DE102004043945A1 - Oral, dental and dental protease care products containing plaque-forming substances - Google Patents

Abstract

The present invention relates to oral and dental care products containing substances that inhibit bacterial biofilm formation and their use for the prevention and degradation of bacterially induced biofilms.

Description

The The present invention relates to oral and dental care products containing substances which inhibit bacterial biofilm formation and their Use for the prevention and removal of bacteria caused Biofilms.

at The human plaque is a bacterial caused biofilm. Organisms involved in the formation of these biofilms are involved, i.a. S. mutans, S. sobrinus and S. cricetus. biofilms consist of "extracellular polymers Substances ", which is why the biofilm is also called EPS matrix. These polymers include, but are not limited to, Polysaccharides such as e.g. Glucan. These glucans bind particularly well smooth surfaces and promote the aggregation of other microorganisms or of e.g. Food waste. Further protect the polymers inhibit the organisms adhering to the tooth from external influences (e.g. Triclosan), so a complete Inactivation or removal of organisms is difficult. The formation of the biofilm may be a crucial one Factor for the development of caries

The Glucansynthese done by an enzyme, the glucosyltransferase or dextran sucrase (EC 2.4.1.5), which in organisms such. S. mutans and S. sobrinus can be found. A possible approach for fighting of plaque and thus to prevent tooth decay is therefore in the inhibition of glucan synthesis by inhibition of dextran sucrase.

Kozai et al. (1984, Microbios Letters 26, 105-108) examined 74 plant extracts, including extracts of traditional Chinese medicine, on her Efficacy in terms of the inhibition of glucan formation starting of sucrose by inhibiting Streptococcus glucosyltransferase mutans, being both aqueous as well as methanolic extracts were tested. The best inhibition values the methanolic extracts were 85, 82 and 81%, respectively each Armeniacaesamen extract, Astragalus root extract or Ledebouriellaewurzel extract (10 mg / ml in DMSO). The best inhibition values of the aqueous extracts were 72, 72 and 70%, respectively, by Corni Fructus, Ephedrae Herba or Gambir extract (10 mg / ml in water). However, showed none of the tested extracts nearly completely inhibited glucan formation, even at the very high concentration of 10 mg / ml, with the methanolic extracts generally providing better inhibition caused as the watery Extracts. The inhibition of glucan formation was only partial attributed to the inhibition of glucosyltransferase, instead in some make primarily on the antibacterial effect of the extracts.

EP0415126 describes the use of tea polyphenol components to prevent biofilm formation by inhibiting glucosyltransferase.

JP2000297022 describes glucosyltransferase inhibiting polyphenols, wherein a Composition described in addition to xylitol, carrageenan, Propylene glycol and sorbitol also contain a leaf extract from the Japanese Medlar (loquat, Eriobotrya japonica) contains.

JP01186813 describes the use of an aqueous extract of red and brown algae to inhibit glucosyltransferase activity.

JP56-81892 describes the use of finely ground leaves of black tea in a toothpaste.

JP63-009366 describes the use of aqueous Extracts of red and brown algae and of tangen (Laminaria) to inhibit the formation of plaque. As a usable red alga are explicitly Gigartinales, especially Gracilaria verrucosa, named as suitable brown algae Fucus, in particular Hizikia fusiformis.

JP2001233751 describes the use of extracts from Hamamelidaceae, Labiatae, Rosaceae and Myrtaceae for the inhibition of glucosyltransferase Streptococcus mutans.

DE3343200 describes the use of chitin and chitin derivatives, in particular of chitosan, in oral or oral preparations, the chitosan derivatives used having molecular weights of 47,000, 88,000 and 114,000 g / mol, the chitosan having a molecular weight of 114,000 g / mol far less good for neutralization of lactic acid is suitable as the chitosan having a molecular weight of 47000 g / mol.

task It was the object of the present invention to provide further substances and / or extracts to disposal to provide a good to very good inhibition of glucosyltransferase cause and thus to inhibit plaque formation are suitable.

Surprisingly it has now been found that extracts selected from the group exist from extracts from the orders Fucales, Ericales, Saxifragales, Malpighiales, Malvales, Lamiales, Rosales, Fagales, Asterales, Myrtales, Apiales, Zingiberales, Magnoliales, Piperales, Laurales, Coniferales and / or Sapindales and isolatable from plant extracts Substances chlorogenic acid, Trigonelline and trans-cinnamic acid and chitosans having an average molecular weight greater than or equal 200000 g / mol and Cardacetil a very good inhibition of glucosyltransferase and / or cause the biofilm formation, wherein with some of said Extracts and / or substances achieved an almost complete inhibition of glucosyltransferase activity could be.

object The present invention therefore provides the use of an extract from the orders Fucales, Ericales, Saxifragales, Malpighiales, Malvales, Lamiales, Rosales, Fagales, Asterales, Myrtales, Apiales, Zingiberal, Magnoliales, Piperales, Laurales, Coniferales and / or Sapindales for the inhibition of glucosyltransferase (dextran sucrase) and / or to prevent or inhibit bacterial biofilm formation and / or for the removal of bacterial biofilms, which are in the bacterial biofilm is preferably plaque, and / or to prevent or inhibit caries formation and / or treatment of tooth decay.

at the extract of the order Fucales is preferably an extract of the family of Fucaceae, more preferred from Fucus sp. or Ascophyllum sp., especially from Fucus vesicolosus, Fucus spiralis or from Ascophyllum nodosum, being Fucus vesiculosus is particularly preferred, since surprisingly it was found that the Fucus vesiculosus extract with 99 a nearly full Inhibition of glycosyltransferase causes one 85% inhibition by Ascophyllum nodosum and a 47% Inhibition by Fucus spiralis.

at the extract of the order Ericales is preferably an extract from the Ericaceae or Theaceae family. at the extract from the Ericaceae family is preferably to an extract from the subfamily of Arbutoideae, in particular it is an extract of Arctostaphylos sp., especially from the Arctostaphylos uva-ursi (bearberry). Surprisingly could with a water / propylene glycol extract from the leaves of the bearberry an almost complete one Inhibition of glycosyltransferase can be achieved.

Of others may be the extract of the Ericaceae family especially an extract from the subfamily Vaccinioideae or the vacciniae, in particular an extract of vaccinium sp., mainly from Vaccinium myrtillus.

at the extract of the Theaceae family is preferably an extract of Camellia sp., in particular Camellia sinensis, wherein the extract is obtained from fermented or non-fermented leaves can be. Fermented with a water / propylene glycol extract Leaves (black Tea) could be a slightly better inhibitor of glycosyltransferase be achieved as with a water / propylene glycol extract non-fermented leaves (green Tea) (95 opposite 85%).

at the extract from the order Saxifragales is preferably to extract from the family Hamamelidaceae, in particular from Hamamelis sp., especially from Hamamelis virginiana. With a Water / propylene glycol extract from Hamamelis virginiana could surprisingly an almost complete one Inhibition of glycosyltransferase can be achieved.

at The extract from the order Saxifragales may be further in particular also an extract of Ribes sp., in particular from Ribes nigrum (blackcurrant) act.

at the extract of order Malpighiales is preferential to an extract from the family of Salicaceae or Saliceae, in particular an extract of Salix sp., especially from Salix alba (willow), or an extract of the family Clusiaceae, in particular from Hypericum sp. (St. John's Wort), especially from Hypericum perforatum. Water / propylene glycol extracts from willow bark and St. John's wort showed with 94 and 89 a very good inhibition of glycosyltransferase.

The extract of the order Malvales is preferably an extract from the Family of the Malvaceae, in particular from the subfamily of the Tilloideae, especially from Tillia sp., In particular from Tillia chordata. With a water / propylene glycol extract from the lime blossom, a very good value could be achieved with 88% inhibition of the glycosyltransferase.

at the extract from the order Sapindales is preferably to extract from the family of Sapindaceae, in particular Paullinia sp., Especially from Paullinia cupana (Guarana). Furthermore In particular, it can also be an extract from the family the Rutaceae, mainly from Citrus sp., especially from Citrus dulcis, act.

at the Lamial extract is preferably an extract from the family Lamiaceae, in particular from the subfamily of Nepetoideae or Nepeteae, particularly preferred this is an extract of Rosmarinus sp., in particular Rosmarinus officinalis, to extract an extract of thymus sp., In particular Thymus vulgaris, Melissa sp., Especially Melissa officinalis, Mentha Sp., in particular Mentha viridis or Mentha piperiada, wherein the Extract of Rosmarinus officinalis is most preferred.

at The extract from the order Rosales is preferably an extract from the family Cannabeceae, in particular from Humulus sp., Especially from Humulus lupus (hops). Furthermore, can it is also an extract from the Rosaceae family, especially an extract of Rubus sp., especially from Rubus idaeus (raspberry) act.

at Extract from the order Fagales is preferential to extract from the family of Juglandaceae, in particular from Juglans sp., especially from Juglans regia.

at the extract from the order Asterales is preferential to extract from the family of the Asteraceae, in particular the subfamily of the Asteroideae, Anthemideae or Matricaria, especially it is preferably an extract from Chamomilla sp., before everything from Chamomilla Recutita.

at the extract of the order Myrtales is preferential an extract from the family Lythraceae or from the family the Myrtaceae. The extract from the family Lythraceae acts it is preferably an extract of Punica sp., especially from Punica granatum. In the extract of the family Myrtaceae it is preferably an extract of Melaleuca sp., especially from Melaleuca alternifolia.

at the extract of order Apiales is preferential to extract from the family Apiaceae, in particular the subfamily Apioideae, more preferably Coriandum sp., especially from Coriandum sativum.

at Extract from order Zingiberales is preferential an extract from the family of Zingiberaceae, in particular from Curcuma sp., especially from Curcuma Zedoaria.

at the extract from the order Magnoliales is preferably to extract from the Myristicaceae family, in particular from Myristica sp., especially from Myristica fragrans.

at the extract from the order Piperales is preferably an extract from the family Piperaceae, in particular from Piper sp., Especially from Piper nigrum.

at the extract from the order Coniferales is preferably to extract from the family Pinaceae, in particular Picea sp., Especially from Picea excelsa.

The Preparation of the extracts can basically be done by anyone skilled in the art known manner using any plant tissue and using any extraction agent. Thus, the plant extract, for example, by extraction of the entire plant, by extraction from flowers, leaves, seeds, roots and / or by extraction from the meristem of the plant.

For example, water, alcohols and mixtures thereof can be used as extractants for the preparation of the plant extracts mentioned. As alcohols, for example, lower alcohols such as ethanol and isopropanol, but especially polyhydric alcohols such as ethylene glycol, propylene glycol and butylene glycol in question, both as the sole extractant and in admixture with water. For example, plant extracts based on water / propylene glycol in a ratio of 1:10 to 10: 1 proved to be particularly suitable. The extraction can be carried out, for example, in the form of steam distillation. Optionally, a dry extraction and / or a carbon dioxide extraction can take place.

at the extract of Fucus vesicolosus is preferably a glycolic extract, from the extracts of Ascophyllum nodosum and Fucus spiralis are preferably water / butylene glycol extracts, in the extracts of bearberry leaves, witch hazel, black and green Tea, willow bark, St. John's wort, lime blossom, guarana seed, walnut leaves, pomegranate, Blueberry and leaves the black currant is preferably water / propylene glycol extracts, for the extracts of rosemary leaves, Hops, chamomile flower, Thyme, melissa leaves, Coriander, turmeric, mace and black pepper is preferably a carbon dioxide extract and the raspberry extract is preferably a hydroalcoholic extract.

object The present invention is therefore further the use selected from at least one substance from the group consisting of chlorogenic acid, trigonellin and trans-cinnamic acid and extracts, containing at least one of the substances mentioned, as well as Cardacetil or one of its components L-carnosine and N-acetyl-L-carnosine and chitosans having an average molecular weight greater than or equal to 200,000 g / mol, in particular with an average molecular weight between 300,000 and 1200,000 g / mol, preferably with a medium Molecular weight between 450000 and 550000 or between 900000 and 1100000 g / mol, for the inhibition of glucosyltransferase (dextran Sucrase) and / or for the prevention or inhibition of bacterial Biofilm formation and / or removal of bacterial biofilms, wherein the bacterial biofilm is preferably plaque, and / or for the prevention or inhibition of caries formation and / or for the treatment of tooth decay.

chitosan having an average molecular weight of about 500,000 g / mol in this case preferably a distribution between 50,000 and 1,000,000 g / mol, chitosans having an average molecular weight of about 700000 a distribution between 300000 and 2 million and Chitosane with an average molecular weight of about 1,000,000 g / mol Distribution between 500000 and 5000000 g / mol.

object The present invention further relates to the use of chitosans having a molecular weight greater than or equal to 200,000 g / mol, in particular greater or equal 300,000 or 400,000 g / mol, for the inhibition of glucosyltransferase (Dextran sucrase) and / or for the prevention or inhibition of bacterial Biofilm formation and / or removal of bacterial biofilms, wherein the bacterial biofilm is preferably plaque and / or for the prevention or inhibition of caries formation and / or for the treatment of tooth decay.

The Chlorgensäure comes as a mixture with isomeric caffeic acid esters of quinic acid u.a. in Chrozophora, Cinchona, Scabiosa, Valeriana, Senecio and Hypericum species and was originally from Liberian coffee isolated. Trigonelline is u.a. contained in the seeds of fenugreek and in coffee beans. cinnamic acid is e.g. available from Styrax, Peruvian Balsam and other resins.

carnosine represents the highest Proportion of all amino acids, with the exception of carnitine, in human muscle tissue and many Chitosan is over a chemical process obtained mainly from crab shells. These are ground, deproteinized (extraction with dilute sodium hydroxide solution), demineralized and decolorized (e.g., with oxidizing agents). After an alkaline or enzymatic Deacetylation and a washing step, chitosan is obtained.

at the glucosyltransferase is preferably an enzyme from Leuconostoc sp. or Peptostreptococcus sp.

Another The present invention relates to oral, dental and / or Denture care agent containing substances according to the invention and / or extracts. The substances and / or extracts according to the invention are preferably in amounts of 0.001-10 wt .-%, particularly preferred from 0.01-2.0% by weight, especially in amounts of 0.05-1.0 wt .-% in the oral or dental care products contain.

The oral, Tooth and / or dental prosthesis care agents can be used, for example, as mouthwash, Gel, liquid Toothbrush lotion, stiff toothpaste, chewing gum, denture cleaner or Denture adhesive cream are present.

For this purpose, it is necessary, the substances of the invention and / or extracts in a suitable To incorporate wearers.

When carrier can e.g. also powdery Preparations or aqueous-alcoholic solutions serve as mouthwashes 0 to 15% by weight of ethanol, 1 to 1.5% by weight of aroma oils and 0.01 to 0.5% by weight sweeteners or as mouthwash concentrates 15 to 60 wt .-% ethanol, 0.05 to 5% by weight aroma oils, 0.1 up to 3% by weight of sweeteners and possibly other excipients may contain and before use with water dilute become. The concentration of the components must be chosen so high, that after dilution the mentioned lower concentration limits in the application not be fallen below.

When carrier can but gels as well as more or less flowable pastes serve that out flexible plastic containers or tubes and with the help of a toothbrush on the teeth be applied. Such products contain higher amounts of humectants and binders or consistency regulators and polishing components. Furthermore Aromatic oils, sweeteners and water are also contained in these preparations.

When Humectants can while e.g. Glycerol, sorbitol, xylitol, propylene glycols, polyethenylene glycols or Mixtures of these polyols, especially those Polyethenylenglycole with molecular weights of 200 to 800 (from 400 to 2000) are used be. Preferred as a humectant sorbitol in an amount from 25 - 40 Wt .-% included.

When Anti-calculus agents and as demineralization inhibitors can condensed phosphates in the form of their alkali metal salts, preferably in Be contained form of their sodium or potassium salts. The aqueous solutions of this Phosphates react alkaline due to hydrolytic effects. By the addition of acid is the pH of the oral, dental and / or dental prosthesis care agents according to the invention adjusted to the preferred values of 7.5-9.

It can also mixtures of different condensed phosphates or hydrated Salts of condensed phosphates are used. The specified Quantities from 2 - 12 However,% by weight refers to the anhydrous salts. Prefers As condensed phosphate is a sodium or potassium tripolyphosphate in an amount of 5 - 10 Wt .-% of the composition.

A preferred active ingredient is a caries-inhibiting fluorine compound, preferably from the group of fluorides or monofluorophosphates in an amount of 0.1 to 0.5 wt .-% fluorine. Suitable fluorine compounds are, for example, sodium monofluorophosphate (Na ₂ PO ₃ F), potassium monofluorophosphate, sodium or potassium fluoride, tin fluoride or the fluoride of an organic amino compound.

Suitable binders and consistency regulators are, for example, natural and synthetic water-soluble polymers such as carrageenan, tragacanth, guar, starch and their non-ionic derivatives such as hydroxypropyl guar, hydroxyethyl starch, cellulose ethers such as hydroxyethyl cellulose or methylhydroxypropyl cellulose. Also, agar-agar, xanthan gum, pectins, water-soluble carboxyvinyl polymers (for example Carbopol ^® types), polyvinyl alcohol, polyvinyl pyrrolidone, high molecular weight polyethylene glycols (molecular weight 10 ³ to 10 ⁶ D). Further substances which are suitable for viscosity control are phyllosilicates such as montmorillonite clays, colloidal thickening silicas, eg airgel silica or fumed silicas.

As polishing components may all heretofore known polishing agent, but preferably precipitated and gel silicas, aluminum hydroxide, aluminum silicate, alumina, alumina trihydrate, insoluble sodium metaphosphate, calcium pyrophosphate, calcium hydrogen phosphate, dicalcium phosphate, chalk, hydroxyapatite, hydrotalcites, talc, magnesium aluminum silicate (Veegum ^®), calcium sulfate, magnesium carbonate, Magnesium oxide, sodium aluminum silicates, such as zeolite A or organic polymers, such as polymethacrylate, are used. The polishing agents are preferably used in smaller amounts of eg 1-10% by weight.

The dental and / or oral care products according to the invention can be improved in their organoleptic properties by adding aroma oils and sweeteners. Aromatic oils are all natural and synthetic flavors which are customary for oral, dental and / or dental care products. Natural flavors can be used both in the form of the essential oils isolated from the drugs and the individual components isolated from them. Preferably, at least one aromatic oil from the group of peppermint oil, spearmint oil, aniseed oil, caraway oil, eucalyptus oil, fennel oil, cinnamon oil, geranium oil, sage oil, thyme oil, marjoram oil, basil oil, citrus oil, Gaultheria oil or one or more synthetic components of these oils isolated therefrom should be included. The most important components of the oils mentioned are, for example, menthol, carvone, anethole, cineol, eugenol, cinnamaldehyde, geraniol, citronellol, linalool, salvos, thy mol, terpinene, terpinol, methylchavicol and methyl salicylate. Further suitable flavors are, for example, menthyl acetate, vanillin, ionone, linalyl acetate, rhodinol and piperitone. Suitable sweeteners are either natural sugars such as sucrose, maltose, lactose and fructose or synthetic sweeteners such as saccharin sodium salt, sodium cyclamate or aspartame.

When Surfactants are especially alkyl and / or alkenyl (oligo) glycosides used. Their preparation and use as surface-active Substances are, for example, from US-A-3,839,318, US-A-3,707,535, US-A-3 547 828 DE-A-19 43,689, DE-A-20 36 472 and DE-A-30 01 064 and EP-A-77 167. Regarding the Glycosidrestes holds that both Monoglycosides (x = 1) in which a pentose or hexose residue is glycosidic to a primary Alcohol is bound with 4 to 16 carbon atoms, as well as oligomeric glycosides with a degree of oligomerization x to 10 are suitable. The degree of oligomerization is a statistical mean, the one for such technical products usual Homolog distribution is based.

As alkyl and / or alkenyl (oligo) glycoside, an alkyl and / or alkenyl (oligo) glucoside of the formula RO (C ₆ H ₁₀ O) _x -H in which R is an alkyl radical and is preferably suitable / or alkenyl group having 8 to 14 carbon atoms and x has an average of 1 to 4. Particular preference is given to alkyl oligoglucosides based on hydrogenated C _12/14 coconut oil having a DP of from 1 to 3. The alkyl and / or alkenyl glycoside surfactant can be used very sparingly, amounts of from 0.005 to 1% by weight being sufficient are.

In addition to the alkyl glucoside surfactants mentioned, other nonionic, ampholytic and cationic surfactants may also be present, for example: fatty alcohol polyglycol ether sulfates, monoglyceride sulfates, monoglyceride ether sulfates, mono- and / or dialkyl sulfosuccinates, fatty acid isethionates, fatty acid sarcosinates, fatty acid taurides, fatty acid glutamates, ether carboxylic acids, fatty acid glucamides, alkylamido betaine and / or protein fatty acid condensates, the latter preferably based on wheat proteins. In particular, to solubilize the usually water-insoluble aroma oils, a non-ionic solubilizer from the group of surface-active compounds may be required. Particularly suitable for this purpose are, for example, ethoxylated fatty acid glycerides, ethoxylated fatty acid sorbitan partial esters or fatty acid partial esters of glycerol or sorbitan ethoxylates. Solubilizers from the group of ethoxylated Fettsäureglyceride include especially adducts of 20 to 60 moles of ethylene oxide with mono- and diglycerides of linear fatty acids having 12 to 18 carbon atoms or triglycerides of hydroxy fatty acids such as oxystearic acid or ricinoleic acid. Further suitable solubilizers are ethoxylated fatty acid sorbitan partial esters; these are preferably addition products of 20 to 60 moles of ethylene oxide with sorbitan monoesters and sorbitan diesters of fatty acids with 12 to 18 carbon atoms. Also suitable solubilizers are fatty acid partial esters of glycerol or sorbitan ethoxylates; these are preferably mono- and diesters of C ₁₂ -C ₁₈ -fatty acids and adducts of 20 to 60 moles of ethylene oxide with 1 mole of glycerol or 1 mole of sorbitol.

The oral, Tooth and / or denture care agents preferably contain as a solubilizer for possibly contained aroma oils Addition products of 20 to 60 moles of ethylene oxide to hardened or uncured castor oil (i.e., oxystearic acid or ricinoleic acid triglyceride), glycerol mono- and / or distearate or sorbitan mono- and / or distearate.

• – Pigmente, z.B. Titandioxid, und/oder Farbstoffe
• – pH-Stellmittel und Puffersubstanzen wie z.B. Natriumbicarbonat, Natriumcitrat, Natriumbenzoat, Zitronensäure, Phosphorsäure oder saure Salze, z.B. NaH₂PO₄
• – wundheilende und entzündungshemmende Stoffe wie z.B. Allantoin, Harnstoff, Panthenol, Azulen bzw. Kamillenextrakt
• – weitere gegen Zahnstein wirksame Stoffe wie z.B. Organophosphonate, z.B. Hydroxyethandiphosphonate oder Azacycloheptandiphosphonat
• – Konservierungsstoffe wie z.B. Sorbinsäure-Salze, p-Hydroxybenzoesäure-Ester.
• – Plaque-Inhibitoren wie z.B. Hexachlorophen, Chlorhexidin, Hexetidin, Triclosan, Bromchlorophen, Phenylsalicylsäureester.

Other common additives for oral, dental and / or denture care medium are, for example

• - Pigments, such as titanium dioxide, and / or dyes
• PH adjusting agents and buffer substances, for example sodium bicarbonate, sodium citrate, sodium benzoate, citric acid, phosphoric acid or acid salts, for example NaH ₂ PO ₄
• - Wound-healing and anti-inflammatory substances such as allantoin, urea, panthenol, azulene or chamomile extract
• - Other anti-calculus substances such as organophosphonates, eg Hydroxyethandiphosphonate or Azacycloheptandiphosphonat
• - Preservatives such as sorbic acid salts, p-hydroxybenzoic acid esters.
• - Plaque inhibitors such as hexachlorophene, chlorhexidine, hexetidine, triclosan, bromochlorophene, Phenylsalicylsäureester.

In a particular embodiment the composition is a mouthwash, a mouthwash, a denture cleanser or a denture adhesive.

For prosthesis cleaners according to the invention, in particular prosthesis cleansing tablets and powders, in addition to the already mentioned ingredients for oral, dental and / or dental prosthesis care, per-compounds such as, for example, peroxoborate, peroxomonosulfate or percarbonate are additionally suitable. They have the advantage that they also deodorant and / or at the same time in addition to the bleaching effect have a disinfecting effect. The use of such per-compounds in prosthesis cleaners is between 0.01 and 10 wt .-%, in particular between 0.5 and 5 wt .-%.

When other ingredients are also enzymes, e.g. Proteases and carbohydrase, suitable for breaking down proteins and carbohydrates. The pH can be between pH 4 and pH 12, in particular between pH 5 and pH 11.

For the prosthesis cleansing tablets, additional auxiliaries are additionally necessary, such as, for example, agents which give off a bubbling effect, for example CO ₂ releasing substances such as sodium bicarbonate, fillers, for example sodium sulfate or dextrose, lubricants, for example magnesium stearate, flow regulators, for example colloidal silica and granulating agents, such as the already mentioned high molecular weight polyethylene glycols or polyvinylpyrrolidone.

Denture adhesives can be offered as powders, creams, foils or liquids and support the adhesion of the prostheses.

When Active ingredients are natural and synthetic swelling substances. As natural swelling substances are in addition Alginates also include plant gums such as e.g. Gum arabic, tragacanth and karaya gum as well as more natural To take rubber. In particular, alginates and synthetic have Swelling agents, e.g. Sodium carboxymethylcellulose, high molecular weight Ethylene oxide copolymers, salts of poly (vinyl ether-co-maleic acid) and Polyacrylamides.

When Excipients for pasty and liquid Products are particularly suitable hydrophobic basics, in particular Hydrocarbons, such as white Vaseline (DAB) or paraffin oil.

embodiments

Example 1: Determination the activity a dextran sucrase in vitro

When Model enzyme will be on sale available Dextran sucrase (E.C. 2.4.1.5) from Leuconostoc mesenteroides (Sigma Chemical Company # D9909). The unrestrained enzyme activity is after a modified method according to Kobayashi M, Matsuda M. (1980) Biochimica et Biophysica Acta 614, 46-62, becomes parallel the same experiment carried out in the presence of the inhibitor substances to be tested. The Reduction of activity of the enzyme compared to the uninhibited activity is considered a measure of the inhibitory effect the respective test substance. The work steps run, if not stated otherwise, at room temperature from:

Solutions:

• A: 50 mM Na acetate buffer with 1 mM CaCl ₂ , pH 5.2 (6.804 g NaCH ₃ COO.3H ₂ O, 0.147 g CaCl ₂ in 90 mL deionized water, pH adjusted to 5.2 with 1 M hydrochloric acid and made up to 1 L with deionized water).
• B: 15 g / 100 mL sucrose solution in solution A set.
• C: enzyme solution: immediately before the beginning of the measurement stated. 0.2 U / mL in ice-cold solution A. Store on ice.
• D: 5.2 mmol (1.2983 g) of CuSO ₄ .5H ₂ O are dissolved in 5 mL of deionized water, 0.26 mol (36.9304 g) of Na ₂ SO ₄ , 45 mmol (4.7695 g) of Na ₂ CO ₃ and 8.6 mmol (2.41272 g) of KNa tartrate 4H ₂ O are dissolved in 150 mL of deionized water and the copper sulfate solution is then added slowly. 38 mmol (3.1924 g) of NaHCO ₃ are dissolved in 30 mL of deionized water and also added to the mixed solution. The solution is made up to 200 mL with deionized water. Storage in the dark at room temperature, if necessary, a precipitate must be filtered off before using the solution.
• E: 8 mmol (9.8872 g) of ammonium molybdate tetrahydrate (NH ₄ ) ₆ Mo ₇ O ₂₄ .4H ₂ O are dissolved in 150 mL of deionized water, 151.2 mmol (15.4476 g) of sulfuric acid are added slowly, and Add a solution of 3.8 mmol (1.1856 g) of Na ₂ HAsO ₄ .7H ₂ O dissolved in 30 mL of deionized water. It is then made up to 200 mL with deionized water.

Water-soluble test substances are dissolved in buffer A. (1g / 100mL), water-insoluble in a suitable solvent (10g / 100mL) and then diluted 1:10 (v / v) with buffer A. Everyone Approach is done in triplicate and the result averaged.

Approaches for unrestrained activity ("standard") and for each test substance ("test") are pipetted; in each case a zero value without enzyme addition is set in parallel:

From the extinctions of the approaches the respective zero values are subtracted, the result is a measure of the enzyme activity. The relative activity in the presence of a test substance, expressed in percent residual activity on the uninhibited standard activity, reflects the suitability of Test substance as an inhibitor.

For example:

The extracts and substances listed in the following table showed a good inhibition of dextran sucrase:

Example 2: Toothbrush Assay

Hydroxyapatite-coated 48 well microtiter plates were mixed with 500 μl of a mixture of artificial saliva (0.1% Lab Lemco Powder, 0.2% yeast extract, 0.5% Proteose peptone, 0.25% mucin, 6 mM NaCl, 2.7 mM KCl, 3.5 mM KH ₂ PO ₄ , 1.5 mM K ₂ HPO ₄ , 0.05% urea, 1.8 mM CaCl ₂ , 10 μM hemin), BHI medium (ratio 3/1), 1% glucose and a bacterial mix consisting of Fusobacferium nucleatum (DSMZ 20482), Actinomyces naeslundii (DSMZ 43325 ), Streptococcus mutans (DSMZ 20523) and Streptococcus gordonii (DSMZ 6777) (1:50) and incubated anaerobically for 24 hours at 37 ° C. The surfaces were treated with a toothpaste formulation (basic formulation including 0.16% green tea extract (water / propylene glycol extract) (diluted 1: 2 with water) for 3 min at 600 rpm on a shaker Water and then filled with 500 .mu.l of medium as described above, the bacterial mixture now being used in a ratio of 1: 1500. The mixture was then incubated anaerobically for 24 h at 37 ° C. This treatment was repeated the following day Treat the plaque with the dentifrice formulation, wash twice with water and dry the remaining plaque.

When Controls were parallel to water instead of the toothpaste formulation or only the toothpaste formulation used without active ingredient.

Of the Biofilm was for Stained for 15 minutes with 0.01% safranine O. The solution was removed and the surfaces Rinsed once with water. After drying, the dye was extracted with DMSO and photometrically determined at 492 nm.

Result of the toothpaste assay:

Claims (42)

Use of an extract from the orders Fucales, Ericales, Saxifragales, Malpighiales, Malvales, Lamiales, Rosales, Fagales, Asterales, Myrtales, Apiales, Zingiberals, Magnolias, Piperales, Laurales, Coniferales and / or Sapindales for inhibition the dextran sucrase. Use of an extract from the orders Fucales, Ericales, Saxifragales, Malpighiales, Malvales, Lamiales, Rosales, Fagales, Asterales, Myrtales, Apiales, Zingiberals, Magnolias, Piperales, Laurales, Coniferales and / or Sapindales for inhibition bacterial biofilm formation and / or removal of bacterial Biofilms. Use according to claim 2, characterized that the bacterial biofilm is plaque. Use of an extract from the orders Fucales, Ericales, Saxifragales, Malpighiales, Malvales, Lamiales, Rosales, Fagales, Asterales, Myrtales, Apiales, Zingiberals, Magnolias, Piperales, Laurales, Coniferales and / or Sapindales for inhibition caries and / or caries. Use of an extract from the orders Fucales, Ericales, Saxifragales, Malpighiales, Malvales, Lamiales, Rosales, Fagales, Asterales, Myrtales, Apiales, Zingiberals, Magnolias, Piperales, Laurales, Coniferales and / or Sapindales in an oral and / or dentifrices. Use according to one of claims 1 to 5, characterized that the extract of the order Fucales is an extract from Fucus vesiculosus. Use according to one of claims 1 to 5, characterized that the extract of the order Fucales is an extract from Ascophyllum nodosum. Use according to one of claims 1 to 5, characterized that the extract of the order Fucales is an extract from Fucus spiralis. Use according to one of claims 1 to 5, characterized that the extract from the class Ericales is an extract from the bearberry is. Use according to one of claims 1 to 5, characterized that the extract from the class Ericales is an extract from Camelia sinensis. Use according to claim 10, characterized that the extract is fermented or unfermented Extract is. Use according to one of claims 1 to 5, characterized that the extract from the class Ericales is an extract from Vaccinuium myrtillus. Use according to one of claims 1 to 5, characterized that the extract from the genus Saxifragales is a Extract of Hamamelis virginiana is. Use according to one of claims 1 to 5, characterized that the extract from the genus Saxifragales is a Extract of Ribes nigrum acts. Use according to one of claims 1 to 5, characterized that the extract from the class Malpighiales is a Extract of St. John's Wort. Use according to one of claims 1 to 5, characterized that the extract from the class Malpighiales is a Extract from Salix alba (willow bark). Use according to one of claims 1 to 5, characterized that the extract from the class, Malvales is an extract from Tilia chordata. Use according to one of claims 1 to 5, characterized that the extract from the class Lamiales is an extract from Rosmarinus officinalis. Use according to one of claims 1 to 5, characterized that the extract from the class Lamiales is an extract from Thymus vulgaris. Use according to one of claims 1 to 5, characterized that the extract from the class Lamiales is an extract from Melissa officinalis. Use according to one of claims 1 to 5, characterized that the extract from the class Lamiales is an extract from Mentha viridis. Use according to one of claims 1 to 5, characterized that the extract from the class Lamiales is an extract from Mentha piperiata. Use according to one of claims 1 to 5, characterized that the extract from the class Rosales is an extract from humulus lupus (hops). Use according to one of claims 1 to 5, characterized that the extract from the class Rosales is an extract from Rubus idaeus. Use according to one of claims 1 to 5, characterized that the extract from the class Fagales is an extract from Juglans Regia (walnut) acts. Use according to one of claims 1 to 5, characterized that the extract from the class Asterales is an extract from Chamomilla Recutita. Use according to one of claims 1 to 5, characterized that the extract from the genus Myrtales is an extract from Punica granatum. Use according to one of claims 1 to 5, characterized that the extract from the genus Myrtales is an extract from Melaleuca alternifolia. Use according to one of claims 1 to 5, characterized that the extract from the genus Apiales is an extract from Coriandum sativum. Use according to one of claims 1 to 5, characterized that the extract from the genus Zingiberale is one Extract from Curcuma Zedoaria trades. Use according to one of claims 1 to 5, characterized that the extract from the class Magnoliales is one Extract from Myristica fragrans acts. Use according to one of claims 1 to 5, characterized that the extract from the class Piperales is an extract from Piper nigrum. Use according to one of claims 1 to 5, characterized that the extract from the class Laurales is an extract from Cinnamon zeylanicum. Use according to one of claims 1 to 5, characterized that the extract from the class Coniferales is a Extract from Picea excelsa. Use according to one of claims 1 to 5, characterized that the extract from the class Sapindales is one Extract of Citrus dulcis is. Use according to one of claims 1 to 5, characterized that the extract from the class Sapindales is one Extract from Paullinia sp. (Guarana) acts. Use of at least one substance selected from the group consisting of chlorogenic acid, trigonelline and trans-cinnamic acid as well Extracts containing at least one of the substances mentioned, as well as Cardacetil or one of its components L-carnosine and N-acetyl-L-carnosine and chitosans having an average molecular weight greater than or equal to 200,000 g / mol Inhibition of dextran sucrase. Use of at least one substance selected from the group consisting of chlorogenic acid, trigonellin and trans-cinnamic acid and extracts, containing at least one of the substances mentioned, as well as Cardacetil or one of its components L-carnosine and N-acetyl-L-carnosine and chitosans having an average molecular weight greater than or equal to 200,000 g / mol Inhibition of bacterial biofilm formation and / or removal of bacterial biofilms. Use according to claim 38, characterized in that the bacterial biofilm is um Plaque acts. Use of at least one substance selected from the group consisting of chlorogenic acid, trigonelline and trans-cinnamic acid as well Extracts containing at least one of the substances mentioned, as well as of Cardacetil or one of its constituents L-carnosine and N-acetyl-L-carnosine and chitosans having an average molecular weight greater than or equal to 200,000 g / mol Inhibition of caries and / or caries. Oral, dental and / or dental prosthesis care products containing at least one extract selected from the group consisting from extracts of Fucales, Ericales, Saxifragales, Malpighiales, Malvales, Lamiales, Rosales, Fagales, Asterales, Myrtales, Apiales, Zingiberal, Magnoliales, Piperales, Laurales, Coniferales and / or Sapindales. Oral, dental and / or dental prosthesis care products containing at least one substance selected from the group consisting from chlorogenic acid, Trigonelline and trans-cinnamic acid and extracts containing at least one of the substances mentioned as well as Cardacetil or one of its components L-carnosine and N-acetyl-L-carnosine and chitosans having an average molecular weight greater than or equal to 200000 g / mol.