WO2002041862A1 - An oral hygiene preparation for inhibiting halitosis - Google Patents

An oral hygiene preparation for inhibiting halitosis Download PDF

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Publication number
WO2002041862A1
WO2002041862A1 PCT/NO2001/000458 NO0100458W WO0241862A1 WO 2002041862 A1 WO2002041862 A1 WO 2002041862A1 NO 0100458 W NO0100458 W NO 0100458W WO 0241862 A1 WO0241862 A1 WO 0241862A1
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WO
WIPO (PCT)
Prior art keywords
oral hygiene
copper
gluconate
tablet
preparation
Prior art date
Application number
PCT/NO2001/000458
Other languages
French (fr)
Inventor
Gunnar Rölla
Original Assignee
Orix As
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Orix As filed Critical Orix As
Priority to AU2002224224A priority Critical patent/AU2002224224A1/en
Publication of WO2002041862A1 publication Critical patent/WO2002041862A1/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0216—Solid or semisolid forms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007—Effervescent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

  • This invention relates to an oral hygiene preparation for inhibiting halitosis, in the form of a tablet or a powder which upon dissolution in water forms a mouthwash.
  • the mouthwash thus produced is effective against oral malodour.
  • oral malodour is caused by volatile sulfur compounds (VSC) produced by bacterial catabolization of proteins in the oral cavity, in particular in the crypts at the back of the tongue and in periodontal pockets.
  • VSC volatile sulfur compounds
  • the VSC are mainly hydrogen sulfide and methyl mercaptan, which have a very unpleasant odour, even in low concentrations.
  • the VSC are also known to be able to penetrate oral epithelium and damage cells in the underlying connective tissue and bone, a process which is believed to be an important aspect of the initiation and progression of periodontal disease.
  • water-soluble salts of certain metals can inhibit oral malodour.
  • metals such as divalent cations of zinc, copper and tin.
  • the metals mentioned above have high affinity for sulfur and eliminate the VSC by forming insoluble sulfides with precursors of the volatile sulfur compounds, a reaction which inhibits further formation of the odiferous gases in the oral cavity.
  • water soluble, cationic, antibacterial agents such as the bis-biguanides and the quaternary ammonium compounds are able to inhibit oral malodour when used as mouth rinses.
  • Japanese Patent Application JP 1996/356310 discloses a composition for oral cavity, which can be used for prevention of bad breath. Possible components of the composition are triclosan, sodium bicarbonate, menthol and other fragrances.
  • Japanese Patent Application JP 1988/317621 (Publication JP 90164816 A2) relates to an aqueous drink containing ferrous sulfate and sodium bicarbonate. It is stated in the application that halitosis is inhibited by drinking said drink.
  • Japanese Patent Application JP 1985/39538 (Publication JP 86197510 A2) relates to a composition which may be in the form of a toothpaste, tooth powder, mouthwash, gingiva massage cream or local liquid or a paste paint.
  • the composition contains small amounts of nitroimidazole.
  • the composition further contains extracts from leaves of camellia plant such as tea tree or camellia or sodium copper-chlorophyllin.
  • the composition is used for prevention of periodental diseases and stomatosis and may also inhibit gram negative, anaerobic microorgansims from forming volatile sulfur compounds in the oral cavity.
  • WO 99/56714 relates to a bactericide for detergents which comprises an inorganic support having antifungal metal ions supported thereon, and a denture detergent containing the bactericide.
  • the bactericide is specifically intended for dentures and it is stated that it suppresses bad breath and denture-specific stomatitis.
  • WO-0023040 relates to a dry composition for inhibiting oral malodour, which comprises: a) at least one carrier material selected from saccharide materials
  • sweeteners b) at least one processing aid selected from oleaginous substances; and c) at least one active ingredient selected among many different types, including metallic ions.
  • Copper gluconate is mentioned as a source of metallic ions. It has now been discovered that a mouthwash produced from a tablet or a powder, which can be rapidly solubilized in water and which contains divalent cations of copper, exhibits a marked inhibiting effect against oral malodour.
  • the present invention provides an oral hygiene preparation for inhibiting halitosis, in the form of a tablet or powder which upon dissolution in water forms a mouthwash.
  • the preparation contains copper(ll)gluconate which provides cupric ions in water, and a physiologically acceptable disintegrating agent selected from sodium and calcium bicarbonate. Copper(ll)gluconate has sufficient solubility so that all of it is dissolved when the composition is added to a suitable amount of water.
  • Copper(ll)gluconate contains about 15% of copper.
  • a suitable amount of copper in a tablet or a powder dosage is an amount which provides a copper concentration of 0.003% to 0,3% by weight in 10 ml of water, and preferably a concentration of about 0,015%.
  • a tablet or a powder dosage should contain copper(ll)gluconate in an amount of 0.3-30 mg, preferably 0,5-5 mg, calculated as free cupric ions. This corresponds to 2-200 mg, preferably 3,5-35 mg, of copper gluconate.
  • the preparation according to the invention contains a physiologically acceptable disintegrating agent which facilitates the rapid solubilisation of the preparation, including the copper(ll)gluconate.
  • the disintegrating agents are selected from sodium and calcium bicarbonate, which may be used in amounts of 20-2000 mg, in particular 50-500 mg in a tablet designed to be dissolved in 10 ml of water. In a powder the amount of disintegrating agent, such as sodium bicarbonate, will generally be less than in a tablet.
  • a particularly preferred preparation according to the invention is a tablet which contains 50-500 mg of sodium bicarbonate and 5-50 mg of copper(ll) gluconate.
  • composition of the invention may also contain further components such as sweetening agents, flavouring agents, excipients and fillers.
  • sweetening agents such as aspartam, saccharin, xylitol and sorbitol.
  • other components such as acesulfam K, aspartam, saccharin, xylitol and sorbitol.
  • Tablets in the form of lozenges containing copper are already on the market as dietary supplements or for inhibiting oral malodour. Such tablets are designed to be solubilized in the mouth by sucking and are then often only sparingly soluble in water. Such tablets are markedly different from the tablets described in the present application.
  • An agent with an inhibiting effect on oral malodour is far more effective in the aqueous form of a mouthwash than in the dry state of a sucking tablet. The reason is that the VSC are highly soluble in water.
  • the aqueous part of a mouthwash is accordingly effective as such, this being in addition to the effect of the solubilized agents present in the mouthwash, as mentioned above.
  • the present invention combines the availability and convenience in the use of tablets, powders or other solid compositions, with the superior effect exhibited by mouthwashes.
  • a further advantage of a mouthwash compared with a sucking tablet is that the use of a mouthwash involves a local effect only of the copper cations in the mouth, because the mouthwash is expectorated after use, whereas the ingredients in a sucking tablet would have to be swallowed.
  • a powder designed to be dissolved in 20 ml of water A powder designed to be dissolved in 20 ml of water:
  • Sweeteners and flavours quantum satisfies

Abstract

An oral hygiene preparation for inhibiting halitosis, in the form of a tablet or a powder forming a mouthwash upon dissolution in water, which contains copper(II)gluconate and a disintegrating agent selected from sodium and calcium bicarbonate.

Description

"An oral hygiene preparation for inhibiting halitosis."
This invention relates to an oral hygiene preparation for inhibiting halitosis, in the form of a tablet or a powder which upon dissolution in water forms a mouthwash. The mouthwash thus produced is effective against oral malodour. It is well established that oral malodour is caused by volatile sulfur compounds (VSC) produced by bacterial catabolization of proteins in the oral cavity, in particular in the crypts at the back of the tongue and in periodontal pockets. The VSC are mainly hydrogen sulfide and methyl mercaptan, which have a very unpleasant odour, even in low concentrations. The VSC are also known to be able to penetrate oral epithelium and damage cells in the underlying connective tissue and bone, a process which is believed to be an important aspect of the initiation and progression of periodontal disease.
It is furthermore known that water-soluble salts of certain metals, such as divalent cations of zinc, copper and tin, can inhibit oral malodour. The metals mentioned above have high affinity for sulfur and eliminate the VSC by forming insoluble sulfides with precursors of the volatile sulfur compounds, a reaction which inhibits further formation of the odiferous gases in the oral cavity.
It is also well known that water soluble, cationic, antibacterial agents such as the bis-biguanides and the quaternary ammonium compounds are able to inhibit oral malodour when used as mouth rinses.
Japanese Patent Application JP 1996/356310 (Publication JP 98182384 A2) discloses a composition for oral cavity, which can be used for prevention of bad breath. Possible components of the composition are triclosan, sodium bicarbonate, menthol and other fragrances.
Japanese Patent Application JP 1988/317621 (Publication JP 90164816 A2) relates to an aqueous drink containing ferrous sulfate and sodium bicarbonate. It is stated in the application that halitosis is inhibited by drinking said drink.
Japanese Patent Application JP 1985/39538 (Publication JP 86197510 A2) relates to a composition which may be in the form of a toothpaste, tooth powder, mouthwash, gingiva massage cream or local liquid or a paste paint. The composition contains small amounts of nitroimidazole. The composition further contains extracts from leaves of camellia plant such as tea tree or camellia or sodium copper-chlorophyllin. The composition is used for prevention of periodental diseases and stomatosis and may also inhibit gram negative, anaerobic microorgansims from forming volatile sulfur compounds in the oral cavity.
WO 99/56714 relates to a bactericide for detergents which comprises an inorganic support having antifungal metal ions supported thereon, and a denture detergent containing the bactericide. The bactericide is specifically intended for dentures and it is stated that it suppresses bad breath and denture-specific stomatitis.
The article "Effects of new flavonoid gums eliminating bad breath", Shokuhin Kogyo (SKGYAQ, 05598990); 1995; Vol.38 (4); pp. 70-8, relates to a chewing gum containing green tea flavonoids, chlorophyll copper complex and Hovenia dulcis. It is used for eliminating bad breath.
WO-0023040 relates to a dry composition for inhibiting oral malodour, which comprises: a) at least one carrier material selected from saccharide materials
(sweeteners); b) at least one processing aid selected from oleaginous substances; and c) at least one active ingredient selected among many different types, including metallic ions.
Copper gluconate is mentioned as a source of metallic ions. It has now been discovered that a mouthwash produced from a tablet or a powder, which can be rapidly solubilized in water and which contains divalent cations of copper, exhibits a marked inhibiting effect against oral malodour. The present invention provides an oral hygiene preparation for inhibiting halitosis, in the form of a tablet or powder which upon dissolution in water forms a mouthwash. The preparation contains copper(ll)gluconate which provides cupric ions in water, and a physiologically acceptable disintegrating agent selected from sodium and calcium bicarbonate. Copper(ll)gluconate has sufficient solubility so that all of it is dissolved when the composition is added to a suitable amount of water. Copper(ll)gluconate contains about 15% of copper. A suitable amount of copper in a tablet or a powder dosage is an amount which provides a copper concentration of 0.003% to 0,3% by weight in 10 ml of water, and preferably a concentration of about 0,015%. In order to obtain a suitable concentration of copper in the mouthwash, a tablet or a powder dosage should contain copper(ll)gluconate in an amount of 0.3-30 mg, preferably 0,5-5 mg, calculated as free cupric ions. This corresponds to 2-200 mg, preferably 3,5-35 mg, of copper gluconate.
The preparation according to the invention contains a physiologically acceptable disintegrating agent which facilitates the rapid solubilisation of the preparation, including the copper(ll)gluconate. The disintegrating agents are selected from sodium and calcium bicarbonate, which may be used in amounts of 20-2000 mg, in particular 50-500 mg in a tablet designed to be dissolved in 10 ml of water. In a powder the amount of disintegrating agent, such as sodium bicarbonate, will generally be less than in a tablet.
A particularly preferred preparation according to the invention is a tablet which contains 50-500 mg of sodium bicarbonate and 5-50 mg of copper(ll) gluconate.
The composition of the invention may also contain further components such as sweetening agents, flavouring agents, excipients and fillers. Examples of such other components are acesulfam K, aspartam, saccharin, xylitol and sorbitol.
Tablets in the form of lozenges containing copper are already on the market as dietary supplements or for inhibiting oral malodour. Such tablets are designed to be solubilized in the mouth by sucking and are then often only sparingly soluble in water. Such tablets are markedly different from the tablets described in the present application. An agent with an inhibiting effect on oral malodour is far more effective in the aqueous form of a mouthwash than in the dry state of a sucking tablet. The reason is that the VSC are highly soluble in water. The aqueous part of a mouthwash is accordingly effective as such, this being in addition to the effect of the solubilized agents present in the mouthwash, as mentioned above. This concept is supported by the well established observation that oral malodour is frequently associated with a dry mouth. Thus, the present invention combines the availability and convenience in the use of tablets, powders or other solid compositions, with the superior effect exhibited by mouthwashes. A further advantage of a mouthwash compared with a sucking tablet is that the use of a mouthwash involves a local effect only of the copper cations in the mouth, because the mouthwash is expectorated after use, whereas the ingredients in a sucking tablet would have to be swallowed.
Example 1
A powder designed to be dissolved in 20 ml of water:
Cupric gluconate 20 mg Sodium bicarbonate 50 mg
Xylitol 2000 mg
Sweeteners and flavours quantum satis
Example 2 Tablet designed to be dissolved in 10 ml of water:
Cupric gluconate 5 mg
Sodium bicarbonate 100 mg
Xylitol/Sorbitol 1000 mg Constituents ad 2000 mg
Example 3
Tablet designed to be dissolved in 10 ml of water:
Cupric gluconate 10 mg
Calcium bicarbonate 90 mg
Acesulfam K quantum satis Constituents ad 500 mg Example 4
Tablet designed to be dissolved in 20 ml of water:
Cupric gluconate 15 mg
Sodium bicarbonate 200 mg
Xylitol 2000 mg
Constituents ad 3000 mg

Claims

C L A I M S
1. An oral hygiene preparation for inhibiting halitosis, in the form of a tablet or a powder forming a mouthwash upon dissolution in water and containing copper(ll)gluconate, wherein said preparation also contains a physiologically acceptable disintegrating agent selected from sodium and calcium bicarbonate.
2. The oral hygiene preparation of claim 1 , which contains a higher alcohol selected from xylitol and sorbitol.
3. The oral hygiene preparation of any of claims 1 and 2 in the form of a tablet or a powder dosage containing copper(ll)gluconate in an amount of
0,3-30 mg, calculated as free cupric ions, and said disintegrating agent in an amount of 20 - 2000 mg.
4. The oral hygiene preparation of claim 3, wherein the amount of copper(ll)gluconate, calculated as free cupric ions, is 0,5-5 mg.
5. The oral hygiene preparation of any of claims 3 and 4, wherein the amount of said disintegrating agent is 50 - 500 mg.
6. The oral hygiene preparation of claim 1 in the form of a tablet containing 50- 500 mg of sodium bicarbonate and 5-50 mg of copper(ll)gluconate.
PCT/NO2001/000458 2000-11-21 2001-11-19 An oral hygiene preparation for inhibiting halitosis WO2002041862A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002224224A AU2002224224A1 (en) 2000-11-21 2001-11-19 An oral hygiene preparation for inhibiting halitosis

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
NO20005877A NO312153B1 (en) 2000-11-21 2000-11-21 Oral hygiene preparations for inhibiting halitosis
NO20005877 2000-11-21

Publications (1)

Publication Number Publication Date
WO2002041862A1 true WO2002041862A1 (en) 2002-05-30

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NO (1) NO312153B1 (en)
WO (1) WO2002041862A1 (en)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3003247A4 (en) * 2013-03-15 2017-01-04 CDA Research Group, Inc. Topical copper ion treatments
US10398733B2 (en) 2013-03-15 2019-09-03 Cda Research Group, Inc. Topical copper ion treatments and methods of treatment using topical copper ion treatments in the dermatological areas of the body
US10813948B2 (en) 2013-03-15 2020-10-27 Cda Research Group, Inc. Methods of treatment using topical copper ion formulations
US11000545B2 (en) 2013-03-15 2021-05-11 Cda Research Group, Inc. Copper ion compositions and methods of treatment for conditions caused by coronavirus and influenza
US11193184B2 (en) 2019-02-22 2021-12-07 Cda Research Group, Inc. System for use in producing a metal ion suspension and process of using same
US11318089B2 (en) 2013-03-15 2022-05-03 Cda Research Group, Inc. Topical copper ion treatments and methods of making topical copper ion treatments for use in various anatomical areas of the body

Citations (6)

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GB1203308A (en) * 1967-10-02 1970-08-26 Miles Lab Improvements in or relating to tableting lubricants and tableting processes
US4112066A (en) * 1976-06-21 1978-09-05 Life Savers, Inc. Breath freshener composition and method
US4971785A (en) * 1988-03-14 1990-11-20 Spectrum Consumer Products Co., Inc. Non-alcoholic delivery system for orally ingestible active ingredients
EP0471396A1 (en) * 1990-08-16 1992-02-19 Unilever N.V. Dental compositions containing stabilized copper
US6030605A (en) * 1997-04-03 2000-02-29 Nabisco, Inc. Breath freshening compositions and methods using them
WO2000023040A1 (en) * 1998-10-16 2000-04-27 Fuisz Technologies Ltd. Dry deodorizing composition for oral administration

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1203308A (en) * 1967-10-02 1970-08-26 Miles Lab Improvements in or relating to tableting lubricants and tableting processes
US4112066A (en) * 1976-06-21 1978-09-05 Life Savers, Inc. Breath freshener composition and method
US4971785A (en) * 1988-03-14 1990-11-20 Spectrum Consumer Products Co., Inc. Non-alcoholic delivery system for orally ingestible active ingredients
EP0471396A1 (en) * 1990-08-16 1992-02-19 Unilever N.V. Dental compositions containing stabilized copper
US6030605A (en) * 1997-04-03 2000-02-29 Nabisco, Inc. Breath freshening compositions and methods using them
WO2000023040A1 (en) * 1998-10-16 2000-04-27 Fuisz Technologies Ltd. Dry deodorizing composition for oral administration

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11083750B2 (en) 2013-03-15 2021-08-10 Cda Research Group, Inc. Methods of treatment using topical copper ion formulations
EP3003247A4 (en) * 2013-03-15 2017-01-04 CDA Research Group, Inc. Topical copper ion treatments
US10398733B2 (en) 2013-03-15 2019-09-03 Cda Research Group, Inc. Topical copper ion treatments and methods of treatment using topical copper ion treatments in the dermatological areas of the body
US10813948B2 (en) 2013-03-15 2020-10-27 Cda Research Group, Inc. Methods of treatment using topical copper ion formulations
US11000545B2 (en) 2013-03-15 2021-05-11 Cda Research Group, Inc. Copper ion compositions and methods of treatment for conditions caused by coronavirus and influenza
US11007143B2 (en) 2013-03-15 2021-05-18 Cda Research Group, Inc. Topical copper ion treatments and methods of treatment using topical copper ion treatments in the oral-respiratory-otic areas of the body
AU2014235706B2 (en) * 2013-03-15 2018-11-01 Cda Research Group, Inc. Topical copper ion treatments
US11857514B2 (en) 2013-03-15 2024-01-02 Cda Research Group, Inc. Topical copper ion treatments and methods of treatment using topical copper ion treatments in the dermatological areas of the body
US11318089B2 (en) 2013-03-15 2022-05-03 Cda Research Group, Inc. Topical copper ion treatments and methods of making topical copper ion treatments for use in various anatomical areas of the body
US11298316B2 (en) 2013-03-15 2022-04-12 Cda Research Group, Inc. Topical copper ion treatments and methods of treatment using topical copper ion treatments in the oral-respiratory-otic areas of the body
US11253544B2 (en) 2013-03-15 2022-02-22 Cda Research Group, Inc. Methods of treatment using topical copper ion formulations
US11717535B2 (en) 2013-03-15 2023-08-08 Cda Research Group, Inc. Copper ion compositions and methods of treatment for conditions caused by coronavirus and influenza
US11459638B2 (en) 2019-02-22 2022-10-04 Cda Research Group, Inc. System for use in producing a metal ion suspension and process of using same
US11193184B2 (en) 2019-02-22 2021-12-07 Cda Research Group, Inc. System for use in producing a metal ion suspension and process of using same

Also Published As

Publication number Publication date
AU2002224224A1 (en) 2002-06-03
NO20005877D0 (en) 2000-11-21
NO20005877A (en) 2002-04-02
NO312153B1 (en) 2002-04-02

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