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WO1999032075A1 - Compositions permettant d'inhiber la gingivite - Google Patents

Compositions permettant d'inhiber la gingivite Download PDF

Info

Publication number
WO1999032075A1
WO1999032075A1 PCT/US1998/025496 US9825496W WO9932075A1 WO 1999032075 A1 WO1999032075 A1 WO 1999032075A1 US 9825496 W US9825496 W US 9825496W WO 9932075 A1 WO9932075 A1 WO 9932075A1
Authority
WO
WIPO (PCT)
Prior art keywords
dentifrice
menthol
composition
eucalyptol
thymol
Prior art date
Application number
PCT/US1998/025496
Other languages
English (en)
Inventor
Rita M. Parikh
David Scott Harper
Anil Kumar Talwar
Bruce Kohut
Original Assignee
Warner-Lambert Company
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 Warner-Lambert Company filed Critical Warner-Lambert Company
Priority to JP2000525071A priority Critical patent/JP2001526202A/ja
Priority to CA002300205A priority patent/CA2300205A1/fr
Priority to BR9813729-8A priority patent/BR9813729A/pt
Priority to AU17076/99A priority patent/AU1707699A/en
Priority to EP98961857A priority patent/EP1041959A1/fr
Publication of WO1999032075A1 publication Critical patent/WO1999032075A1/fr

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • 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
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25Silicon; Compounds 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
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • 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
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37Esters of carboxylic acids
    • 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
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin

Definitions

  • the present invention relates to compositions and a method for
  • the invention is directed to a dentifrice
  • composition with particular amounts of specific essential oils and a method for
  • Volatile or essential oils are widely used in oral care products.
  • Essential oils are aromatic compounds that are derived from plant sources or
  • Thymol is a well-known substance that is associated with oral malodor, plaque and gingivitis.
  • oils include menthol, methyl salicylate, eucalyptol, anethol and eugenol. Essential oils have been included in formulations of toothpaste. U.S.
  • Patent No. 1,526,940 to Staegemann teaches a toothpaste with the germicide
  • Euthymol toothpaste has a pH
  • an antiplaque oral composition including a toothpaste, with triclosan.
  • antiplaque activity of the triclosan is increased by essential oils such as eucalyptol,
  • an antiseptic, anticaries dentifrice having a pH of about 3.0 to about 5.5.
  • dentifrice contains thymol from about 0.01% w/w to about 1.0 % w/w, menthol
  • formula contains 20 grains each of thymol, menthol, eucalyptol and oil of
  • dental hygiene composition in an acidic pH range of from 3.0 to 5.0, pH buffers,
  • composition is methyl salicylate or thyme oil and other flavors such that the composition is
  • compositions with antiseptic essential oils there is a need for dentifrice
  • compositions providing antigingivitis efficacy. Additionally, there is a need for a
  • dentifrice composition containing antigingivitis ingredients that remain stable for
  • the present invention is directed to a method of inhibiting gingivitis
  • methyl salicylate about 0.7 % w/w to about 1.0% w/w eucalyptol and about 0.3%
  • a dentifrice composition used in conjunction with a toothbrush cleans
  • Dentifrice compositions of this invention contain
  • the composition also has anticaries activity.
  • Dentifrice compositions of this invention also contain, but are not limited to, one
  • dentifrice additives acidifiers, abrasives, surfactants,
  • binders and thickeners binders and thickeners, humectants, sweeteners, desensitizing agents, flavors,
  • the dentifrice composition of the invention is acidified
  • acidifiers including, but not limited to,
  • Essential oils are volatile aromatic oils that are synthetic or are derived
  • compositions of this invention antigingivitis activity is provided by essential oils.
  • inventions include, but are not limited to, thymol, menthol, methyl salicylate
  • Thymol is a white crystalline
  • Thymol is soluble in organic solvents but
  • Menthol is isolated principally from the oil of Mentha arvensis. In its
  • menthol is available as L-menthol crystals obtained from a
  • Eucalyptol is derived from the eucalyptus tree. Having a cam-
  • Combinations of menthol and eucalyptol are widely used. Particularly preferred uses of the menthol-eucalyptol combination include, according to the
  • dentifrices such as toothpastes or dental gels.
  • Methyl salicylate is the main ingredient in many essential oils
  • the four essential oils used in the present invention are also used in the present invention.
  • Listerine® well .known mouthwash Listerine®. The amount of the oils in Listerine®
  • mouthwash is 0.064% thymol, 0.092% eucalyptol, 0.060% methyl salicylate and
  • Listerine® mouthwash is known to help reduce the incidence of
  • the recommended amount of mouthwash used at one time is the recommended amount of mouthwash used at one time.
  • thymol about 0.4644% to about 0.5676% methyl salicylate, about 0.306% to
  • Fluoride-releasing compounds may be used in the dentifrice
  • compositions of the present invention may be fully or slightly
  • compositions containing fluoride-releasing compounds help prevent dental caries.
  • Typical fluoride-releasing compounds are inorganic fluoride salts such as
  • compositions are preferred.
  • compositions of this invention must be nontoxic. The specific amount depends on
  • the fluoride-releasing compound will be present in an amount by weight
  • composition so as to provide 800 - 1500 ppm F " .
  • invention is from about 4.0 to about 5.0.
  • a pH greater than about 5.0 has been
  • pH of the dentifrice compositions from about 4.0 to about 5.0 also provides for a
  • the pH of the claimed dentifrice is adjusted to below 5.0 using suitable
  • Acidifiers in the present invention include
  • o sodium phosphate from about 0.01% w/w to about 1% w/w, preferably from about
  • the pH of the products may be buffered with salts of the acids in
  • citric acid-sodium citrate examples include citric acid-sodium citrate, phosphoric acid-sodium phosphate, sodium
  • composition and most preferably from about 0.1% w/w to about 0.5% w/w of the
  • compositions of the present invention may also contain
  • conventional dentifrice additives including, but not limited to, humectants,
  • binders thickeners, surfactants, preservatives, sweeteners, flavors, colors,
  • glycerin glycerin, and a buffer. These additives are present in amounts that do not interfere with the antiseptic, antigingivitis and anticaries properties of the composition of
  • Surfactants or surface active agents are organic compounds that reduce
  • the surfactant in the present invention may be anionic,
  • present invention may contain surfactants in amounts up to about 5.0% w/w; pre ⁇
  • the most preferred surfactants are anionic. These anionic
  • surfactants include, but are not limited to, sodium lauryl sulfate, sodium lauroyl
  • compositions according to the invention are sodium lauryl sulfate.
  • present invention are substantially free from one or more highly pure alkali metal
  • .Amphoteric surfactants have the capacity to behave as either an acid or
  • a base and include quaternized imidazole derivatives.
  • surfactants include long chain (alkyl) amino-alkylene aklylated amine derivatives
  • MIRANOL® manufactured by Rhone-Poulanc, Cranberry, New
  • the sweetener may be selected from a wide range of well .known
  • soluble saccharin salts e.g., sodium or calcium
  • Dipeptide sweeteners include
  • Naturally occurring water-soluble sweeteners include,
  • sugar alcohols including sorbitol as 70% sorbitol solution,
  • mannitol xylitol
  • maltitol hydrogenated starch hydrolysates and mixtures thereof.
  • water-soluble sweeteners include, but are not limited to, chlorinated derivatives of sucrose, .known, for example, under the product designation of Sucralose; and
  • Protein-based sweeteners such as thaumaoccous danielli (Thaumatin I and II).
  • Sorbitol solution supplies sweetness and body to the composition
  • Sorbitol solution also enhances flavor, prevents
  • an effective amount of sweetener is utilized to provide the
  • composition The exact range of amounts for each type of sweetener in a
  • dentifrice is readily determined by those skill in the art.
  • the flavors that may be used in the invention include natural and
  • Suitable flavors include, but are not
  • mints such as peppermint
  • citrus flavors such as orange and lemon
  • camphor, p-propenyl anisole is a flavor constituent of anise and fennel oils that
  • the flavors are preferably utilized in amounts that may
  • the dentifrice composition range from about 0.01% w/w to about 6% w/w of the dentifrice composition.
  • flavors used in the compositions according to the present invention comprise
  • flavoring oils that are not substantially free of terpenes.
  • coloring agents may be incorporated in amounts up to
  • the coloring agents may also
  • coloring agents are known as FD & C dyes and lakes.
  • coloring materials are preferably water-soluble.
  • Illustrative nonlimiting examples are exemplary nonlimiting examples
  • titanium dioxide may be incorporated in amounts up to about 2.0% w/w,
  • composition preferably less than about 1.0% w/w of the composition and most preferably less
  • Suitable humectants in this invention include sorbitol, as 70% sorbitol
  • Humectants may be present in amounts from about 1.0% to about 75.0% by
  • Suitable abrasive substances for use in this invention must be
  • composition according to this invention may include among others, ZEODENT®
  • polishing agents manufactured by W.R. Grace Co. These polishing agents may be used in amounts
  • composition up to about 75.0% w/w of the composition, preferably in amounts from about
  • the dentifrice composition includes an oral vehicle that can be a paste,
  • composition may also include binders or gelling agents to provide a desired
  • Gelling agents such as hydroxyethyl cellulose, carboxymethyl
  • cellulose methyl cellulose, xanthan gum, gelling silicas and the like may be used
  • the preferred gelling system is a mixture of carboxy
  • Gelling agents may be used in
  • the dentifrice composition of this invention may also contain a
  • desensitizing agent such as strontium chloride, potassium nitrate or sodium citrate-
  • citric acid which may be used in an amount from about 0.5% w/w to about 10%
  • Suitable preservatives include benzoic acid, butylated hydroxyanisole
  • BHA butylated hydroxytoluene
  • BHT butylated hydroxytoluene
  • ascorbic acid methyl paraben
  • methyl paraben propyl
  • Dentifrice compositions were formulated with the ingredients listed in
  • the plaque index used was the Turesky modification of the Quigley-Hein
  • index scores the amount of the toothsurface covered with plaque using a 0-5 point
  • the bleeding index used was the Gingival Bleeding Index as described in
  • Example 1 The subjects using Example 1 had a 39.6% reduction in Plaque Index, a
  • Example 2 The procedures and indices used in Example 2 were also used in
  • Example 3 In addition to the indices measured in the three week study, the
  • interproximal Plaque Index The subjects were measured at three and six months.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Cette invention concerne une composition dentifrice stable contenant du thymol, de l'eucalyptol, du salicylate de méthyle et du menthol, laquelle composition permet de lutter efficacement contre la gingivite.
PCT/US1998/025496 1997-12-22 1998-12-02 Compositions permettant d'inhiber la gingivite WO1999032075A1 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
JP2000525071A JP2001526202A (ja) 1997-12-22 1998-12-02 歯肉炎抑制のための組成物
CA002300205A CA2300205A1 (fr) 1997-12-22 1998-12-02 Compositions permettant d'inhiber la gingivite
BR9813729-8A BR9813729A (pt) 1997-12-22 1998-12-02 Composições para inibição da gengivite
AU17076/99A AU1707699A (en) 1997-12-22 1998-12-02 Compositions for inhibiting gingivitis
EP98961857A EP1041959A1 (fr) 1997-12-22 1998-12-02 Compositions permettant d'inhiber la gingivite

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US6839197P 1997-12-22 1997-12-22
US60/068,391 1997-12-22

Publications (1)

Publication Number Publication Date
WO1999032075A1 true WO1999032075A1 (fr) 1999-07-01

Family

ID=22082272

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1998/025496 WO1999032075A1 (fr) 1997-12-22 1998-12-02 Compositions permettant d'inhiber la gingivite

Country Status (7)

Country Link
EP (1) EP1041959A1 (fr)
JP (1) JP2001526202A (fr)
AU (1) AU1707699A (fr)
BR (1) BR9813729A (fr)
CA (1) CA2300205A1 (fr)
WO (1) WO1999032075A1 (fr)
ZA (1) ZA9811727B (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002525306A (ja) * 1998-09-25 2002-08-13 ワーナー−ランバート・カンパニー 急速溶解性口内消耗性フィルム
CN114306141A (zh) * 2021-12-31 2022-04-12 赣南医学院 一种漱口水用活性组合物和漱口水及其制备方法

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4482270B2 (ja) * 2002-10-31 2010-06-16 花王株式会社 口腔用組成物
JP2017119639A (ja) * 2015-12-28 2017-07-06 花王株式会社 Trpv4活性化剤

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5094843A (en) * 1990-09-10 1992-03-10 Beecham Inc. Antimicrobial toothpaste
WO1996003109A1 (fr) * 1994-07-25 1996-02-08 Warner-Lambert Company Dentifrice antiseptique
WO1997015277A1 (fr) * 1995-10-23 1997-05-01 Warner-Lambert Company Composition orale stanneuse amelioree
EP0803243A2 (fr) * 1996-04-24 1997-10-29 Pfizer Inc. Produits dentaires contenant des cyclodextrines et des composés phénoliques
WO1997040812A1 (fr) * 1996-04-26 1997-11-06 Warner-Lambert Company Composition buccale amelioree contenant du zinc

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5094843A (en) * 1990-09-10 1992-03-10 Beecham Inc. Antimicrobial toothpaste
WO1996003109A1 (fr) * 1994-07-25 1996-02-08 Warner-Lambert Company Dentifrice antiseptique
WO1997015277A1 (fr) * 1995-10-23 1997-05-01 Warner-Lambert Company Composition orale stanneuse amelioree
EP0803243A2 (fr) * 1996-04-24 1997-10-29 Pfizer Inc. Produits dentaires contenant des cyclodextrines et des composés phénoliques
WO1997040812A1 (fr) * 1996-04-26 1997-11-06 Warner-Lambert Company Composition buccale amelioree contenant du zinc

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002525306A (ja) * 1998-09-25 2002-08-13 ワーナー−ランバート・カンパニー 急速溶解性口内消耗性フィルム
US7407669B2 (en) 1998-09-25 2008-08-05 Mcneil-Ppc, Inc. Fast dissolving orally consumable films
US7491406B2 (en) 1998-09-25 2009-02-17 Mcneil-Ppc, Inc. Fast dissolving orally consumable films
CN114306141A (zh) * 2021-12-31 2022-04-12 赣南医学院 一种漱口水用活性组合物和漱口水及其制备方法

Also Published As

Publication number Publication date
ZA9811727B (en) 1999-06-24
EP1041959A1 (fr) 2000-10-11
BR9813729A (pt) 2000-10-10
CA2300205A1 (fr) 1999-07-01
JP2001526202A (ja) 2001-12-18
AU1707699A (en) 1999-07-12

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