindungs¬ gemäß bevorzugte Betainverbindungen sind Betain (Me3N+-CH2-COO") und Carnitin (Me3N+-CH2-CHOH-CH2-COO-), jeweils mit Me = Methyl.Naturally preferred natural betaine compounds according to the invention are naturally occurring compounds with the atomic grouping R 3 N + -CH 2 -X-COO "" according to IUPAC Rule C-816.1. So-called betaine surfactants (synthetic) do not fall under the betaine compounds used according to the invention, nor any other zwitterionic compounds in which the positive charge on N or P and the negative charge formally reside on O, S, B or C, but which are not those of IUPAC. Comply with rule C-816.1. According to the invention preferred betaine compounds are betaine (Me 3 N + -CH 2 -COO " ) and carnitine (Me 3 N + -CH 2 -CHOH-CH 2 -COO-), each with Me = methyl.
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass sie mindestens eine natürliche Betainverbindung in einer Gesamtmenge von 0,05 bis 5 Gew.-%, bevorzugt 0,1 bis 3 Gew.-%, besonders bevorzugt 0,5 bis 2 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, enthalten.Preferred compositions according to the invention are characterized in that they contain at least one natural betaine compound in a total amount of 0.05 to 5 wt.%, Preferably 0.1 to 3 wt.%, Particularly preferably 0.5 to 2 wt. in each case based on the total composition.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen mindestens ein Vitamin, Provitamin oder eine als Vitaminvorstufe bezeichnete Verbindung aus den Vitamingruppen A, B, C, E, H und K und den Estern der vorgenannten Substanzen.In a further preferred embodiment, the compositions according to the invention comprise at least one vitamin, provitamin or a compound designated as vitamin precursor from the vitamin groups A, B, C, E, H and K and the esters of the abovementioned substances.
Zur Gruppe der als Vitamin A bezeichneten Substanzen gehören das Retinol (Vitamin A1) sowie das 3,4-Didehydroretinol (Vitamin A2). Das ß-Carotin ist das Provitamin des Retinols. Als Vitamin A-Komponente kommen erfindungsgemäß beispielsweise Vitamin A-Säure und deren Ester, Vitamin A-Aldehyd und Vitamin A-Alkohol sowie dessen Ester, wie Retinylpalmitat und Retinylacetat in Betracht. Die erfindungsgemäßen Zusammen¬ setzungen enthalten die Vitamin A-Komponente bevorzugt in Mengen von 0,05 - 1 Gew.- %, bezogen auf die gesamte Zusammensetzung.The group of substances called vitamin A includes retinol (vitamin A 1 ) and 3,4-didehydroretinol (vitamin A 2 ). The ß-carotene is the provitamin of retinol. As vitamin A component according to the invention, for example, vitamin A acid and its esters, vitamin A aldehyde and vitamin A alcohol and its esters, such as retinyl palmitate and retinyl acetate into consideration. The compositions according to the invention preferably contain the vitamin A component in quantities of 0.05-1% by weight, based on the total composition.
Zur Vitamin B-Gruppe oder zu dem Vitamin B-Komplex gehören unter anderem Vitamin B1, Trivialname Thiamin, chemische Bezeichung 3-[(4'-Amino-2'-methyl- 5'-pyrimidinyl)-methyl]-5-(2-hydroxyethyl)-4-methylthiazoliumchlorid. Bevorzugt wird Thiaminhydrochlorid in Mengen von 0,05 bis 1 Gew.-%, bezogen auf die ge¬ samte Zusammensetzung, eingesetzt.The vitamin B group or the vitamin B complex include, among others Vitamin B 1, thiamine trivial name, chemical designation 3 - [(4 '-amino-2'-methyl-5' -pyrimidinyl) methyl] -5- (2-hydroxyethyl) -4-methylthiazolium chloride. Thiamine hydrochloride is preferably used in amounts of from 0.05 to 1% by weight, based on the total composition.
Vitamin B2, Trivialname Riboflavin, chemische Bezeichung 7,8-Dimethyl-10-(1-D- ribityl)-benzo[g]pteridin-2,4(3/-/,10/-/)-dion. Bevorzugt werden Riboflavin oder seine Derivate in Mengen von 0,05 bis 1 Gew.-%, bezogen auf die gesamte Zu¬ sammensetzung, eingesetzt.Vitamin B 2 , common name riboflavin, chemical name 7,8-dimethyl-10- (1-D-ribityl) -benzo [g] pteridine-2,4 (3 / - /, 10 / - /) - dione. Riboflavin or its derivatives are preferably used in amounts of from 0.05 to 1% by weight, based on the total composition.
Vitamin B3. Unter dieser Bezeichnung werden die Verbindungen Nicotinsäure und Nicotinsäureamid (Niacinamid) geführt. Erfindungsgemäß bevorzugt ist das Nicotinsäureamid, das in den erfindungsgemäßen Mitteln bevorzugt in Mengen von 0,05 bis 1 Gew.-%, bezogen auf die gesamte Zusammensetzung, enthalten ist.Vitamin B 3 . Under this name, the compounds nicotinic acid and nicotinamide (niacinamide) are performed. Preferred according to the invention is the nicotinic acid amide, which is preferably present in the agents according to the invention in amounts of from 0.05 to 1% by weight, based on the total composition.
Vitamin B5 (Pantothensäure und Panthenol). Bevorzugt wird Panthenol einge¬ setzt. Erfindungsgemäß einsetzbare Derivate des Panthenols sind insbesondere die Ester und Ether des Panthenols sowie kationisch derivatisierte Panthenole. In einer weiteren bevorzugten Ausführungsform der Erfindung können an Stelle von sowie zusätzlich zu Pantothensäure oder Panthenol auch Derivate des 2-Furanon mit der allgemeinen Strukturformel (I) eingesetzt werden.Vitamin B 5 (pantothenic acid and panthenol). Panthenol is preferably used. Derivatives of panthenol which can be used according to the invention are, in particular, the esters and ethers of panthenol and also cationically derivatized panthenols. In a further preferred embodiment of the invention, instead of and in addition to pantothenic acid or panthenol, it is also possible to use derivatives of 2-furanone having the general structural formula (I).
Figure imgf000018_0001
Figure imgf000018_0001
(D(D
Bevorzugt sind die 2-Furanon-Derivate, in denen die Substituenten R1 bis R6 unab¬ hängig voneinander ein Wasserstoffatom, einen Hydroxylrest, einen Methyl-, Meth- oxy-, Aminomethyl- oder Hydroxymethylrest, einen gesättigten oder ein- oder zwei¬ fach ungesättigten, linearen oder verzweigten C2-C4 - Kohlenwasserstoffrest, einen gesättigten oder ein- oder zweifach ungesättigten, verzweigten oder linearen Mono-, Di- oder Trihydroxy-C2-C4 - Kohlenwasserstoffrest oder einen gesättigten oder ein- oder zweifach ungesättigten, verzweigten oder linearen Mono-, Di- oder Triamino- C2-C4 - Kohlenwasserstoffrest darstellen. Besonders bevorzugte Derivate sind die auch im Handel erhältlichen Substanzen Dihydro-3-hydroxy-4,4-dimethyl-2(3H)-fura- non mit dem Trivialnamen Pantolacton (Merck), 4-Hydroxymethyl-γ-butyrolacton (Merck), 3,3-Dimethyl-2-hydroxy-γ-butyrolacton (Aldrich) und 2,5-Dihydro-5-methoxy- 2-furanon (Merck), wobei ausdrücklich alle Stereoisomeren eingeschlossen sind. Das erfindungsgemäß außerordentlich bevorzugte 2-Furanon-Derivat ist Pantolacton (Di- hydro-3-hydroxy-4,4-dimethyl-2(3H)-furanon), wobei in Formel (I) R1 für eine Hydro¬ xylgruppe, R2 für ein Wasserstoffatom, R3 und R4 für eine Methylgruppe und R5 und R6 für ein Wasserstoffatom stehen. Das Stereoisomer (R)-Pantolacton entsteht beim Abbau von Pantothensäure.Preference is given to the 2-furanone derivatives in which the substituents R 1 to R 6 independently of one another are a hydrogen atom, a hydroxyl radical, a methyl, methoxy, aminomethyl or hydroxymethyl radical, a saturated or one or two unsaturated, linear or branched C 2 -C 4 -hydrocarbon radical, a saturated or mono- or diunsaturated, branched or linear mono-, di- or trihydroxy-C 2 -C 4 -hydrocarbon radical or a saturated or mono- or diunsaturated one , branched or linear mono-, di- or triamino- Represent C 2 -C 4 hydrocarbon radical. Particularly preferred derivatives are the commercially available substances dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone with the trivial name pantolactone (Merck), 4-hydroxymethyl-γ-butyrolactone (Merck), 3 , 3-dimethyl-2-hydroxy-γ-butyrolactone (Aldrich) and 2,5-dihydro-5-methoxy-2-furanone (Merck), expressly including all stereoisomers. The inventively extraordinarily preferred 2-furanone derivative is pantolactone (dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone), wherein in formula (I) R 1 is a hydroxyl group, R 2 represents a hydrogen atom, R 3 and R 4 represent a methyl group, and R 5 and R 6 represent a hydrogen atom. The stereoisomer (R) -pantolactone is formed during the degradation of pantothenic acid.
Die genannten Verbindungen des Vitamin B5-Typs sowie die 2-Furanonderivate sind in den erfindungsgemäßen Mitteln in einer Gesamtmenge von 0,05 bis 5 Gew.-%, bevorzugt 0,1 bis 3 Gew.-%, besonders bevorzugt 0,5 bis 2 Gew.-%, jeweils bezo¬ gen auf die gesamte Zusammensetzung, enthalten.The said compounds of the vitamin B 5 type and the 2-furanone derivatives are present in the compositions according to the invention in a total amount of 0.05 to 5 wt.%, Preferably 0.1 to 3 wt.%, Particularly preferably 0.5 to 2% by weight, in each case based on the total composition.
Vitamin B6, wobei man hierunter keine einheitliche Substanz, sondern die unter den Trivialnamen Pyridoxin, Pyridoxamin und Pyridoxal bekannten Derivate des 5-Hydroxymethyl-2-methylpyridin-3-ols versteht. Vitamin B6 ist in den erfindungs¬ gemäßen Zusammensetzungen bevorzugt in Mengen von 0,0001 bis 1,0 Gew.- %, insbesondere in Mengen von 0,001 bis 0,01 Gew.-%, enthalten.Vitamin B 6 , which is understood hereunder not a uniform substance, but the known under the common names pyridoxine, pyridoxamine and pyridoxal derivatives of 5-hydroxymethyl-2-methylpyridin-3-ol. Vitamin B 6 is preferably present in the compositions according to the invention in amounts of 0.0001 to 1.0% by weight, in particular in amounts of 0.001 to 0.01% by weight.
Vitamin B7 (Biotin), auch als Vitamin H oder "Hautvitamin" bezeichnet. Bei Biotin handelt es sich um (3aS,4S, 6aR)-2-Oxohexahydrothienol[3,4-c/j-imidazol-4-vale- riansäure. Biotin ist in den erfindungsgemäßen Zusammensetzungen bevorzugt in Mengen von 0,0001 bis 1 ,0 Gew.-%, insbesondere in Mengen von 0,001 bis 0,01 Gew.-% enthalten.Vitamin B 7 (biotin), also known as vitamin H or "skin vitamin". Biotin is (3aS, 4S, 6aR) -2-oxohexahydrothienol [3,4-c / i-imidazole-4-valeric acid. Biotin is preferably present in the compositions according to the invention in amounts of from 0.0001 to 1.0% by weight, in particular in amounts of from 0.001 to 0.01% by weight.
Zur Vitamin C-Gruppe zählen Vitamin C (Ascorbinsäure) und seine Derivate, insbeson¬ dere die Ester der Ascorbinsäure mit organischen und anorganischen Säuren und deren Salze, sowie die Acetale mit Glucose oder anderen Zuckern, insbesondere Ascorbylglu- cosid. Vitamin C und/oder mindestens eines seiner Derivate wird bevorzugt in einer Gesamtmenge von 0,1 bis 3 Gew.-%, bezogen auf die gesamte Zusammensetzung, ein¬ gesetzt. Die Verwendung der Derivate Ascorbylpalmitat, -stearat, -dipalmitat, -acetat, Mg-Ascorbylphosphat, Na-Ascorbylphosphat, Natrium- und Magnesiumascorbat, Dinatri- umascorbylphosphat und -sulfat, Kaliumascorbyltocopherylphosphat, Chitosanascorbat oder Ascorbylglucosid kann bevorzugt sein. Die Verwendung mindestens eines Mitglieds der Vitamin C - Gruppe in Kombination mit Tocopherolen und/oder anderen Mitgliedern der Vitamin E - Gruppe kann ebenfalls bevorzugt sein.The vitamin C group includes vitamin C (ascorbic acid) and its derivatives, in particular the esters of ascorbic acid with organic and inorganic acids and their salts, and also the acetals with glucose or other sugars, in particular ascorbyl glucoside. Vitamin C and / or at least one of its derivatives is preferably used in a total amount of from 0.1 to 3% by weight, based on the total composition. The use of the derivatives ascorbyl palmitate, stearate, dipalmitate, acetate, Mg ascorbyl phosphate, Na ascorbyl phosphate, sodium and magnesium ascorbate, disodium ascorbyl phosphate and sulfate, potassium ascorbyl tocopheryl phosphate, chitosan ascorbate or ascorbyl glucoside may be preferred. The use of at least one member of the vitamin C group in combination with tocopherols and / or other members of the vitamin E group may also be preferred.
Zur Vitamin E-Gruppe zählen Tocopherol, insbesondere α-Tocopherol, und seine Deri¬ vate. Bevorzugte Derivate sind insbesondere die Ester, wie Tocopherylacetat, -nicotinat, -phosphat, -succinat, -linoleat, -oleat, Tocophereth-5, Tocophereth-10, Tocophereth-12, Tocophereth-18, Tocophereth-50 und Tocophersolan. Tocopherol und seine Derivate sind bevorzugt in einer Gesamtmenge von 0,05 - 1 Gew.-%, bezogen auf die gesamte Zusammensetzung, enthalten.The vitamin E group includes tocopherol, in particular α-tocopherol, and its derivatives Deri. Preferred derivatives are in particular the esters, such as tocopheryl acetate, nicotinate, phosphate, succinate, linoleate, oleate, tocophereth-5, tocophereth-10, tocophereth-12, tocophereth-18, tocophereth-50 and tocopherol. Tocopherol and its derivatives are preferably contained in a total amount of 0.05 - 1 wt .-%, based on the total composition.
Unter Vitamin F werden üblicherweise essentielle Fettsäuren, insbesondere Linolsäure, Linolensäure und Arachidonsäure, verstanden.Vitamin F is usually understood as meaning essential fatty acids, in particular linoleic acid, linolenic acid and arachidonic acid.
Vitamin H ist eine andere Bezeichnung für Biotin oder Vitamin B7 (siehe oben). Zu den fettlöslichen Vitaminen der Vitamin K-Gruppe, denen das Grundgerüst des 2-Methyl-1 ,4-naphthochinons zugrunde liegt, gehören Phyllochinon (Vitamin Ki), Farno- chinon oder Menachinon-7 (Vitamin K2) und Menadion (Vitamin K3). Vitamin K ist bevor¬ zugt in Mengen von 0,0001 bis 1,0 Gew.-%, insbesondere 0,01 bis 0,5 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, enthalten.Vitamin H is another name for biotin or vitamin B 7 (see above). The fat-soluble vitamins of the vitamin K group, which the backbone of 2-methyl-1, is 4-naphthoquinone based belong phylloquinone (vitamin Ki), quinone Farno- or menaquinone-7 (vitamin K2) and menadione (vitamin K 3 ). Vitamin K is preferably present in amounts of from 0.0001 to 1.0% by weight, in particular from 0.01 to 0.5% by weight, in each case based on the total composition.
Vitamin A-palmitat (Retinylpalmitat), Panthenol, Pantolacton, Nicotinsäureamid, Pyrido- xin, Pyridoxamin, Pyridoxal, Biotin, Ascorbylpalmitat, -acetat, Mg-Ascorbylphosphat, Na- Ascorbylphosphat, Natrium- und Magnesiumascorbat und die Tocopherolester, beson¬ ders Tocopherylacetat, sind erfindungsgemäß besonders bevorzugt.Vitamin A palmitate (retinyl palmitate), panthenol, pantolactone, nicotinamide, pyridoxine, pyridoxamine, pyridoxal, biotin, ascorbyl palmitate, acetate, Mg ascorbyl phosphate, Na ascorbyl phosphate, sodium and magnesium ascorbate and the tocopherol esters, especially tocopheryl acetate, are particularly preferred according to the invention.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen mindestens eine α-Hydroxycarbonsäure, α-Ketocarbonsäure oder ß-Hydroxycarbonsäure oder deren Ester-, Lacton- oder Salzform. Erfindungsgemäß be¬ vorzugte α-Hydroxycarbonsäuren oder α-Ketocarbonsäuren sind Glycolsäure, Milch¬ säure, Weinsäure, Citronensäure, 2-Hydroxybutansäure, 2,3-Dihydroxypropansäure, 2- Hydroxypentansäure, 2-Hydroxyhexansäure, 2-Hydroxyheptansäure, 2-Hydroxyoctan- säure, 2-Hydroxydecansäure, 2-Hydroxydodecansäure, 2-Hydroxytetradecansäure, 2- Hydroxyhexadecansäure, 2-Hydroxyoctadecansäure, Mandelsäure, 4-Hydroxymandel- säure, Äpfelsäure, Erythrarsäure, Threarsäure, Glucarsäure, Galactarsäure, Mannar- säure, Gularsäure, 2-Hydroxy-2-methylbernsteinsäure, Gluconsäure, Brenztrauben- säure, Glucuronsäure und Galacturonsäure. Besonders bevorzugte α-Hydroxycarbon¬ säuren sind Milchsäure, Citronensäure, Glycolsäure und Gluconsäure. Eine besonders bevorzugte ß-Hydroxycarbonsäure ist Salicylsäure. Die Ester der genannten Säuren sind bevorzugt ausgewählt aus den Methyl-, Ethyl-, Propyl-, Isopropyl-, Butyl-, Amyl-, Pentyl-, Hexyl-, 2-Ethylhexyl-, Octyl-, Decyl-, Dodecyl- und Hexadecylestern. Besonders bevor¬ zugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass min¬ destens eine α-Hydroxycarbonsäure, α-Ketocarbonsäure und/ oder ß-Hydroxycarbon- säure und/oder mindestens ein Derivat hiervon in einer Gesamtmenge von 0,1 - 10 Gew.-%, bevorzugt 0,5 - 5 Gew.-%, jeweils bezogen auf die gesamte Zusammenset¬ zung, enthalten ist.In a further preferred embodiment, the compositions according to the invention contain at least one α-hydroxycarboxylic acid, α-ketocarboxylic acid or β-hydroxycarboxylic acid or their ester, lactone or salt form. Preferred α-hydroxycarboxylic acids or α-ketocarboxylic acids according to the invention are glycolic acid, lactic acid, tartaric acid, citric acid, 2-hydroxybutanoic acid, 2,3-dihydroxypropanoic acid, 2-hydroxypentanoic acid, 2-hydroxyhexanoic acid, 2-hydroxyheptanoic acid, 2-hydroxyoctanoic acid, 2-hydroxydecanoic acid, 2-hydroxydodecanoic acid, 2-hydroxytetradecanoic acid, 2-hydroxyhexadecanoic acid, 2-hydroxyoctadecanoic acid, mandelic acid, 4-hydroxymandelic acid, malic acid, erythraric acid, threaric acid, glucaric acid, galactaric acid, mannaric acid, gular acid, 2-hydroxy-2- methylsuccinic acid, gluconic acid, pyruvic acid, glucuronic acid and galacturonic acid. Particularly preferred α-hydroxycarboxylic acids are lactic acid, citric acid, glycolic acid and gluconic acid. A particularly preferred β-hydroxycarboxylic acid is salicylic acid. The esters of said acids are preferably selected from the methyl, ethyl, propyl, isopropyl, butyl, amyl, pentyl, hexyl, 2-ethylhexyl, octyl, decyl, dodecyl and hexadecyl esters. Particularly preferred compositions according to the invention are characterized in that at least one α-hydroxycarboxylic acid, α-ketocarboxylic acid and / or β-hydroxycarboxylic acid and / or at least one derivative thereof are present in a total amount of 0.1-10% by weight. , Preferably 0.5 to 5 wt .-%, in each case based on the total composition, is contained.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen mindestens ein Flavonoid oder mindestens einen Flavonoid- reichen Pflanzenextrakt.In a further preferred embodiment, the compositions according to the invention contain at least one flavonoid or at least one flavonoid-rich plant extract.
Die erfindungsgemäß bevorzugten Flavonoide umfassen die Glycoside der Flavone, der Flavanone, der 3-Hydroxyflavone (Flavonole), der Aurone und der Isoflavone. Besonders bevorzugte Flavonoide sind ausgewählt aus Naringin (Aurantiin, Naήngenin-7-rhamno- glucosid), α-Glucosylrutin, α-Glucosylmyricetin, α-Glucosylisoquercetin, α-Glucosylquer- cetin, Isoquercitrin (Quercetin-3-O-ß-D-glucofuranosid), Hesperidin (3',5,7-Trihydroxy-4'- methoxyflavanon-7-rhamnoglucosid, Hesperitin-7-O-rhamnoglucosid), Neohesperidin, Rutin (S.S'^'.δJ-Pentahydroxyflavon-S-rhamnoglucosid, Quercetin-3-rhamnoglucosid), Troxerutin (3,5-Dihydroxy-3',4',7-tris(2-hydroxyethoxy)-flavon-3-(6-O-(6-deoxy-α-L-man- nopyranosyl)-ß-D-glucopyranosid)), Monoxerutin (3,3',4',5-Tetrahydroxy-7-(2-hydroxy- ethoxy)-flavon-3-(6-O-(6-deoxy-α-L-mannopyranosyl)-ß-D-glucopyranosid)), Diosmin (3',4',7-Trihydroxy-5-methoxyflavanon-7-rhamnoglucosid), Eriodictin, Apigenin-7-glucosid (4',5,7-Trihydroxyflavon-7-glucosid), (S)- und (R)-Eriodictyol-6-C-ß-D-glucopyranosid, Orientin, Isoorientin.Vitexin, Isovitexin, Vicenin-2, Schaftosid, Isoschaftosid und Luteolin. Erfindungsgemäß außerordentlich bevorzugte Flavonoide sind α-Glucosylrutin, Naringin, Apigenin-7-glucosid, α-Glucosylquercetin, Isoquercitrin und Orientin. Ebenfalls bevorzugt sind die aus zwei Flavonoideinheiten aufgebauten Biflavonoide, die z. B. in Gingko-Arten vorkommen. Weitere bevorzugte Flavonoide sind die Chalkone, vor allem Phloricin, Neohesperidindihydrochalkon, Aspalathin und Nothofagin. Besonders bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekenn¬ zeichnet, dass mindestens ein Flavonoid und/oder mindestens einen Flavonoid-reicher Pflanzenextrakt in einer Gesamtmenge von 0,0001 bis 1 Gew.-%, bevorzugt 0,0005 bis 0,5 Gew.-% und besonders bevorzugt 0,001 bis 0,1 Gew.-%, jeweils bezogen auf die Flavonoidaktivsubstanz in der gesamten Zusammensetzung, enthalten ist. In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen mindestens ein Isoflavonoid oder mindestens einen Isoflavonoid- reichen Pflanzenextrakt. Zu den Isoflavonoiden werden an dieser Stelle die Isoflavone und die Isoflavon-Glycoside gezählt.The flavonoids preferred according to the invention include the glycosides of the flavones, the flavanones, the 3-hydroxyflavones (flavonols), the aurones and the isoflavones. Particularly preferred flavonoids are selected from naringin (aurantiin, Naήngenin-7-rhamnoglucosid), α-glucosylrutin, α-glucosylmyricetin, α-glucosylisoquercetin, α-glucosyl-cerecetin, isoquercitrin (quercetin-3-O-β-D-glucofuranoside ), Hesperidin (3 ', 5,7-trihydroxy-4'-methoxyflavanone-7-rhamnoglucoside, hesperetin-7-O-rhamnoglucoside), neohesperidin, rutin (S.S'''.δJ-pentahydroxyflavone-S-rhamnoglucoside, Quercetin-3-rhamnoglucoside), troxerutin (3,5-dihydroxy-3 ', 4', 7-tris (2-hydroxyethoxy) -flavone-3- (6-O- (6-deoxy-α-L-man-) nopyranosyl) -β-D-glucopyranoside)), monoxerutin (3,3 ', 4', 5-tetrahydroxy-7- (2-hydroxyethoxy) flavone-3- (6-O- (6-deoxy-α -L-mannopyranosyl) -β-D-glucopyranoside)), diosmin (3 ', 4', 7-trihydroxy-5-methoxyflavanone-7-rhamnoglucoside), eriodictin, apigenin-7-glucoside (4 ', 5,7- Trihydroxyflavone-7-glucoside), (S) - and (R) -iodiodictyol-6-C-.beta.-D-glucopyranoside, orientin, isoorientin. Vitexin, isovitexin, vicenin-2, shankoside, isoschaftoside and luteolin. Extremely preferred flavonoids according to the invention are α-glucosylrutin, naringin, apigenin-7-glucoside, α-glucosylquercetin, isoquercitrin and orientin. Also preferred are the constructed from two flavonoid biflavonoids, z. B. occur in gingko species. Other preferred flavonoids are the chalcones, especially phloricin, neohesperidin dihydrochalcone, aspalathin and nothofagin. Particularly preferred compositions according to the invention are characterized in that at least one flavonoid and / or at least one flavonoid-rich plant extract in a total amount of 0.0001 to 1 wt .-%, preferably 0.0005 to 0.5 wt .-% and particularly preferably 0.001 to 0.1 wt .-%, each based on the flavonoid active substance in the total composition is included. In a further preferred embodiment, the compositions according to the invention contain at least one isoflavonoid or at least one isoflavonoid-rich plant extract. The isoflavones and the isoflavone glycosides are counted at this point as isoflavonoids.
Unter Isoflavonen sind im Sinne der vorliegenden Erfindung Stoffe zu verstehen, die Hydrierungs-, Oxidations- oder Substitutionsprodukte des 3-Phenyl-4H-1-benzopyrans darstellen, wobei eine Hydrierung in der 2,3-Stellung des Kohlenstoffgerüsts vorliegen kann, eine Oxidation unter Ausbildung einer Carbonylgruppe in der 4-Stellung vorliegen kann, und unter Substitution der Ersatz eines oder mehrerer Wasserstoffatome durch Hydroxy- oder Methoxy-Gruppen zu verstehen ist. Zu den erfindungsgemäß bevorzugten Isoflavonen zählen beispielsweise Daidzein, Genistein, Prunetin, Biochanin, Orobol, Santal, Pratensein, Irigenin, Glycitein, Biochanin A und Formononetin. Als Isoflavone besonders bevorzugt sind Daidzein, Genistein, Glycitein und Formononetin. In den erfindungsgemäß bevorzugten Isoflavon-Glycosiden sind die Isoflavone über min¬ destens eine Hydroxygruppe mit mindestens einem Zucker glycosidisch verknüpft. Als Zucker kommen Mono- oder Oligosaccharide, insbesondere D-Glucose, D-Galactose, D- Glucuronsäure, D-Galacturonsäure, D-Xylose, D-Apiose, L-Rhamnose, L-Arabinose und Rutinose in Betracht. Erfindungsgemäß besonders bevorzugte Isoflavon-Glycoside sind Daidzin und Genistin.For the purposes of the present invention, isoflavones are to be understood as meaning substances which are hydrogenation, oxidation or substitution products of 3-phenyl-4H-1-benzopyran, hydrogenation of which may be in the 2,3-position of the carbon skeleton, oxidation under Formation of a carbonyl group in the 4-position may be present, and by substitution of the replacement of one or more hydrogen atoms by hydroxy or methoxy groups to understand. The isoflavones preferred according to the invention include, for example, daidzein, genistein, prunetin, biochanin, orobol, santal, pratense, irigenin, glycitein, biochanin A and formononetin. Particularly preferred isoflavones are daidzein, genistein, glycitein and formononetin. In the isoflavone glycosides which are preferred according to the invention, the isoflavones are glycosidically linked to at least one sugar via at least one hydroxy group. Suitable sugars are mono- or oligosaccharides, in particular D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and rutinose. Particularly preferred isoflavone glycosides according to the invention are daidzin and genistin.
Erfindungsgemäß weiterhin bevorzugt ist es, wenn die Isoflavone und/oder deren Glyco- side als Bestandteile eines aus einer Pflanze gewonnenen Substanzgemisches, insbe¬ sondere eines pflanzlichen Extraktes, in den Zubereitungen enthalten sind. Solche pflanzlichen Substanzgemische können in dem Fachmann geläufiger Weise beispiels¬ weise durch Auspressen oder Extrahieren aus Pflanzen wie Soja, insbesondere aus den Sojakeimen, Rotklee oder Kichererbsen gewonnen werden. Besonders bevorzugt wer¬ den in den erfindungsgemäßen Zubereitungen Isoflavone oder Isoflavon-Glycoside in Form von aus Soja gewonnenen Extrakten eingesetzt, wie sie beispielsweise unter der Produktbezeichnung Soy Protein lsolate SPI (Protein Technology International, St. Louis) oder Soy Phytochemicals Concentrate SPC (Archer Daniels Midland, Decatur) im Handel erhältlich sind. Ein weiterer besonders bevorzugter Isoflavonoid-reicher Pflanzen¬ extrakt ist Apfelkernextrakt, insbesondere das Handelsprodukt Ederline von Seporga. Ederline enthält Phytohormone, Isoflavonoide, Phytosterole, Triterpenoide, Tocopherole und natürliche Wachse.It is furthermore preferred according to the invention if the isoflavones and / or their glycosides are contained in the preparations as constituents of a substance mixture obtained from a plant, in particular a vegetable extract. Such vegetable substance mixtures can be obtained, for example, by pressing or extracting from plants such as soy, in particular from the soybean seeds, red clover or chickpeas, in a manner familiar to the person skilled in the art. Particular preference is given to using isoflavones or isoflavone glycosides in the form of soya-derived extracts in the preparations according to the invention, as described, for example, under the product name Soy Protein Isolate SPI (Protein Technology International, St. Louis) or Soy Phytochemicals Concentrate SPC (Archer Daniels Midland, Decatur) are commercially available. Another particularly preferred isoflavonoid-rich plant extract is apple seed extract, in particular the commercial product Ederline from Seporga. Ederline contains phytohormones, isoflavonoids, phytosterols, triterpenoids, tocopherols and natural waxes.
Besonders bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekenn¬ zeichnet, dass mindestens ein Isoflavonoid und/oder mindestens ein Isoflavonoid-reicher Pflanzenextrakt in einer Gesamtmenge von 0,00001 bis 1 Gew.-%, bevorzugt 0,0005 bis 0,5 Gew.-% und besonders bevorzugt 0,001 bis 0,1 Gew.-%, jeweils bezogen auf die Isoflavonoidaktivsubstanz in der gesamten Zusammensetzung, enthalten ist.Particularly preferred compositions according to the invention are characterized in that at least one isoflavonoid and / or at least one isoflavonoid richer Plant extract in a total amount of 0.00001 to 1 wt .-%, preferably 0.0005 to 0.5 wt .-% and particularly preferably 0.001 to 0.1 wt .-%, each based on the Isoflavonoidaktivsubstanz in the total composition, is included.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zu¬ sammensetzungen zusätzlich mindestens ein Polyphenol oder einen Polyphenol-reichen Pflanzenextrakt.In a further preferred embodiment, the compositions according to the invention additionally comprise at least one polyphenol or a polyphenol-rich plant extract.
Unter Polyphenolen sind erfindungsgemäß aromatische Verbindungen zu verstehen, die mindestens zwei phenolische Hydroxy-Gruppen im Molekül enthalten. Hierzu zählen die drei Dihydroxybenzole Brenzcatechin, Resorcin und Hydrochinon, weiterhin Phloroglu- cin, Pyrogallol und Hexahydroxybenzol. In der Natur treten freie und veretherte Polyphe- nole beispielsweise in Blütenfarbstoffen (Anthocyanidine, Flavone), in Gerbstoffen (Catechine, Tannine), als Flechten- oder Farn-Inhaltsstoffe (Usninsäure, Acylpolyphe- nole), in Ligninen und als Gallussäure-Derivate auf. Bevorzugte Polyphenole sind Fla¬ vone, Catechine, Usninsäure, und als Tannine die Derivate der Gallussäure, Digallus¬ säure und Digalloylgallussäure. Besonders bevorzugte Polyphenole sind die monomeren Catechine, das heißt die Derivate der Flavan-3-ole, und Leukoanthocyanidine, das heißt die Derivate der Leukoanthocyanidine, die bevorzugt in öJ^'^'^'-Stellung phenolische Hydroxygruppen tragen, bevorzugt Epicatechin und Epigallocatechin, sowie die daraus durch Selbstkondensation entstehenden Gerbstoffe. Solche Gerbstoffe werden bevor¬ zugt nicht in isolierter Reinsubstanz, sondern als Extrakte gerbstoffreicher Pflanzenteile eingesetzt, z. B. Extrakte von Catechu, Quebracho, Eichenrinde und Pinienrinde sowie anderen Baumrinden, Blättern von Grünem Tee (camellia sinensis) und Mate. Ebenfalls besonders bevorzugt sind die Tannine.According to the invention, polyphenols are aromatic compounds which contain at least two phenolic hydroxyl groups in the molecule. These include the three dihydroxybenzenes catechol, resorcinol and hydroquinone, as well as phloroglucin, pyrogallol and hexahydroxybenzene. In nature, free and etherified polyphenols occur, for example, in floral dyes (anthocyanidins, flavones), in tannins (catechins, tannins), as lichen or fern ingredients (usnic acid, acyl polyphenols), in lignins and as gallic acid derivatives , Preferred polyphenols are flavones, catechols, usnic acid, and tannins are the derivatives of gallic acid, digallic acid and digalloylgallic acid. Particularly preferred polyphenols are the monomeric catechins, that is, the derivatives of flavan-3-ols, and leucoanthocyanidins, that is, the derivatives of leucoanthocyanidins which preferably carry phenolic hydroxyl groups in the ω, ω '' position, preferably epicatechin and epigallocatechin, and the resulting by self-condensation tannins. Such tannins are preferably not used in isolated pure substance but as extracts of tannin-rich plant parts, eg. Extracts of catechu, quebracho, oak bark and pine bark, as well as other tree bark, leaves of green tea (camellia sinensis) and mate. Also particularly preferred are the tannins.
Ein besonders bevorzugter Polyphenol-reicher kosmetischer Wirkstoff ist das Handels¬ produkt Sepivinol R, ein Extrakt aus Rotwein, erhältlich von der Firma Seppic. Ein weite¬ rer besonders bevorzugter Polyphenol-reicher kosmetischer Wirkstoff ist das Handels¬ produkt Crodarom Chardonnay, ein Extrakt aus den Kernen der Chardonnay-Traube, erhältlich von der Firma Croda.A particularly preferred polyphenol-rich cosmetic active ingredient is the commercial product Sepivinol R, an extract of red wine, available from Seppic. Another particularly preferred polyphenol-rich cosmetic active ingredient is the commercial product Crodarom Chardonnay, an extract from the kernels of the Chardonnay grape, obtainable from Croda.
Besonders bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekenn¬ zeichnet, dass mindestens ein Polyphenol und/oder mindestens ein Polyphenol-reicher Pflanzenextrakt in einer Gesamtmenge von 0,001 bis 10 Gew.-%, bevorzugt 0,005 bis 5 Gew.-% und besonders bevorzugt 0,01 bis 3 Gew.-%, jeweils bezogen auf die Polyphe- nolaktivsubstanz in der gesamten Zusammensetzung, enthalten ist. In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen mindestens ein Ubichinon oder ein Ubichinol oder deren Derivate. Ubichinole sind die reduzierte Form der Ubichinone. Die erfindungsgemäß bevorzugten Ubichinone weisen die Formel (II) auf:Particularly preferred compositions according to the invention are characterized in that at least one polyphenol and / or at least one polyphenol-rich plant extract are present in a total amount of 0.001 to 10% by weight, preferably 0.005 to 5% by weight and more preferably 0.01 to 3 wt .-%, in each case based on the Polyphe- nolaktivsubstanz in the entire composition. In a further preferred embodiment, the compositions according to the invention comprise at least one ubiquinone or a ubiquinol or derivatives thereof. Ubiquinols are the reduced form of ubiquinones. The preferred ubiquinones according to the invention have the formula (II):
Figure imgf000024_0001
Figure imgf000024_0001
(H)(H)
mit n = 6, 7, 8, 9 oder 10.with n = 6, 7, 8, 9 or 10.
Besonders bevorzugt ist das Ubichinon der Formel (II) mit n = 10, auch bekannt als Coenzym Q10.Particularly preferred is the ubiquinone of formula (II) with n = 10, also known as coenzyme Q10.
Besonders bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekenn¬ zeichnet, dass mindestens ein Ubichinon und/oder mindestens ein Ubichinol und/oder mindestens ein Derivat dieser Substanzen in einer Gesamtmenge von 0,0001 bis 1 Gew.-%, bevorzugt 0,001 bis 0,5 Gew.-% und besonders bevorzugt 0,005 bis 0,1 Gew.- %, jeweils bezogen auf die gesamte Zusammensetzung, enthalten ist.Particularly preferred compositions according to the invention are characterized in that at least one ubiquinone and / or at least one ubiquinol and / or at least one derivative of these substances in a total amount of 0.0001 to 1 wt .-%, preferably 0.001 to 0.5 wt. % and more preferably 0.005 to 0.1% by weight, in each case based on the total composition.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen mindestens ein natürlich vorkommendes Xanthin-Derivat, insbe¬ sondere ein natürlich vorkommendes Di- oder Trialkylxanthin, bevorzugt ausgewählt aus Coffein, Theophyllin, Theobromin und Aminophyllin.In a further preferred embodiment, the compositions according to the invention contain at least one naturally occurring xanthine derivative, in particular a naturally occurring di- or trialkylxanthine, preferably selected from caffeine, theophylline, theobromine and aminophylline.
Bevorzugte erfindungsgemäßeZusammensetzungen sind dadurch gekennzeichnet, dass sie mindestens ein natürlich vorkommendes Xanthin-Derivat in einer Gesamtmenge von 0,0001 bis 1 Gew.-%, bevorzugt 0,001 bis 0,5 Gew.-% und besonders bevorzugt 0,005 bis 0,1 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, enthalten.Preferred compositions according to the invention are characterized in that they contain at least one naturally occurring xanthine derivative in a total amount of 0.0001 to 1% by weight, preferably 0.001 to 0.5% by weight and more preferably 0.005 to 0.1% by weight. %, in each case based on the total composition.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen Ectoin. Ectoin ist der Trivialname für 2-Methyl-1 ,4,5,6-tetrahydro- pyrimidin-4-carboxylat. Besonders bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass Ectoin in Mengen von 0,0001 bis 1 Gew.-%, bevor¬ zugt 0,001 bis 0,5 Gew.-% und besonders bevorzugt 0,005 bis 0,01 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, enthalten ist.In a further preferred embodiment, the compositions according to the invention contain ectoine. Ectoin is the common name for 2-methyl-1, 4,5,6-tetrahydro- pyrimidin-4-carboxylate. Particularly preferred compositions according to the invention are characterized in that ectoine is used in amounts of from 0.0001 to 1% by weight, preferably from 0.001 to 0.5% by weight and particularly preferably from 0.005 to 0.01% by weight, in each case on the entire composition, is included.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen mindestens eine anorganische und/oder mindestens eine organi¬ sche UV-Filtersubstanz.In a further preferred embodiment, the compositions according to the invention contain at least one inorganic and / or at least one organic UV filter substance.
Bei den UV-Filtersubstanzen handelt es sich um bei Raumtemperatur flüssig oder kristal¬ lin vorliegende Substanzen, die in der Lage sind, ultraviolette Strahlen zu absorbieren und die aufgenommene Energie in Form längerwelliger Strahlung, z. B. Wärme wieder abzugeben. Man unterscheidet UVA-Filter und UVB-Filter. Die UVA- und UVB-Filter können sowohl einzeln als auch in Mischungen eingesetzt werden. Der Einsatz von Filter-mischungen ist erfindungsgemäß bevorzugt.The UV filter substances are liquids which are liquid or crystalline at room temperature and are capable of absorbing ultraviolet rays and of absorbing the absorbed energy in the form of longer-wave radiation, eg. B. to give off heat again. One differentiates between UVA filters and UVB filters. The UVA and UVB filters can be used individually or in mixtures. The use of filter mixtures is preferred according to the invention.
Die erfindungsgemäß verwendeten organischen UV-Filter sind ausgewählt aus den Deri¬ vaten von Dibenzoylmethan, Zimtsäureestern, Diphenylacrylsäureestern, Benzophenon, Campher, p-Aminobenzoesäureestern, o-Aminobenzoesäureestern, Salicylsäureestern, Benzimidazolen, symmetrisch oder unsymmetrisch substituierten 1 ,3,5-Triazinen, mono¬ meren und oligomeren 4,4-Diarylbutadiencarbonsäureestern und -carbonsäureamiden, Ketotricyclo(5.2.1.0)decan, Benzalmalonsäureestern, Benzoxazol sowie beliebigen Mischungen der genannten Komponenten. Die organischen UV-Filter können öllöslich oder wasserlöslich sein. Die Benzoxazol-Derivate liegen vorteilhaft in gelöster Form in den erfindungsgemäßen kosmetischen Zubereitungen vor. Es kann ggf. aber auch von Vorteil sein, wenn die Benzoxazol-Derivate in pigmentärer, d. h. ungelöster Form - bei¬ spielsweise in Partikelgrößen von 10 nm bis zu 300 nm - vorliegen. Erfindungsgemäß besonders bevorzugte öllösliche UV-Filter sind 1-(4-tert.-Butylphenyl)-3-(4'-methoxyphe- nyl)propan-1 ,3-dion (Parsol® 1789), 1-Phenyl-3-(4'-isopropylphenyl)-propan-1 ,3-dion, 3- (4*-Methylbenzyliden)-D,L-campher, 4-(Dimethylamino)-benzoesäure-2-ethylhexylester, 4-(Dimethylamino)benzoesäure-2-octylester, 4-(Dimethylamino)-benzoesäureamylester, 4-Methoxyzimtsäure-2-ethylhexylester, 4-Methoxyzimtsäurepropylester, 4-Methoxyzimt- säureisopentylester, 2-Cyano-3,3-phenylzimtsäure-2-ethylhexylester (Octocrylene), SaIi- cylsäure-2-ethylhexylester, Salicylsäure-4-isopropylbenzylester, Salicylsäurehomo- menthylester (3,3,5-Trimethyl-cyclohexylsalicylat), 2-Hydroxy-4-methoxybenzophenon, 2-Hydroxy-4-methoxy-4'-methylbenzophenon, 2,2'-Dihydroxy-4-methoxybenzophenon, 2-(4'-Diethylamino-2'-hydroxybenzoyl)-benzoesäurehexylester (auch: Aminobenzophe- non, unter der Bezeichnung Uvinul A Plus bei der Firma BASF erhältlich), 4-Methoxy- benzmalonsäuredi-2-ethylhexylester, an Polymere gebundene UV-Filter, z. B. das 3-(4- (2,2-Bis-Ethoxycarbonylvinyl)-phenoxy)propenyl)-methoxysiloxan/Dimethylsiloxan-Copo- lymer mit der INCI-Bezeichnung Dimethicodiethylbenzal malonate (CAS-Nr. 207574-74- 1 , Parsol® SLX), Triazinderivate, wie z. B. 2,4-Bis-{[4-(2-Ethyl-hexyloxy)-2-hydroxy]-phe- nyl}-6-(4-methoxyphenyl)-1 ,3,5-triazin (INCI: Bis-Ethylhexyloxyphenol Methoxyphenyl Triazin, unter dem Namen Tinosorb S bei CIBA erhältlich), Dioctylbutylamidotriazon (INCI: Diethylhexyl Butamido Triazone, unter dem Namen Uvasorb® HEB bei Sigma 3V erhältlich), 2,4,6-Trianilino-(p-carbo-2'-ethyl-1'-hexyloxy)-1 ,3,5-triazin (Ethylhexyl Tria¬ zone, Uvinul® T 150), 2-[4,6-Bis(2,4-dimethylphenyl)-1 ,3,5-triazin-2-yl]-5-(octyloxy)phenol (CAS Nr.: 2725-22-6), 2,4-bis-[5-1 (di-methylpropyl)benzoxazol-2-yl-(4-phenyl)-imino]-6- (2-ethylhexyl)-imino-1 ,3,5-triazin (CAS Nr. 288254-16-0, Uvasorb® K2A von 3V Sigma), die Benzotriazolderivate 2,2'-Methylen-bis-(6-(2H-benzotriazol-2-yl)-4-(1 ,1 ,3,3-tetra- methylbutyl)-phenol) [Tinosorb M (Ciba)], 2,2'-Methyl-bis-[6(2H-benzotriazol-2-yl)-4- (methyl)phenol] (MIXXIM BB/200 der Firma Fairmount Chemical), 2-(2'-Hydroxy-3',5'-di-t- amylphenyl)benzotriazol (CAS- Nr.: 025973-551), 2-(2'- Hydroxy-5'-octylphenyl)-ben- zotriazol (CAS-Nr. 003147-75-9), 2-(2'-Hydroxy-5'-methylphenyl)benzotriazol (CAS-Nr. 2440-22-4), 2-(2H-benzotriazol-2-yl)-4-methyl-6-[2-methyl-3-[1 ,3,3,3-tetramethyl-1 -((tri- methylsilyl)oxy]disiloxanyl)propyl]-phenol (CAS-Nr.: 155633-54-8) mit der INCI-Bezeich¬ nung Drometrizole Trisiloxane, 2,4-Bis-{[4-(2-ethyl-hexyloxy)-2-hydroxy]-phenyl}-6-(4- methoxyphenyl)-1 ,3,5-triazin (INCI: Bis-Ethylhexyloxyphenol Methoxyphenyl Triazin oder auch Aniso Triazin, erhältlich als Tinosorb® S von CIBA), 2,4-Bis-{[4-(3-sulfonato)-2- hydroxy-propyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1 ,3,5-triazin-Natriumsalz, 2,4-Bis-{[4-(3-(2-propyloxy)-2-hydroxy-propyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphe- nyl)-1 ,3,5-triazin, 2,4-Bis-{[4-(2-ethyl-hexyloxy)-2-hydroxy]-phenyl}-6-[4-(2-methoxyethyl- carboxyl)-phenylamino]-1 ,3,5-triazin, 2,4-Bis-{[4-(3-(2- propyloxy)-2-hydroxy-propyloxy)- 2-hydroxy]-phenyl}-6-[4-(ethylcarboxyl)-phenylamino]-1 ,3,5-triazin, 2,4-Bis-{[4-(2-ethyl- hexyloxy)-2-hydroxy]-phenyl}-6-(1-methyl-pyrrol-2-yl)-1 ,3,5-triazin, 2,4-Bis- {[4- tris(trimethylsiloxy-silylpropyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1 ,3,5-triazin, 2,4-Bis-{[4-(2-methylpropenyloxy)-2-hydroxy]-phenyl}-6-(4-methoxyphenyl)-1 ,3,5-triazin, 2,4-Bis-{[4-(1',1l,1',3I,5',5l,5I-Heptamethylsiloxy-2-methyl-propyloxy)-2-hydroxy]-phenyl}- 6-(4-methoxyphenyl)-1 ,3,5-triazin sowie Mischungen der genannten Komponenten.The organic UV filters used according to the invention are selected from the derivatives of dibenzoylmethane, cinnamic acid esters, diphenylacrylic acid esters, benzophenone, camphor, p-aminobenzoic acid esters, o-aminobenzoic acid esters, salicylic acid esters, benzimidazoles, symmetrically or asymmetrically substituted 1,3,5-triazines, mono ¬ mers and oligomeric 4,4-Diarylbutadiencarbonsäureestern and -carbonsäureamiden, Ketotricyclo (5.2.1.0) decane, Benzalmalonsäureestern, benzoxazole and any mixtures of the above components. The organic UV filters can be oil-soluble or water-soluble. The benzoxazole derivatives are advantageously present in dissolved form in the cosmetic preparations according to the invention. However, it may also be advantageous if the benzoxazole derivatives are present in a pigmentary, ie undissolved form, for example in particle sizes of 10 nm to 300 nm. According to the invention particularly preferred oil-soluble UV filters are 1- (4-tert-butylphenyl) -3- (4'-methoxyphe- nyl) propane-1, 3-dione (Parsol ® 1789), 1-phenyl-3- (4 '-isopropylphenyl) propane-1, 3-dione, 3- (4 * methylbenzylidene) -D, L-camphor, 4- (dimethylamino) benzoic acid 2-ethylhexyl ester, 4- (dimethylamino) benzoic acid 2-octyl ester Ethyl 4- (dimethylamino) benzoate, 2-ethylhexyl 4-methoxycinnamate, propyl 4-methoxycinnamate, isopentyl 4-methoxycinnamate, 2-ethylhexyl 2-cyano-3,3-phenylcinnamate (octocrylene), salicylic acid-2 ethylhexyl ester, salicylic acid 4-isopropylbenzyl ester, salicylic acid homo-ethyl ester (3,3,5-trimethylcyclohexylsalicylate), 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy 4-methoxybenzophenone, 2- (4'-diethylamino-2'-hydroxybenzoyl) -benzoic acid hexyl ester (also: aminobenzophenone) non, available under the name Uvinul A Plus from BASF), 4-methoxy-benzmalonsäuredi-2-ethylhexylester, bound to polymers UV filters, eg. B. 3- (4- (2,2-bis-ethoxycarbonylvinyl) phenoxy) propenyl) -methoxysiloxan / dimethylsiloxane Copo- lymer with the INCI name Dimethicodiethylbenzal malonate (CAS no. 207574-74- 1, Parsol ® SLX), triazine derivatives, such as. B. 2,4-bis - {[4- (2-ethyl-hexyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1, 3,5-triazine (INCI: Bis- Ethylhexyloxyphenol methoxyphenyl triazine, available) under the name Tinosorb S from CIBA, dioctylbutylamidotriazone (INCI: Diethylhexyl Butamido Triazone, available) under the name Uvasorb HEB from Sigma 3V ®, 2,4,6-trianilino- (p-carbo-2'- ethyl-1'-hexyloxy) -1, 3,5-triazine (ethylhexyl Tria¬ zone, Uvinul ® T 150), 2- [4,6-bis (2,4-dimethylphenyl) -1, 3,5-triazine -2-yl] -5- (octyloxy) phenol (CAS No .: 2725-22-6), 2,4-bis [5-1 (di-methylpropyl) benzoxazol-2-yl (4-phenyl) imino] -6- (2-ethylhexyl) imino-1, 3,5-triazine (CAS no. 288254-16-0, Uvasorb K2A ® from 3V Sigma), the benzotriazole derivatives of 2,2'-methylene-bis- (6- (2H-benzotriazol-2-yl) -4- (1,1,3,3-tetramethylbutyl) -phenol) [Tinosorb M (Ciba)], 2,2'-methyl-bis- [6 (2H-benzotriazol-2-yl) -4- (methyl) phenol] (MIXXIM BB / 200 from Fairmount Chemical), 2- (2'-hydroxy-3 ', 5'-di-t-amylphenyl) benzotriazole ( CAS No .: 025973-551), 2- (2'-hydroxy-5'-o ctylphenyl) benzotriazole (CAS no. 003147-75-9), 2- (2'-hydroxy-5'-methylphenyl) benzotriazole (CAS No. 2440-22-4), 2- (2H-benzotriazol-2-yl) -4-methyl-6 - [2-methyl-3- [1,3,3,3-tetramethyl-1 - ((trimethylsilyl) oxy] disiloxanyl) propyl] phenol (CAS No .: 155633-54-8) with the INCI DESCRIPTION Drometrizole Trisiloxanes, 2,4-bis - {[4- (2-ethyl-hexyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1, 3,5-triazine (INCI : bis-Ethylhexyloxyphenol methoxyphenyl triazine or Aniso triazine, available as Tinosorb S from CIBA ®), 2,4-bis - {[4- (3-sulfonato) -2-hydroxy-propyloxy) -2-hydroxy] phenyl} -6- (4-methoxyphenyl) -1, 3,5-triazine sodium salt, 2,4-bis - {[4- (3- (2-propyloxy) -2-hydroxy-propyloxy) -2-hydroxy] - phenyl} -6- (4-methoxyphenyl) -1,3,5-triazine, 2,4-bis - {[4- (2-ethyl-hexyloxy) -2-hydroxy] -phenyl} -6- [ 4- (2-methoxyethylcarboxyl) -phenylamino] -1, 3,5-triazine, 2,4-bis - {[4- (3- (2-propyloxy) -2-hydroxy-propyloxy) -2-hydroxy ] -phenyl} -6- [4- (ethylcarboxyl) -phenylamino] -1, 3,5-triazine, 2,4-bis - {[4- (2-ethyl-hexyloxy) -2-hydroxy] -phenyl} -6- (1-methyl- pyrrol-2-yl) -1, 3,5-triazine, 2,4-bis {[4-tris (trimethylsiloxy-silylpropyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1, 3,5-triazine, 2,4-bis - {[4- (2-methylpropenyloxy) -2-hydroxy] -phenyl} -6- (4-methoxyphenyl) -1, 3,5-triazine, 2,4- Bis - {[4- (1 ', 1 L , 1', 3 I , 5 ', 5 L , 5 I -Heptamethylsiloxy-2-methyl-propyloxy) -2-hydroxy] -phenyl} - 6- (4- methoxyphenyl) -1, 3,5-triazine and mixtures of the said components.
Bevorzugte wasserlösliche UV-Filter sind 2-Phenylbenzimidazol-5-sulfonsäure, Pheny- len-1 ,4-bis-(2-benzimidazyl)-3,3'-5,5'-tetrasulfonsäure und deren Alkali-, Erdalkali-, Ammonium-, Alkylammonium-, Alkanolammonium- und Glucammoniumsalze, insbeson¬ dere die Sulfonsäure selbst mit der INCI Bezeichnung Phenylbenzimidazole Sulfonic Acid (CAS.-Nr. 27503-81-7), die beispielsweise unter dem Handelsnamen Eusolex 232 bei Merck oder unter Neo Heliopan Hydro bei Symrise erhältlich ist, und das Phenylen- 1 ^-bis^-benzimidazyO-S.S'-δ.δ'-tetrasulfonsäure-bis-natriumsalz mit der INCI-Bezeich- nung Disodium Phenyl Dibenzimidazol Tetrasulfonate (CAS-Nr.: 180898-37-7), das bei¬ spielsweise unter dem Handelsnamen Neo Heliopan AP bei Symrise erhältlich ist, SuI- fonsäurederivate von Benzophenonen, vorzugsweise 2-Hydroxy-4-methoxybenzophe- non-5-sulfonsäure und ihre Salze, Sulfonsäurederivate des 3-Benzylidencamphers, wie z. B. 4-(2-Oxo-3-bornylidenmethyl)benzolsulfonsäure und 2-Methyl-5-(2-oxo-3-bornyli- den)sulfonsäure und deren Salze mit der INCI-Bezeichnung Terephthalydene Dicampher Sulfonic Acid (CAS.-Nr.: 90457-82-2, als Mexoryl SX von der Firma Chimex erhältlich).Preferred water-soluble UV filters are 2-phenylbenzimidazole-5-sulfonic acid, phenylene-1, 4-bis (2-benzimidazyl) -3,3'-5,5'-tetrasulfonic acid and its alkali metal, alkaline earth metal, Ammonium, alkylammonium, alkanolammonium and glucammonium salts, in particular the sulfonic acid itself with the INCI name phenylbenzimidazole sulfonic acid (CAS No. 27503-81-7), for example under the trade name Eusolex 232 at Merck or under Neo Heliopan Hydro is available from Symrise, and the phenylene-1 ^ -bis ^ -benzimidazyO-S.S'-δ.δ'-tetrasulfonic acid bis-sodium salt with the INCI name Disodium Phenyl Dibenzimidazole Tetrasulfonate (CAS No .: 180898-37-7), which is available, for example, under the trade name Neo Heliopan AP from Symrise, sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts, sulfonic acid derivatives of Benzylidencamphers, such as. B. 4- (2-oxo-3-bomylidenemethyl) benzenesulfonic acid and 2-methyl-5- (2-oxo-3-bornyliden) sulfonic acid and its salts with the INCI name Terephthalydene Dicampher Sulfonic Acid (CAS.No. .: 90457-82-2, available as Mexoryl SX from Chimex).
Einige der öllöslichen UV-Filter können selbst als Lösungsmittel oder Lösungsvermittler für andere UV-Filter dienen. So lassen sich beispielsweise Lösungen des UV-A-Filters 1-(4-tert.-Butylphenyl)-3-(4'methoxyphenyl)propan-1 ,3-dion (z. B. Parsol® 1789) in ver¬ schiedenen UV-B-Filtern herstellen. Die erfindungsgemäßen Zusammensetzungen ent¬ halten daher in einer weiteren bevorzugten Ausführungsform 1-(4-tert.-Butylphenyl)-3- (4'-methoxyphenyl)propan-1 ,3-dion in Kombination mit mindestens einem UV-B-Filter, ausgewählt aus 4-Methoxyzimtsäure-2-ethylhexylester, 2-Cyano-3,3-phenylzimtsäure-2- ethylhexylester, Salicylsäure-2-ethylhexylester und 3,3,5-Trimethyl-cyclohexylsalicylat. In diesen Kombinationen liegt das Gewichtsverhältnis von UV-B-Filter zu 1-(4-tert.-Butyl- phenyl)-3-(4'methoxyphenyl)propan-1 ,3-dion zwischen 1 :1 und 10:1 , bevorzugt zwischen 2:1 und 8:1, das molare Verhältnis liegt entsprechend zwischen 0,3 und 3,8, bevorzugt zwischen 0,7 und 3,0.Some of the oil-soluble UV filters can themselves serve as solvents or solubilizers for other UV filters. Thus, solutions of the UV-A filter 1- (4-tert-butylphenyl) -3- (4'methoxyphenyl) propane-1, 3-dione (z. B. Parsol ® 1789) can for example be different in ver¬ UV Make -B filters. Therefore, in a further preferred embodiment, the compositions according to the invention contain 1- (4-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1,3-dione in combination with at least one UV-B filter of 4-methoxycinnamic acid 2-ethylhexyl ester, 2-cyano-3,3-phenylcinnamic acid 2-ethylhexyl ester, 2-ethylhexyl salicylate and 3,3,5-trimethylcyclohexylsalicylate. In these combinations, the weight ratio of UV-B filter to 1- (4-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1,3-dione is between 1: 1 and 10: 1, preferably between 2: 1 and 8: 1, the molar ratio being between 0.3 and 3.8, preferably between 0.7 and 3.0.
Bei den erfindungsgemäß bevorzugten anorganischen Lichtschutzpigmenten handelt es sich um feindisperse oder kolloiddisperse Metalloxide und Metallsalze, beispielsweise Titandioxid, Zinkoxid, Eisenoxid, Aluminiumoxid, Ceroxid, Zirkoniumoxid, Silicate (Talk) und Bariumsulfat. Die Partikel sollten dabei einen mittleren Durchmesser von weniger als 100 nm, vorzugsweise zwischen 5 und 50 nm und insbesondere zwischen 15 und 30 nm aufweisen, so genannte Nanopigmente. Sie können eine sphärische Form aufweisen, es können jedoch auch solche Partikel zum Einsatz kommen, die eine ellipsoide oder in sonstiger Weise von der sphärischen Gestalt abweichende Form besitzen. Die Pigmente können auch oberflächenbehandelt, d.h. hydrophilisiert oder hydrophobiert vorliegen. Typische Beispiele sind gecoatete Titandioxide, wie z. B. Titandioxid T 805 (Degussa) oder Eusolex® T2000 (Merck). Als hydrophobe Coatingmittel kommen dabei vor allem Silicone und dabei speziell Trialkoxyoctylsilane oder Simethicone in Frage. Besonders bevorzugt sind Titandioxid und Zinkoxid.The inventively preferred inorganic photoprotective pigments are finely dispersed or colloidally disperse metal oxides and metal salts, for example titanium dioxide, zinc oxide, iron oxide, aluminum oxide, cerium oxide, zirconium oxide, silicates (talc) and barium sulfate. The particles should have an average diameter of less than 100 nm, preferably between 5 and 50 nm and in particular between 15 and 30 nm, so-called nanopigments. They may have a spherical shape, but it is also possible to use those particles which have an ellipsoidal or otherwise deviating shape from the spherical shape. The pigments can also be surface-treated, ie hydrophilized or hydrophobized. Typical examples are coated titanium dioxides, such as. Example, titanium dioxide T 805 (Degussa) or Eusolex ® T2000 (Merck). Suitable hydrophobic coating agents are in particular silicones and in particular trialkoxyoctylsilanes or simethicones. Particularly preferred are titanium dioxide and zinc oxide.
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass sie mindestens eine organische UV-Filtersubstanz in einer Gesamtmenge von 0,1 - 30 Gew.-%, bevorzugt 0,5 - 20 Gew.-%, besonders bevorzugt 1 ,0 - 1O Gew.-% und außerordentlich bevorzugt 2 oder 3 - 7 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, enthalten.Preferred compositions according to the invention are characterized in that they contain at least one organic UV filter substance in a total amount of 0.1-30% by weight, preferably 0.5-20% by weight, more preferably 1.0-0.0% by weight. % and most preferably 2 or 3 - 7 wt .-%, each based on the total composition.
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass sie mindestens eine anorganische UV-Filtersubstanz in einer Gesamtmenge von 0,1 - 15 Gew.-%, bevorzugt 0,5 - 10 Gew.-%, besonders bevorzugt 1 - 5 Gew.-% und außerordentlich bevorzugt 2 - 4 Gew.-%, jeweils bezogen auf die gesamte Zusammen¬ setzung, enthalten.Preferred compositions according to the invention are characterized in that they comprise at least one inorganic UV filter substance in a total amount of 0.1-15% by weight, preferably 0.5-10% by weight, more preferably 1-5% by weight and extraordinarily preferably 2 to 4% by weight, based in each case on the total composition.
In einer weiteren bevorzugten Ausführungsform enthalten die erfind ungsgemäßen Zusammensetzungen mindestens einen selbstbräunenden Wirkstoff. Erfindungsgemäß bevorzugte selbstbräunende Wirkstoffe sind ausgewählt aus Dihydroxyaceton und Erythrulose. Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekenn¬ zeichnet, dass sie mindestens einen selbstbräunenden Wirkstoff in einer Gesamtmenge von 0,1 - 15 Gew.-%, bevorzugt 0,5 - 10 Gew.-%, besonders bevorzugt 1 ,0 - 5 Gew.-% und außerordentlich bevorzugt 2,0 - 4,0 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, enthalten.In a further preferred embodiment, the compositions according to the invention contain at least one self-tanning active ingredient. Self-tanning active ingredients preferred according to the invention are selected from dihydroxyacetone and erythrulose. Preferred compositions according to the invention are characterized in that they contain at least one self-tanning active ingredient in a total amount of 0.1-15% by weight, preferably 0.5-10% by weight, more preferably 1.0-0.5% by weight. % and most preferably 2.0 to 4.0 wt .-%, each based on the total composition.
In einer weiteren bevorzugten Ausführungsform enthalten die erfindungsgemäßen Zusammensetzungen mindestens einen hautaufhellenden Wirkstoff. Erfindungsgemäß bevorzugte hautaufhellende Wirkstoffe sind ausgewählt aus Ascorbinsäure, den Estern der Ascorbinsäure mit Phosphorsäure und/oder organischen C2-C2o-Carbonsäuren sowie deren Alkali- und Erdalkalimetallsalzen, Kojisäure, Hydrochinon, Arbutin, Maulbeerbaum¬ extrakt und Süßholzextrakt sowie Mischungen hiervon. Sowohl als Einzelsubstanz wie auch in Mischung bevorzugt sind die Ascorbinsäurederivate sowie Kojisäure bevorzugt. Besonders bevorzugt sind Natriumascorbylphosphat, Magnesiumascorbylphosphat, Ascorbylmonopalmitat, Ascorbyldipalmitat, Ascorbylmonostearat, Ascorbyldistearat, Ascorbylmonoethylhexanoat, Ascorbyldiethylhexanoat, Ascorbylmonooctanoat, Ascorbyl- dioctanoat, Ascorbylmonoisostearat und Ascorbyldiisostearat. Die erfindungsgemäß außerordentlich bevorzugten Ascorbinsäurederivate sind Natriumascorbylphosphat und Magnesiumascorbylphosphat.In a further preferred embodiment, the compositions according to the invention comprise at least one skin-lightening active ingredient. According to the invention preferred skin lightening agents are selected from ascorbic acid, the esters of ascorbic acid with phosphoric acid and / or organic C 2 -C 2 o-carboxylic acids and their alkali and alkaline earth metal salts, kojic acid, hydroquinone, arbutin, Maulbeerbaum¬ thereof extract and licorice extract and mixtures thereof. Both as a single substance and as a mixture, the ascorbic acid derivatives and kojic acid are preferred. Particularly preferred are sodium ascorbyl phosphate, magnesium ascorbyl phosphate, ascorbyl monopalmitate, ascorbyl dipalmitate, ascorbyl monostearate, ascorbyl distearate, ascorbyl monoethyl hexanoate, ascorbyl diethylhexanoate, ascorbyl monooctanoate, ascorbyl dioctanoate, ascorbyl monoisostearate and ascorbyl diisostearate. The invention exceptionally preferred ascorbic acid derivatives are sodium ascorbyl phosphate and magnesium ascorbyl phosphate.
Bevorzugte erfindungsgemäße Zusammensetzungen sind dadurch gekennzeichnet, dass sie mindestens einen hautaufhellenden Wirkstoff in einer Gesamtmenge von 0,05 bis 5 Gew.-%, bevorzugt von 0,1 - 2 Gew-%, jeweils bezogen auf die gesamte Zusam¬ mensetzung, enthalten.Preferred compositions according to the invention are characterized in that they contain at least one skin-lightening active ingredient in a total amount of from 0.05 to 5% by weight, preferably from 0.1 to 2% by weight, in each case based on the total composition.
Ein weiterer Gegenstand der vorliegenden Erfindung ist die Verwendung einer kosmeti¬ schen und/oder dermatologischen topischen Zusammensetzung, die in einem geeigne¬ ten Träger mindestens einen Wirkstoff, der die Prostaglandin-Synthese und/oder die Leukotrien-Synthese inhibiert und mindestens einen Wirkstoff, der die kutane Synthese von Neuromediatoren stimuliert, enthält, zur nicht-therapeutischen, kosmetischen Behandlung von empfindlicher Haut, trockener Haut, atopischer Dermatitis, Altershaut, UV-geschädigter Haut und/oder gereizter Haut.A further subject matter of the present invention is the use of a cosmetic and / or dermatological topical composition which, in a suitable carrier, comprises at least one active ingredient which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active ingredient which which stimulates cutaneous synthesis of neuromediators, for the non-therapeutic, cosmetic treatment of sensitive skin, dry skin, atopic dermatitis, aging skin, UV-damaged skin and / or irritated skin.
Ein weiterer Gegenstand der vorliegenden Erfindung ist die Verwendung einer kosmeti¬ schen und/oder dermatologischen topischen Zusammensetzung, die in einem geeigne¬ ten Träger mindestens einen Wirkstoff, der die Prostaglandin-Synthese und/oder die Leukotrien-Synthese inhibiert und mindestens einen Wirkstoff, der die kutane Synthese von Neuromediatoren stimuliert, enthält, zur Herstellung eines Mittels zur thera¬ peutischen Behandlung von empfindlicher Haut, trockener Haut, atopischer Dermatitis, Altershaut, UV-geschädigter Haut und/oder gereizter Haut.A further subject matter of the present invention is the use of a cosmetic and / or dermatological topical composition which, in a suitable carrier, comprises at least one active ingredient which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active ingredient which which stimulates the cutaneous synthesis of neuromediators, for the preparation of an agent for the therapeutic treatment of sensitive skin, dry skin, atopic dermatitis, aging skin, UV-damaged skin and / or irritated skin.
Ein weiterer Gegenstand der vorliegenden Erfindung ist ein Verfahren zur nicht-thera¬ peutischen kosmetischen Hautbehandlung, bei dem eine kosmetische oder dermatologi¬ sche topische Zusammensetzung, die in einem geeigneten Träger mindestens einen Wirkstoff, der die Prostaglandin-Synthese und/oder die Leukotrien-Synthese inhibiert und mindestens einen Wirkstoff, der die kutane Synthese von Neuromediatoren stimuliert, enthält, auf die Haut, insbesondere die Gesichtshaut, aufgetragen wird.A further subject matter of the present invention is a process for the non-therapeutic cosmetic skin treatment, in which a cosmetic or dermatological topical composition comprising at least one active ingredient in a suitable carrier, the prostaglandin synthesis and / or the leukotriene synthesis inhibited and at least one drug that stimulates the cutaneous synthesis of neuromediators, is applied to the skin, especially the facial skin.
Als optionale Komponenten enthalten die erfindungsgemäßen Zusammensetzungen neben mindestens einem Wirkstoff, der die Prostaglandin-Synthese und/oder die Leuko¬ trien-Synthese inhibiert und mindestens einem Wirkstoff, der die kutane Synthese von Neuromediatoren stimuliert, weiterhin mindestens einen konditionierenden Wirkstoff. Unter konditionierenden Wirkstoffen sind erfindungsgemäß solche Substanzen zu ver¬ stehen, die auf keratinische Materialien, insbesondere auf die Haut, aufziehen und die physikalischen und sensorischen Eigenschaften verbessern. Konditionierungsmittel glätten die oberste Schicht der Haut und machen sie weich und geschmeidig. Erfindungsgemäß bevorzugte konditionierende Wirkstoffe sind ausgewählt aus Fettstof¬ fen, insbesondere pflanzlichen Ölen, wie Sonnenblumenöl, Olivenöl, Sojaöl, Rapsöl, Mandelöl, Jojobaöl, Orangenöl, Weizenkeimöl, Pfirsichkernöl und den flüssigen Anteilen des Kokosöls, Lanolin und seinen Derivaten, flüssigen Paraffinölen, Isoparaffinölen und synthetischen Kohlenwasserstoffen, Di-n-alkylethem mit insgesamt 12 bis 36 C-Atomen, z. B. Di-n-octylether und n-Hexyl-n-octylether, Fettsäuren, besonders linearen und/oder verzweigten, gesättigten und/oder ungesättigten C8-3o-Fettsäuren, Fettalkoholen, beson¬ ders gesättigten, ein- oder mehrfach ungesättigten, verzweigten oder unverzweigten Fettalkoholen mit 4 - 30 Kohlenstoffatomen, die mit 1 - 75, bevorzugt 5 - 20 Ethylenoxid- Einheiten ethoxyliert und/oder mit 3 - 30, bevorzugt 9 - 14 Propylenoxid-Einheiten prop- oxyliert sein können, Esterölen, das heißt Estern von C6-30-Fettsäuren mit C2-3o-Fettalko- holen, Hydroxycarbonsäurealkylestem, Dicarbonsäureestem wie Di-n-butyladipat sowie Diolestern wie Ethylenglykoldioleat oder Propylenglykoldi(2-ethylhexanoat), symmetri¬ schen, unsymmetrischen oder cyclischen Estern der Kohlensäure mit Fettalkoholen, z. B. Glycerincarbonat oder Dicaprylylcarbonat (Cetiol® CC), Mono,- Di- und Trifettsäure- estern von gesättigten und/oder ungesättigten linearen und/oder verzweigten Fettsäuren mit Glycerin, die mit 1 - 10, bevorzugt 7 - 9 Ethylenoxid-Einheiten ethoxyliert sein kön¬ nen, z. B. PEG-7 Glyceryl Cocoate, Wachsen, insbesondere Insektenwachsen, Pflan¬ zenwachsen, Fruchtwachsen, Ozokerit, Mikrowachsen, Ceresin, Paraffinwachsen, Triglyceriden gesättigter und gegebenenfalls hydroxylierter C-|6-3o-Fettsäuren, z. B. gehärteten Triglyceridfetten, Phospholipiden, beispielsweise Sojalecithin, Ei-Lecithin und Kephalinen, Siliconverbindungen, ausgewählt aus Decamethylcyclopentasiloxan, Dodecamethylcyclohexasiloxan und Siliconpolymeren, die gewünschtenfalls querver¬ netzt sein können, z. B. Polydialkylsiloxanen, Polyalkylarylsiloxanen, ethoxylierten und/oder propoxylierten Polydialkylsiloxanen mit der früheren INCI-Bezeichnung Dime- thicone Copolyol, sowie Polydialkylsiloxanen, die Amin- und/oder Hydroxy-Gruppen ent¬ halten, bevorzugt Substanzen mit den INCI-Bezeichnungen Dimethiconol, Amodimethi- cone oder Trimethylsilylamodimethicone.As optional components, the compositions according to the invention contain, in addition to at least one active ingredient which inhibits prostaglandin synthesis and / or leukotriene synthesis and at least one active substance which stimulates the cutaneous synthesis of neuromediators, furthermore at least one conditioning agent. According to the invention, the term "conditioning active ingredients" is understood to mean those substances which are applied to keratinic materials, in particular to the skin, and which improve physical and sensory properties. Conditioners smooth the top layer of the skin and make it soft and supple. Conditioning agents which are preferred according to the invention are selected from fatty substances, in particular vegetable oils, such as sunflower oil, olive oil, soybean oil, rapeseed oil, almond oil, jojoba oil, orange oil, wheat germ oil, peach kernel oil and the liquid portions of coconut oil, lanolin and its derivatives, liquid paraffin oils, isoparaffin oils and synthetic hydrocarbons, di-n-alkyl ethers having a total of 12 to 36 carbon atoms, z. B. di-n-octyl ether and n-hexyl n-octyl ether, fatty acids, especially linear and / or branched, saturated and / or unsaturated C 8-3 o fatty acids, fatty alcohols, especially saturated, mono- or polyunsaturated , branched or unbranched fatty alcohols having 4 to 30 carbon atoms, which may be ethoxylated with 1 to 75, preferably 5 to 20 ethylene oxide units and / or propoxylated with 3 to 30, preferably 9 to 14 propylene oxide units, ester oils, ie esters of C 6 - 30 fatty acids with C 2-3 pick o-fatty alcohol, Hydroxycarbonsäurealkylestem, dicarboxylic acid esters of di-n-butyl adipate and diol esters such as Ethylenglykoldioleat or propylene glycol di (2-ethylhexanoate), symmetri¬ rule, asymmetrical or cyclic esters of carbonic acid with fatty alcohols, eg. As glycerol carbonate or dicaprylyl (Cetiol ® CC), mono, - di- and Trifettsäure- esters of saturated and / or unsaturated linear and / or branched fatty acids with glycerol, which are ethoxylated with 1-10, preferably 7-9 ethylene oxide units kön¬ nen, z. B. PEG-7 glyceryl cocoate, waxes, especially insect waxes, Pflan¬ zenwachsen, fruit waxes, ozokerite, microwaxes, ceresin, paraffin waxes, triglycerides of saturated and optionally hydroxylated C | 6 - 3 o-fatty acids, eg. As hardened triglyceride fats, phospholipids, for example, soybean lecithin, egg lecithin and cephalins, silicone compounds selected from decamethylcyclopentasiloxane, Dodecamethylcyclohexasiloxan and silicone polymers, which can be cross-linked if desired, z. B. Polydialkylsiloxanen, Polyalkylarylsiloxanen, ethoxylated and / or propoxylated polydialkylsiloxanes with the earlier INCI name Dime- thicone Copolyol, and polydialkylsiloxanes containing amine and / or hydroxyl groups ent, preferably substances with the INCI names Dimethiconol, Amodimethi- cone or trimethylsilylamodimethicone.
Die Einsatzmenge der Fettstoffe beträgt bevorzugt 0,1 - 50 Gew.%, besonders bevor¬ zugt 0,1 - 20 Gew.% und außerordentlich bevorzugt 0,1 - 15 Gew.%, jeweils bezogen auf die gesamte Zusammensetzung. Vorteilhafterweise liegen die erfindungsgemäßen kosmetischen oder dermatologischen Zusammensetzungen in Form einer flüssigen, fließfähigen oder festen Öl-in-Wasser- Emulsion, Wasser-in-ÖI-Emulsion, Mehrfach-Emulsion, insbesondere einer Öl-in-Was- ser-in-ÖI- oder Wasser-in-ÖI-in-Wasser-Emulsion, Makroemulsion, Miniemulsion, Mikro- emulsion, PIT-Emulsion, Nanoemulsion, Pickering-Emulsion, Hydrodispersion, eines Hydrogels, eines Lipogels, einer ein- oder mehrphasigen Lösung, eines Schaumes, eines Puders oder einer Mischung mit mindestens einem als medizinischen Klebstoff geeigneten Polymer vor. Die Mittel können auch in wasserfreier Form, wie beispiels¬ weise einem Öl oder einem Balsam, dargereicht werden. Hierbei kann der Träger ein pflanzliches oder tierisches Öl, ein Mineralöl, ein synthetisches Öl oder eine Mischung solcher Öle sein.The amount of fatty substances used is preferably 0.1-50% by weight, more preferably 0.1-20% by weight, and most preferably 0.1-15% by weight, based in each case on the entire composition. Advantageously, the cosmetic or dermatological compositions according to the invention are in the form of a liquid, flowable or solid oil-in-water emulsion, water-in-oil emulsion, multiple emulsion, in particular an oil-in-water-in-oil. or water-in-oil-in-water emulsion, macroemulsion, miniemulsion, microemulsion, PIT emulsion, nanoemulsion, Pickering emulsion, hydrodispersion, a hydrogel, a lipogel, a mono- or multiphase solution, a foam, a Powder or a mixture with at least one suitable as a medical adhesive polymer. The agents may also be presented in anhydrous form, such as, for example, an oil or a balm. Here, the carrier may be a vegetable or animal oil, a mineral oil, a synthetic oil or a mixture of such oils.
In einer besonderen Ausführungsform der Erfindung liegen die Zusammensetzungen als Mikroemulsion vor. Unter Mikroemulsionen werden im Rahmen der Erfindung neben den thermodynamisch stabilen Mikroemulsionen auch die sogenannten "PIT"-Emulsionen verstanden. Bei diesen Emulsionen handelt es sich um Systeme mit den 3 Komponenten Wasser, Öl und Emulgator, die bei Raumtemperatur als ÖI-in-Wasser-Emulsion vorlie¬ gen. Beim Erwärmen dieser Systeme bilden sich in einem bestimmten Temperaturbe¬ reich (als Phaseninversiontemperatur oder "PIT" bezeichnet) Mikroemulsionen aus, die sich bei weiterer Erwärmung in Wasser-in-ÖI-Emulsionen umwandeln. Beim anschließenden Abkühlen werden wieder O/W-Emulsionen gebildet, die aber auch bei Raumtemperatur als Mikroemulsionen oder als sehr feinteilige Emulsionen mit einem mittleren Teilchendurchmesser unter 400 nm und insbesondere von etwa 100-300 nm, vorliegen. Erfindungsgemäß können solche Mikro- oder "PIT"-Emulsionen bevorzugt sein, die einen mittleren Teilchendurchmesser von etwa 200 nm aufweisen. In der Ausführungsform als Emulsion enthalten die erfindungsgemäßen Zusammenset¬ zungen mindestens eine oberflächenaktive Substanz als Emulgator oder Dispergiermit¬ tel. Geeignete Emulgatoren sind beispielsweise Anlagerungsprodukte von 4 bis 30 Mol Ethylenoxid und/oder 0 bis 5 Mol Propylenoxid an lineare C8-C22-Fettalkohole, an C12- C22-Fettsäuren und an C8-C15-Alkylphenole, C12-C22-Fettsäuremono- und -diester von Anlagerungsprodukten von 1 bis 30 Mol Ethylenoxid an C3-C6-Polyole, insbesondere an Glycerin, Ethylenoxid- und Polyglycerin-Anlagerungsprodukte an Methylglucosid-Fett- säureester, Fettsäurealkanolamide und Fettsäureglucamide, C8-C22-Alkylmono- und - oligoglycoside und deren ethoxylierte Analoga, wobei Oligomerisierungsgrade von 1 ,1 bis 5, insbesondere 1 ,2 bis 2,0, und Glucose als Zuckerkomponente bevorzugt sind, Gemische aus Alkyl-(oligo)-glucosiden und Fettalkoholen, z. B. das im Handel erhältliche Produkt Montanov® 68, Anlagerungsprodukte von 5 bis 60 Mol Ethylenoxid an Rizinusöl und gehärtetes Rizinusöl, Partialester von Polyolen mit 3-6 Kohlenstoffatomen mit gesät¬ tigten C8-C22-Fettsäuren, Sterole (Sterine), insbesondere Cholesterol, Lanosterol, Beta- Sitosterol, Stigmasterol, Campesterol und Ergosterol sowie Mykosterole, Phospholipide, vor allem Glucose-Phospolipide, Fettsäureester von Zuckern und Zuckeralkoholen wie Sorbit, Polyglycerine und Polyglycerinderivate, bevorzugt Polyglyceryl-2-dipolyhydroxy- stearat (Handelsprodukt Dehymuls® PGPH) und Polyglyceryl-3-diisostearat (Handels¬ produkt Lameform® TGI) sowie lineare und verzweigte C8-C30-Fettsäuren und deren Na-, K-, Ammonium-, Ca-, Mg- und Zn - Salze.In a particular embodiment of the invention, the compositions are present as a microemulsion. In the context of the invention, microemulsions are understood as meaning not only the thermodynamically stable microemulsions but also the so-called "PIT" emulsions. These emulsions are systems with the 3 components water, oil and emulsifier which are present at room temperature as an oil-in-water emulsion. Upon heating of these systems, they form in a specific temperature range (as phase inversion temperature or " PIT ") denotes microemulsions which, on further heating, convert to water-in-oil emulsions. During the subsequent cooling, O / W emulsions are again formed, but they are also present at room temperature as microemulsions or as very finely divided emulsions having an average particle diameter of less than 400 nm and in particular of about 100-300 nm. According to the invention, those micro- or "PIT" emulsions may be preferred which have an average particle diameter of about 200 nm. In the embodiment as emulsion, the compositions according to the invention contain at least one surface-active substance as emulsifier or dispersant. Suitable emulsifiers are for example adducts of from 4 to 30 mol ethylene oxide and / or 0 to 5 mol propylene oxide onto linear C 8 -C 22 fatty alcohols, on C 12 - C 22 fatty acids and C 8 -C 15 alkylphenols, C 12 - C 22 -fatty acid mono- and diesters of addition products of 1 to 30 moles of ethylene oxide onto C 3 -C 6 -polyols, in particular to glycerol, ethylene oxide and polyglycerol addition products of methylglucoside fatty acid esters, fatty acid alkanolamides and fatty acid glucamides, C 8 -C 22 alkyl mono- and - oligoglycosides and their ethoxylated analogues, wherein degrees of oligomerization of 1, 1 to 5, in particular 1, 2 to 2.0, and glucose are preferred as the sugar component, mixtures of alkyl (oligo) -glucosiden and fatty alcohols, eg , B. the commercially available Product Montanov ® 68, addition products of 5 to 60 moles of ethylene oxide with castor oil and hydrogenated castor oil, partial esters of polyols having 3-6 carbon atoms with saturated C 8 -C 22 fatty acids, sterols (sterols), in particular cholesterol, lanosterol, beta Sitosterol, stigmasterol, campesterol and ergosterol and mycosterols, phospholipids, especially glucose phospholipids, fatty acid esters of sugars and sugar alcohols such as sorbitol, polyglycerols and polyglycerol derivatives, preferably polyglyceryl-2-dipolyhydroxy stearate (commercial product Dehymuls ® PGPH) and polyglyceryl-3-diisostearat (Handels¬ product Lameform ® TGI) as well as linear and branched C 8 -C 30 fatty acids and their Na, K, ammonium, Ca, Mg and Zn - salts.
Die erfindungsgemäßen Mittel enthalten die Emulgatoren bevorzugt in Mengen von 0,1 bis 25 Gew.-%, insbesondere 0,5 - 15 Gew.-%, bezogen auf das gesamte Mittel. In einer besonders bevorzugten Ausführungsform ist mindestens ein nichtionischer Emulgator mit einem HLB-Wert von 8 und darunter enthalten. Derart geeignete Emulga¬ toren sind beispielsweise Verbindungen der allgemeinen Formel R1 - O - R2, in der R1 eine primäre lineare Alkyl-, Alkenyl- oder Acylgruppe mit 20 - 30 C-Atomen und R2 Was¬ serstoff, eine Gruppe mit der Formel -(CnH2nO)x-H mit x = 1 oder 2 und n = 2 - 4 oder eine Polyhydroxyalkylgruppe mit 4 - 6 C-Atomen und 2 - 5 Hydroxylgruppen ist. Beson¬ ders bevorzugt sind Behenylalkohol und Arachidylalkohol, die bevorzugt lamellare Öl-in¬ Wasser-Emulsionen bilden. Weitere bevorzugt geeignete Emulgatoren mit einem HLB- Wert von 8 und darunter sind die Anlagerungsprodukte von 1 oder 2 Mol Ethylenoxid oder Propylenoxid an Behenylalkohol, Erucylalkohol, Arachidylalkohol oder auch an Behensäure oder Erucasäure. Bevorzugt eignen sich auch die Monoester von C16-C30- Fettsäuren mit Polyolen wie z. B. Pentaerythrit, Trimethylolpropan, Diglycerin, Sorbit, Glucose oder Methylglucose. Beispiele für solche Produkte sind z. B. Sorbitanmono- behenat oder Pentaerythrit-monoerucat.The agents according to the invention preferably contain the emulsifiers in amounts of 0.1 to 25% by weight, in particular 0.5 to 15% by weight, based on the total agent. In a particularly preferred embodiment, at least one nonionic emulsifier having an HLB value of 8 and below is included. Such suitable emulsifiers are, for example, compounds of the general formula R 1 -O-R 2 , in which R 1 is a primary linear alkyl, alkenyl or acyl group having 20-30 C atoms and R 2 is hydrogen, a group having of the formula - (C n H 2n O) x -H where x = 1 or 2 and n = 2 - 4 or a polyhydroxyalkyl group having 4-6 C atoms and 2-5 hydroxyl groups. Behenyl alcohol and arachidyl alcohol, which preferably form lamellar oil-in-water emulsions, are particularly preferred. Further preferred emulsifiers with an HLB value of 8 and below are the adducts of 1 or 2 moles of ethylene oxide or propylene oxide with behenyl alcohol, erucyl alcohol, arachidyl alcohol or behenic acid or erucic acid. Preferably, the monoesters of C 16 -C 30 fatty acids with polyols such as. As pentaerythritol, trimethylolpropane, diglycerol, sorbitol, glucose or methyl glucose. Examples of such products are z. Sorbitan mono- behenate or pentaerythritol monoerucate.
Weitere geeignete Zusatzstoffe sind Verdickungsmittel, z. B. natürliche und synthetische Tone und Schichtsilikate wie Bentonit, Hectorit, Montmorillonit oder Laponite®, oder anionische Polymere aus Acrylsäure, Methacrylsäure, Crotonsäure, Maleinsäure¬ anhydrid und 2-Acrylamido-2-methylpropansulfonsäure, wobei die sauren Gruppen ganz oder teilweise als Natrium-, Kalium-, Ammonium-, Mono- oder Triethanolammonium-Salz vorliegen können und wobei mindestens ein nichtionisches Monomer enthalten sein kann. Bevorzugte nichtionogene Monomere sind Acrylamid, Methacrylamid, Acrylsäure- ester, Methacrylsäureester, Vinylpyrrolidon, Vinylether und Vinylester. Bevorzugte anio¬ nische Copolymere sind Acrylsäure-Acrylamid-Copolymere sowie insbesondere PoIy- acrylamidcopolymere mit Sulfonsäuregruppen-haltigen Monomeren. Diese Copolymere können auch vernetzt vorliegen. Geeignete Handelsprodukte sind Sepigel®305, Simul- gel®600, Simulgel® NS und Simulgel® EG der Firma SEPPIC. Weitere besonders bevor¬ zugte anionische Homo- und Copolymere sind unvernetzte und vernetzte Polyacrylsäu- ren. Solche Verbindungen sind zum Beispiel die Handelsprodukte Carbopol®. Ein beson¬ ders bevorzugtes anionisches Copolymer enthält als Monomer zu 80 - 98 % eine unge¬ sättigte, gewünschtenfalls substituierte C3-6-Carbonsäure oder ihr Anhydrid sowie zu 2 - 20 % gewünschtenfalls substituierte Acrylsäureester von gesättigten C10-3o-Carbon- säuren, wobei das Copolymer mit den vorgenannten Vernetzungsagentien vernetzt sein kann. Entsprechende Handelsprodukte sind Pemulen® und die Carbopol®-Typen 954, 980, 1342 und ETD 2020 (ex B.F. Goodrich).Other suitable additives are thickeners, for. B. natural and synthetic clays and phyllosilicates such as bentonite, hectorite, montmorillonite or Laponite ® , or anionic polymers of acrylic acid, methacrylic acid, crotonic acid, maleic anhydride and 2-acrylamido-2-methylpropanesulfonic acid, wherein the acidic groups wholly or partly as sodium , Potassium, ammonium, mono- or triethanolammonium salt, and wherein at least one nonionic monomer may be contained. Preferred nonionic monomers are acrylamide, methacrylamide, acrylates, methacrylates, vinylpyrrolidone, vinyl ethers and vinyl esters. Preferred anionic copolymers are acrylic acid-acrylamide copolymers and in particular polyacrylamide copolymers with monomers containing sulfonic acid groups. These copolymers can also be networked. Suitable commercial products are Sepigel ® 305 Simulgel® ® 600, Simulgel® ® NS and Simulgel® ® EC SEPPIC. More particularly bevor¬ ferred anionic homo- and copolymers are uncrosslinked and crosslinked polyacrylic ren. Such compounds are for example the commercial products Carbopol ®. A particularly preferred anionic copolymer contains 80 to 98% of an unsaturated, optionally substituted C 3-6 -carboxylic acid or its anhydride as well as 2 to 20%, if desired, substituted acrylic acid esters of saturated C 10 -3 o-carboxylic acid. acids, wherein the copolymer may be crosslinked with the aforementioned crosslinking agents. Corresponding commercial products are Pemulen ® and Carbopol ® grades 954, 980, 1342 and ETD 2020 (ex BF Goodrich).
Geeignete nichtionische Polymere sind beispielsweise Polyvinylalkohole, die teilverseift sein können, z. B. die Handelsprodukte Mowiol® sowie VinylpyrrolidonΛ/inylester-Copoly- mere und Polyvinylpyrrolidone, die z. B. unter dem Warenzeichen Luviskol® (BASF) ver¬ trieben werden.Suitable nonionic polymers include polyvinyl alcohols, which may be partially saponified, for. As the commercial products Mowiol ® and VinylpyrrolidonΛ / inylester copolymers and polyvinylpyrrolidones, the z. B. under the trademark Luviskol ® (BASF) ver¬ be driven.
Weitere geeignete Zusatzstoffe sind Antioxidantien, Konservierungsmittel, Lösungsmittel wie Ethanol, Isopropanol, Ethylenglykol, Propylenglykol, Propylenglykolmonoethylether, Glycerin und Diethylenglykol, Adsorbentien und Füllstoffe, wie Talkum und Veegum®, Parfümöle, Pigmente sowie Farbstoffe zum Anfärben des Mittels, Substanzen zur Ein¬ stellung des pH-Wertes, Komplexbildner wie EDTA, NTA, ß-Alanindiessigsäure und Phosphonsäuren, Treibmittel wie Propan-Butan-Gemische, Pentan, Isopentan, Isobutan, N2O, Dimethylether, CO2 und Luft.Other suitable additives are antioxidants, preservatives, solvents such as ethanol, isopropanol, ethylene glycol, propylene glycol, propylene glycol, glycerol and diethylene glycol, adsorbents and fillers such as talc and Veegum ®, perfume oils, pigments and dyes for coloring the composition, substances position suitability for adjusting the pH, complexing agents such as EDTA, NTA, β-alaninediacetic acid and phosphonic acids, propellants such as propane-butane mixtures, pentane, isopentane, isobutane, N 2 O, dimethyl ether, CO 2 and air.
Experimenteller TeilExperimental part
Die Bestimmung der Inhibierung der Prostaglandinsynthese, der Leukotrien-Synthese, der Cyclooxygenase und der 5-Lipoxygenase erfolgte nach üblichen, dem Fachmann be¬ kannten Standardmethoden.The determination of the inhibition of prostaglandin synthesis, leukotriene synthesis, cyclooxygenase and 5-lipoxygenase was carried out by standard methods known to those skilled in the art.
Zur Bestimmung der kutanen Synthese von Neuromediatoren wurden in-vitro-Messun- gen der Stimulierung der ß-Endorphinausschüttung von Keratinozyten herangezogen. Dazu wurden Keratinozytenkulturen jeweils mit einer wässrigen Lösung von 1 Gew.-% beziehungsweise 5 Gew.-% des zu untersuchenden Rohstoffes teile quelle für 24 Stun¬ den versetzt. Der produzierte ß-Endorphingehalt wurde mit Hilfe von einem Enzym Immunoassay Kit (ß-Endorphin Human, EIA Kit der Firma Phoenix Pharmaceuticals) im Kulturmedium bestimmt. Überprüfung der inhibitorischen Wirkung der 5-Lipoxyqenase-lnhibitoren (in vitro) Das Enzym 5-Lipoxygenase katalysiert die Umsetzung von Arachidonsäure zu den Leu¬ kotrienen LTB4, LTC4, LTD4 und LTE4. Leukotriene sind Mediatoren in entzündlichen und allergischen Reaktionen von Granulozyten, Mastzellen, Monozyten und Macrophagen. Auch in den Keratinozyten der Haut werden bei entzündlichen Reaktionen Leukotriene gebildet. Inhibitoren der Leukotrien-Synthese können demnach eine entzündungshem¬ mende bzw. hautberuhigende Wirkung haben.In order to determine the cutaneous synthesis of neuromediators, in vitro measurements of the stimulation of the β-endorphin release of keratinocytes were used. For this purpose, keratinocyte cultures were each mixed with an aqueous solution of 1% by weight or 5% by weight of the raw material source to be investigated for 24 hours. The produced β-endorphin content was determined with the aid of an enzyme immunoassay kit (β-endorphin human, EIA kit from Phoenix Pharmaceuticals) in the culture medium. Examination of the inhibitory effect of the 5-lipoxygenase inhibitors (in vitro) The enzyme 5-lipoxygenase catalyses the conversion of arachidonic acid into the leucotrienes LTB 4 , LTC 4 , LTD 4 and LTE 4 . Leukotrienes are mediators in inflammatory and allergic reactions of granulocytes, mast cells, monocytes and macrophages. Also in the keratinocytes of the skin leukotrienes are formed in inflammatory reactions. Accordingly, inhibitors of leukotriene synthesis can have an antiinflammatory or skin-calming effect.
Bereitstellung der 5-LipoxygenaseProvision of 5-lipoxygenase
Die 5-üpoxigenase wurde aus menschlichen Leukämie-Zelllinien durch Zugabe von Di- methylsulfoxid (DMSO), TGF-ß1 (transforming growth factor ß1 ) und Dihydroxyvitamin D3 differenziert und dabei zugleich die 5-Lipoxygenase induziert. Nach 4 Tagen im Diffe¬ renzierungsmedium wurden die Zellen geerntet, in einem Glucose-haltigen PBS-Puffer aufgenommen und durch Ultraschallbehandlung aufgeschlossen. Größere Zellbestand¬ teile wurden bei 100 000 g abzentrifugiert, wobei 5-Lipoxigenase im Überstand verblieb.The 5-lipoxygenase was differentiated from human leukemia cell lines by addition of dimethylsulfoxide (DMSO), TGF-β1 (transforming growth factor β1) and dihydroxyvitamin D3 and simultaneously induced 5-lipoxygenase. After 4 days in the differentiation medium, the cells were harvested, taken up in a glucose-containing PBS buffer and disrupted by sonication. Larger Zellbestand¬ parts were centrifuged off at 100 000 g, with 5-lipoxigenase remaining in the supernatant.
Messung der 5-üpoxygenase-lnhibierunqMeasurement of 5-Oxygenase Inhibition
Die Bestimmung der 5-üpoxygenase-lnhibitionswirkung erfolgte gemäß Werz et al., Naunyn-Schmiedeberg's Arch. Pharmacol., 1997, Vol. 456, 441 - 445. Dem Überstand aus der 5-Lipoxygenase-Herstellung wurden Adenosintriphosphat (ATP) und die zu testenden Rohstoffe zugesetzt. Im vorliegenden Falle wurden 100 μg Roh¬ stoff, so wie er ist, pro Milliliter Überstand eingesetzt. Als Lösemittel wurden je nach Substanz Wasser, Ethanol, DMSO oder Chloroform verwendet.The determination of the 5-üpoxygenase inhibitory activity was carried out according to Werz et al., Naunyn-Schmiedeberg's Arch. Pharmacol., 1997, Vol. 456, 441-445. The supernatant from the 5-lipoxygenase production were adenosine triphosphate (ATP) and the added to testing raw materials. In the present case, 100 μg of raw material was used as it is per milliliter of supernatant. The solvents used were, depending on the substance, water, ethanol, DMSO or chloroform.
Die Ansätze wurden für 30 Sekunden bei 37° C vorinkubiert. Anschließend wurde die 5-Lipoxygenase-Reaktion durch Zusatz von Arachidonsäure gestartet. Nach 10 Minuten Reaktionszeit wurde die Reaktion durch Zugabe von Methanol gestoppt. Die durch die Einwirkung der 5-Lipoxygenase auf Arachidonsäure produzierten Leukotriene wurden mittels HPLC quantifiziert.The batches were preincubated for 30 seconds at 37 ° C. Subsequently, the 5-lipoxygenase reaction was started by addition of arachidonic acid. After 10 minutes reaction time, the reaction was stopped by addition of methanol. The leukotrienes produced by the action of 5-lipoxygenase on arachidonic acid were quantified by HPLC.
Die nachfolgenden Beispiele sollen die Erfindung verdeutlichen, ohne sie hierauf zu be¬ schränken. BeispielrezepturenThe following examples are intended to illustrate the invention, without restricting it to be¬ thereto. example recipes
Alle Angaben sind in Gew.-%, bezogen auf die gesamte Zusammensetzung.All data are in wt .-%, based on the total composition.
1. Oel-in-Wasser-Emulsionen 1. Hautcremes1. Oil-in-water emulsions 1. Skin creams
Figure imgf000035_0001
Figure imgf000035_0001
2. Hautcremes:2. Skin creams:
Figure imgf000035_0002
Figure imgf000035_0002
Figure imgf000036_0001
Figure imgf000036_0001
3. Tagescremes:3rd day creams:
Figure imgf000036_0002
Figure imgf000036_0002
Figure imgf000037_0001
Figure imgf000037_0001
4. Tagescremes mit Lichtschutzfaktor:4. Day Creams with SPF:
Figure imgf000037_0002
Figure imgf000037_0002
Figure imgf000038_0001
Figure imgf000038_0001
Figure imgf000038_0002
Figure imgf000038_0002
Figure imgf000039_0001
Figure imgf000039_0001
5. Tagescremes:5th day creams:
Figure imgf000039_0002
Figure imgf000039_0002
Figure imgf000040_0001
Figure imgf000040_0001
Hautcremes auf Basis einer Lipoprotein-CremeSkin creams based on a lipoprotein cream
Figure imgf000040_0002
2. Wasser-in-Oel-Emulsion
Figure imgf000040_0002
2. Water-in-oil emulsion
Figure imgf000041_0001
Figure imgf000041_0001
3. Wasser-in-Silicon-Emulsion3. Water-in-silicone emulsion
Figure imgf000041_0002
Figure imgf000041_0002
Figure imgf000042_0001
Figure imgf000042_0001
3. Reinigungszubereitungen3. Cleaning preparations
1. Gesichtswasser-Zubereitungen:1. Tonic preparations:
Figure imgf000042_0002
Figure imgf000042_0002
Figure imgf000043_0001
Figure imgf000043_0001
Beispiele für Zusammensetzungen zum Tränken von TüchernExamples of compositions for soaking wipes
Figure imgf000043_0002
Mit diesen Tränkzusammensetzungen wurden verschiedene Viskose-Vliesstoffe ausge¬ rüstet. Es wurden gelochte, ungelochte, genoppte, einlagige, zweilagige und dreilagige Vliese ausgerüstet. Die Tücher wurden sowohl als feuchte Tücher als auch als trockene Tücher (das heißt, nach dem Ausrüsten wurden die Tücher bis auf einen Restwasser¬ gehalt kleiner 10 Gew.-%, bevorzugt kleiner 5 Gew.-%, getrocknet) verwendet. Beispiel 1 stellt eine Tränkzusammensetzung für ein Lotions- und Make up-Entferner- Tuch dar.
Figure imgf000043_0002
Various viscose nonwovens were equipped with these impregnating compositions. Perforated, unperforated, dimpled, single-ply, two-ply and three-ply nonwovens were finished. The wipes were used both as wet wipes and as dry wipes (that is, after finishing the wipes to a residual water content of less than 10 wt .-%, preferably less than 5 wt .-%, dried) were used. Example 1 illustrates a lotion composition for a lotion and make-up remover cloth.
Beispiel 2 stellt eine Tränkzusammensetzung für ein Selbstbräuner-Tuch dar. Beispiel 3 stellt eine Tränkzusammensetzung für ein Sonnenschutz-Tuch dar. Beispiel 4 stellt eine Tränkzusammensetzung für ein Gesichtsreinigungs-Tuch dar.Example 2 illustrates a soak composition for a self-tanner cloth. Example 3 illustrates a soak composition for a sunscreen cloth. Example 4 illustrates a soak composition for a facial cleansing wipe.
Hautaufhellende Anti Age-MatrixpflasterSkin lightening anti age matrix patch
Figure imgf000044_0001
Figure imgf000044_0001
Hautberuhigende Anti-Age-ReservoirpflasterSkin soothing anti-aging reservoir plasters
Bestandteile des Wirkstoffreservoirs Nr. 1 Nr. 2Components of the drug reservoir no. 1 no. 2
CaomintCaomint
Calmosensine 0,5Calmosensine 0.5
Ederline H 1 ,0 1 ,0Ederline H 1, 0 1, 0
Matrixyl 3000 2,0 2,0Matrixyl 3000 2.0 2.0
Ridulisse C 1 ,0 1 ,0Ridulisse C 1, 0 1, 0
Phytokine 2,0Phytokines 2.0
Carbopof 980 0,5
Figure imgf000045_0001
Carbopof 980 0.5
Figure imgf000045_0001
Liste der verwendeten RohstoffeList of raw materials used
Figure imgf000045_0002
Figure imgf000046_0001
Figure imgf000045_0002
Figure imgf000046_0001
Figure imgf000047_0001
Figure imgf000047_0001

Claims

Patentansprüche claims
1. Kosmetische und/oder dermatologische topische Zusammensetzung, enthaltend in einem geeigneten Träger mindestens einen Wirkstoff, der die Prostaglandinsynthese und/oder die Leukotrien-1. Cosmetic and / or dermatological topical composition comprising, in a suitable carrier, at least one active ingredient which inhibits prostaglandin synthesis and / or leukotriene
Synthese inhibiert und mindestens einen Wirkstoff, der die kutane Synthese von Neuromediatoren stimuliert.Synthesis inhibits and at least one drug that stimulates the cutaneous synthesis of neuromediators.
2. Zusammensetzung gemäß Anspruch 1 , dadurch gekennzeichnet, dass der die Prostaglandin-Synthese inhibierende Wirkstoff ausgewählt ist aus Wirkstoffen, die das Enzym Cyclooxygenase inhibieren.2. The composition according to claim 1, characterized in that the prostaglandin synthesis inhibiting agent is selected from drugs that inhibit the enzyme cyclooxygenase.
3. Zusammensetzung gemäß Anspruch 1 oder 2, dadurch gekennzeichnet, dass der die Prostaglandin-Synthese inhibierende Wirkstoff ausgewählt ist aus Wirkstoffen, die die Ausschüttung von Interleukinen, insbesondere von lnterleukin-1 -alpha, inhibieren.3. Composition according to claim 1 or 2, characterized in that the prostaglandin synthesis-inhibiting active ingredient is selected from active substances which inhibit the secretion of interleukins, in particular of interleukin-1-alpha.
4. Zusammensetzung gemäß Anspruch 1 , dadurch gekennzeichnet, dass der die Leukotrien-Synthese inhibierende Wirkstoff ausgewählt ist aus Wirkstoffen, die das Enzym 5-Lipoxygenase inhibieren.4. The composition according to claim 1, characterized in that the leukotriene synthesis-inhibiting active ingredient is selected from drugs that inhibit the enzyme 5-lipoxygenase.
5. Zusammensetzung gemäß einem der Ansprüche 1 - 4, dadurch gekennzeichnet, dass der die kutane Synthese von Neuromediatoren stimulierende Wirkstoff ausge¬ wählt ist aus Wirkstoffen, die die ß-Endorphinsynthese in Keratinozyten stimulieren.5. The composition according to any one of claims 1-4, characterized in that the cutaneous synthesis of Neuromediatoren stimulating active ingredient is selected from drugs that stimulate the ß-endorphin synthesis in keratinocytes.
6. Zusammensetzung gemäß einem der Ansprüche 1 - 5, dadurch gekennzeichnet, dass der die Prostaglandin-Synthese inhibierende Wirkstoff ausgewählt ist aus6. The composition according to any one of claims 1-5, characterized in that the prostaglandin synthesis inhibiting agent is selected from
Silymarin,silymarin,
- Extrakten aus Centella asiatica,- extracts from Centella asiatica,
- Glycyrrethinsäure,Glycyrrethinic acid,
- Mischungen aus Getreidewachsen, Extrakten aus Schibutter und Argania Spinosa-Öl,- mixtures of grain waxes, extracts of shea butter and Argania spinosa oil,
- Extrakten aus Vanilla Tahitensis, Extrakten aus Olivenblättern, Alginhydrolysaten,- extracts of vanilla tahitensis, extracts of olive leaves, algin hydrolyzates,
- Extrakten aus Bacopa Monniera, Extrakten aus der Rooibos-Pflanze, den physiologisch verträglichen Salzen von Sterolsulfaten, sowie beliebigen Mischungen dieser Wirkstoffe.- extracts from Bacopa Monniera, Extracts from the rooibos plant, the physiologically acceptable salts of sterol sulfates, as well as any mixtures of these active ingredients.
7. Zusammensetzung gemäß einem der Ansprüche 1 - 6, dadurch gekennzeichnet, dass die Konzentration des/der Inhibitors/en der Prostaglandin-Synthese 0,0001 - 10,0 Gew.-%, bevorzugt 0,001 - 2,0 Gew.-%, besonders bevorzugt 0,05 - 1 ,0 Gew.- % und außerordentlich bevorzugt 0,1 - 0,5 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, beträgt.7. A composition according to any one of claims 1-6, characterized in that the concentration of the inhibitor (s) of the prostaglandin synthesis 0.0001 - 10.0 wt .-%, preferably 0.001 - 2.0 wt .-%, more preferably 0.05-1.0% by weight and most preferably 0.1-0.5% by weight, based in each case on the total composition.
8. Zusammensetzung gemäß einem der Ansprüche 1 - 7, dadurch gekennzeichnet, dass der die Leukotrien-Synthese inhibierende Wirkstoff ausgewählt ist aus8. The composition according to any one of claims 1-7, characterized in that the leukotriene synthesis inhibiting agent is selected from
- Alginhydrolysaten,- algin hydrolyzates,
- Aminodicarbonsäuren mit einer C-Kettenlänge von 3 - 6 Kohlenstoffato¬ men sowie deren physiologisch verträglichen Salzen,Aminodicarboxylic acids having a C chain length of 3 to 6 carbon atoms and their physiologically tolerated salts,
- N-alkylierten Ca-Cn-Aminosäuren mit CrC22-Alkylresten sowie deren physiologisch verträglichen Salzen,N-alkylated Ca-Cn-amino acids with C r C 22 -alkyl radicals and their physiologically tolerated salts,
- N-acylierten C2-C1 -i-Aminosäuren mit C2-C22-ACyI resten sowie deren physiologisch verträglichen Salzen,N-acylated C 2 -C 1 -i-amino acids with C 2 -C 22 -alkyl radicals and their physiologically tolerated salts,
- Hefeextrakten,- yeast extracts,
- α-Bisabolol,α-bisabolol,
- α-Liponsäure,- α-lipoic acid,
- sowie beliebigen Mischungen dieser Wirkstoffe.- As well as any mixtures of these agents.
9. Zusammensetzung gemäß einem der Ansprüche 1 - 8, dadurch gekennzeichnet, dass die Konzentration des/der Inhibitors/en der Leukotrien-Synthese 0,0001 - 10,0 Gew.-%, bevorzugt 0,001 - 2,0 Gew.-%, besonders bevorzugt 0,05 - 1 ,0 Gew.-% und außerordentlich bevorzugt 0,1 - 0,5 Gew.-%, jeweils bezogen auf die gesamte Zusammensetzung, beträgt.Composition according to any one of Claims 1-8, characterized in that the concentration of the inhibitor (s) of the leukotriene synthesis is from 0.0001 to 10.0% by weight, preferably from 0.001 to 2.0% by weight, more preferably 0.05-1.0% by weight and most preferably 0.1-0.5% by weight, based in each case on the total composition.
10. Zusammensetzung gemäß einem der Ansprüche 1 - 9, dadurch gekennzeichnet, dass der die kutane Synthese von Neuromediatoren stimulierende Wirkstoff ausge¬ wählt ist aus10. The composition according to any one of claims 1-9, characterized in that the cutaneous synthesis of neuromediators stimulating active ingredient is selected aus¬
Mischungen aus mindestens einem Extrakt aus den Blättern der Mentha piperita und mindestens einem Extrakt aus Kakaobohnen, dem Dipeptidderivat N-Acetyl-Tyr-Arg-hexyldecylester,Mixtures of at least one extract of Mentha piperita leaves and at least one extract of cocoa beans, the dipeptide derivative N-acetyl-Tyr-Arg-hexyldecylester,
Extrakten aus Helichrysum italicum,Extracts of Helichrysum italicum,
Extrakten aus Crithmum Maritimum,Extracts from Crithmum Maritimum,
Extrakten aus Lavandula stoechas,Extracts from Lavandula stoechas,
Extrakten aus Mentha piperita,Extracts from Mentha piperita,
Extrakten aus den Schalen von Kakaobohnen,Extracts from the skins of cocoa beans,
Glutamylamidoethyl Indole,Glutamylamidoethyl indole,
Biosaccharide Gum-2,Biosaccharides Gum-2,
Extrakten aus den Samen von Tephrosia Purpurea,Extracts from the seeds of Tephrosia Purpurea,
Mischungen aus dem Öl von Mentha arvensis-Blättern, Limonenschalen- öl, Zypressenöl, Lavendelöl und Cistus Ladaniferus-Öl,Mixtures of the oil of Mentha arvensis leaves, lime peel oil, cypress oil, lavender oil and Cistus ladaniferus oil,
- Hexasacchariden gemäß FR 2842201- Hexasaccharides according to FR 2842201
- sowie beliebigen Mischungen dieser Wirkstoffe.- As well as any mixtures of these agents.
11. Zusammensetzung gemäß einem der Ansprüche 1 - 10, dadurch gekennzeichnet, dass der/die die kutane Synthese von Neuromediatoren stimulierende/n Wirkstoff/e in Konzentrationen von 0,0001 - 10,0 Gew.-%, bevorzugt 0,001 - 3,0 Gew.-%, beson¬ ders bevorzugt 0,05 - 3,0 Gew.-% und außerordentlich bevorzugt 0,1 - 0,5 - 2,0 Gew.-%, enthalten ist/sind, jeweils bezogen auf die gesamte Zusammensetzung.11. A composition according to any one of claims 1-10, characterized in that / the cutaneous synthesis of neuromediators stimulating / e drug / s in concentrations of 0.0001 - 10.0 wt .-%, preferably 0.001 - 3.0 Wt .-%, particularly preferably 0.05 to 3.0 wt .-% and most preferably 0.1 to 0.5 to 2.0 wt .-%, is / are, in each case based on the total composition ,
12. Kosmetische Zusammensetzung gemäß einem der Ansprüche 1 - 11 , dadurch ge¬ kennzeichnet, dass mindestens ein weiterer kosmetischer Wirkstoff enthalten ist, aus gewählt aus: a) Feuchthaltemitteln, b) Oligomeren und Polymeren von Aminosäuren, N-C2-C24-Acylaminosäuren, den Estern und/oder den physiologisch verträglichen Metallsalzen dieser Substanzen, c) DNA- oder RNA-Oligonucleotiden, d) natürlichen Betainverbindungen, e) Vitaminen, Provitaminen und Vitaminvorstufen der Gruppen A, B, C, E, H und K und den Estern der vorgenannten Substanzen, f) α-Hydroxycarbonsäuren, α-Ketocarbonsäuren, ß-Hydroxycarbonsäuren und deren Ester-, Lacton- oder Salzform, g) Flavonoiden und Flavonoid-reichen Pflanzenextrakten, h) Isoflavonoiden und Isoflavonoid-reichen Pflanzenextrakten, i) Polyphenolen und Polyphenol-reichen Pflanzenextrakten, j) Ubichinon und Ubichinol sowie deren Derivaten, k) natürlich vorkommenden Xanthin-Derivaten, ausgewählt aus Coffein, Theo¬ phyllin, Theobromin und Aminophyllin,12. Cosmetic composition according to any one of claims 1-11, characterized ge indicates that at least one further cosmetic active ingredient is contained, selected from: a) humectants, b) oligomers and polymers of amino acids, NC 2 -C 24 -acylamino acids, the esters and / or the physiologically acceptable metal salts of these substances, c) DNA or RNA oligonucleotides, d) natural betaine compounds, e) vitamins, provitamins and vitamin precursors of groups A, B, C, E, H and K and the esters of the aforementioned substances, f) α-hydroxycarboxylic acids, α-ketocarboxylic acids, β-hydroxycarboxylic acids and their ester, lactone or salt form, g) flavonoids and flavonoid-rich plant extracts, h) isoflavonoids and isoflavonoid-rich plant extracts, i) polyphenols and polyphenol-rich plant extracts, j) ubiquinone and ubiquinol and derivatives thereof, k) naturally occurring xanthine derivatives selected from caffeine, theophylline, theobromine and aminophylline,
I) Ectoin, m) anorganischen und organischen UV-Filtersubstanzen, n) selbstbräunenden Wirkstoffen o) sowie hautaufhellenden Wirkstoffen.I) Ectoin, m) inorganic and organic UV filter substances, n) self-tanning active ingredients o) and skin-lightening active ingredients.
13. Verwendung einer kosmetischen Zusammensetzung gemäß einem der vorhergehen¬ den Ansprüche zur nicht-therapeutischen, kosmetischen Behandlung von13. Use of a cosmetic composition according to one of the vorhergehen¬ claims for non-therapeutic, cosmetic treatment of
- empfindlicher Haut,- sensitive skin,
- trockener Haut,- dry skin,
- atopischer Dermatitis,- atopic dermatitis,
- Altershaut,- aging skin,
- UV-geschädigter Haut,- UV-damaged skin,
- und/oder gereizter Haut.- and / or irritated skin.
14. Verwendung einer kosmetischen Zusammensetzung gemäß einem der Ansprüche 1 - 12 zur Herstellung eines Mittels zur therapeutischen Behandlung von14. Use of a cosmetic composition according to any one of claims 1-12 for the preparation of an agent for the therapeutic treatment of
- empfindlicher Haut,- sensitive skin,
- trockener Haut,- dry skin,
- atopischer Dermatitis,- atopic dermatitis,
- Altershaut,- aging skin,
- UV-geschädigter Haut,- UV-damaged skin,
- und/oder gereizter Haut.- and / or irritated skin.
15. Verfahren zur nicht-therapeutischen kosmetischen Hautbehandlung, dadurch gekennzeichnet, dass eine kosmetische Zusammensetzung gemäß einem der Ansprüche 1 - 12 auf die Haut, insbesondere die Gesichtshaut, aufgetragen wird. 15. A method for non-therapeutic cosmetic skin treatment, characterized in that a cosmetic composition according to any one of claims 1-12 applied to the skin, in particular the facial skin.
PCT/EP2005/010524 2004-10-15 2005-09-29 Compositions with inhibitors of the synthesis of prostaglandin and/or of leukotriene in conjunction with stimulators of the release of cutaneous neuromediators WO2006042625A2 (en)

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FR2894142A1 (en) * 2005-12-05 2007-06-08 Oreal Use of a combination of niacinamide and tyrosine-arginine dipeptide or its derivatives e.g. to prevent and/or decrease cutaneous rednesses and/or swellings
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CN110251411B (en) * 2019-08-09 2022-06-14 北昊干细胞与再生医学研究院有限公司 Transparent aqueous sunscreen spray and preparation method thereof

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