WO1994000103A1 - Compositions agissant contre le tartre dentaire - Google Patents

Compositions agissant contre le tartre dentaire Download PDF

Info

Publication number
WO1994000103A1
WO1994000103A1 PCT/US1993/005521 US9305521W WO9400103A1 WO 1994000103 A1 WO1994000103 A1 WO 1994000103A1 US 9305521 W US9305521 W US 9305521W WO 9400103 A1 WO9400103 A1 WO 9400103A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition according
anticalculus
acid
fluoride
anticalculus composition
Prior art date
Application number
PCT/US1993/005521
Other languages
English (en)
Inventor
Donald James White, Jr.
Giles Jude Leonard
Original Assignee
The Procter & Gamble 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 The Procter & Gamble Company filed Critical The Procter & Gamble Company
Publication of WO1994000103A1 publication Critical patent/WO1994000103A1/fr

Links

Classifications

    • 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
    • A61K8/55—Phosphorus compounds
    • 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/8141—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
    • A61K8/8147—Homopolymers or copolymers of acids; Metal or ammonium salts thereof, e.g. crotonic acid, (meth)acrylic acid; Compositions of derivatives of such polymers
    • 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

  • the present invention relates to oral compositions containing a mixture of certain polyphosphonate and a limiting anionic polycar- boxylate, which compositions provide unexpected anticalculus benefits.
  • Dental calculus or tartar as it is sometimes called, is a deposit which forms on the surfaces of the teeth at the gingival margin. Supragingival calculus appears principally in the areas near the orifices of the salivary ducts; e.g., on the lingual surfaces of the lower anterior teeth and on the buccal surfaces of the upper first and second molars, and on the distal surfaces of the posterior molars.
  • British Patent 490.384. February 15, 1937 discloses oral compositions containing ethylenediaminetetraacetic acid, nitrilotriacetic acid and related compounds including pyrophosphates as anticalculus agents.
  • U.S. Patent 3.678.154. July 18, 1972 to Widder et al discloses oral compositions containing certain polyphosphonates and fluoride.
  • U.S. Patent 3,737.533. June 5, 1973 to Francis discloses oral compositions containing certain carbonyl c diphosphonates.
  • compositions 5 which deliver an anticalculus benefit.
  • the present invention embraces an oral composition comprising:
  • safe and effective amount means sufficient amount of material to provide the desired benefit while being safe to the hard and soft tissues of the oral cavity.
  • polyphosphonates found useful in the present invention are those set forth in U.S. Patent 3,488,419, to McCune et al., January 6, 1970 incorporated herein in its entirety by reference.
  • the polyphosphonates useful herein are selected from the group consisting of those of the formulae:
  • R ⁇ and R 2 are hydrogen or CH 2 0H; n is an integer of from 3 to 10; R 3 is hydrogen, alkyl containing from 1 to about 20 carbon atoms, alkenyl containing from 2 to about 20 carbon atoms, aryl (e.g., phenyl and naphthyl), phenylethenyl, benzyl, halogen (e.g., dimethylamino, diethylamino, N-hydroxy-N-ethylamino, acetylamino), -CH 2 C00H, -CH 2 P0 3 H 2 ,
  • R 4 is hydrogen, lower alkyl (e.g., methyl, ethyl, propyl, and butyl), amino, benzyl, halogen (e.g., chlorin bromine and fluorine), hydroxyl, -CH 2 C00H, -CH 2 P0 3 H 2 , or -CH 2 CH 2 P0 3 H 2 ; or a pharmaceutically acceptable salt thereof such as alkali metal (e.g., sodium and potassium), alkaline earth metal (e.g., calcium an magnesium), and ammonium or low molecular weight substituted ammoniu (e.g., mono-, di, and triethanolammonium) salts, and a carrie suitable for use in the oral cavity, the pH of the composition bein within the range from about 5.0 to about 11.0.
  • alkali metal e.g., sodium and potassium
  • alkaline earth metal e.g., calcium an magnesium
  • ammonium or low molecular weight substituted ammoniu e.g.
  • Formula (II) are ethane-l-hydroxy-l,l-diphosphonic acid; ethanediphosphonic acid; methanehydroxydiphosphonic acid; - 0 ethane-l,l,2-triphosphonic acid; propane-l,l,3,3-tetraphosphonic acid; ethane-2-phenyl-l,l-diphosphonic acid; ethane-2-naphthyl-l,l-diphosphonic acid; ethanephenyldiphosphonic acid; ?5 ethane-l-amino-l,l-diphosphonic acid; methanedichlorodiphosphonic acid; nonane-5,5-diphosphonic acid; n-pentane-l,l-diphosphonic acid; ethanedifluorodiphosphonic acid; _ 0 methanedibromodiphosphonic acid; propane-2,2-diphosphonic acid; ethane-2-carboxy
  • 1-diphosphonic acid propane-1-hydroxy-1,1,3-triphosphonic acid; 35 ethane-2-hydroxy-l,l,2-triphosphonic acid; propane-l,3-diphenyl-2,2-diphosphonic acid; nonane-l,l-diphosphonic acid; decane-l,-hydroxy-l,l-diphosphonic acid hexadecane-1,1-diphosphonic acid; pent-4-ene-l-hydroxy-l,l-diphosphonic acid; octadec-9-ene-l-hydroxy-l,l-diphosphonic acid; 3-phenyl-l,l-diphosphonoprop-2-ene; octane-l,l-diphosphonic acid; dodecane-l,l-disphosphonic acid; phenylaminomethanediphosphonic acid; naphthylaminomethanediphosphonic acid; N,N-dimethylaminomethanediphosphonic acid; N
  • Ethane-l-hydroxy-l,l-diphosponic acid an especially preferred polyphosphonate, has the molecular formula CH 3 C(0H)(P0 3 H 2 ) 2 .
  • the acid might also be named 1-hydroxyethylidene diphosphonic acid.
  • the most readily crystallizable salt of this acid is obtained when three of the acid hydrogens are replaced by sodium.
  • Preferred salts for the purpose of this invention are the trisodium hydrogen salt which has the structure:
  • the trisodium hydrogen salt normally crystallizes as the hexahydrate which loses some water during air-drying to yield a mixture of the hexa- and monohydrate averaging 3 to 4 molecules of water of hydration.
  • the polyphosphonate is used as an effective amount generally from about 0.1 about 6% preferably from about .5 to about 2.0%.
  • the synthetic anionic polycarboxylates employed herein are well known, being employed in the form of their free acids or partially or preferably fully neutralized water soluble alkali metal (e.g. 0 potassium and preferably sodium) or ammonion salts.
  • Preferred are 1:4 to 4:1 copolymers of aleic anhydride or acid with another polymerizable ethylenically unsaturated monomer, preferably methyl vinyl ether (methoxyethylene) having a molecular weight (M.W.) of about 30,000 to about 1,000,000.
  • M.W. molecular weight
  • These copolymers are available for C example as Gantrez (AN 139(M.W. 500,000), A.N. 119 (M.W. 250,000) and preferably S-97 Pharmaceutical Grade (M.W. 70,000), of GAF Corporation.
  • Suitable generally are polymerized olefinically or ethylenically unsaturated carboxylic acids containing an activated carbon-to-carbon olefinic double bond and at least one carboxyl group, that is, an acid containing an olefinic double bond which readily functions in poly ⁇ merization because of its presence in the monomer molecule either in the alpha-beta position with respect to a carboxyl group or as part of a terminal ethylene grouping.
  • Such acids are acrylic, methacrylic, ethacrylic, alpha-chloroacrylic, crotonic, beta-acryloxy propionic, sorbic, alpha-chlorsorbic, cinnamic, beta- styrylacrylic, muconic, itaconic, citraconic, mesaconic, glutaconic, aconitic, alpha-phenyl-acrylic, 2-benzyl acrylic, 2-cyclohexylacrylic, angelic, umbellic, fumaric, maleic acids and anhydrides.
  • Other different olefinic monomers copolymerizable with such carboxylic monomers include vinylacetate, vinyl chloride, dimethyl aleate and the like. Copolymers contain sufficient carboxylic salt groups for water-solubility.
  • the synthetic anionic polymeric polycarboxylate component is mainly a hydrocarbon with optional halogen and O-containing substituents and linkages as present in for example ester, ether and OH groups, and when present is generally employed in the instant compositions in approximate weight amounts of 0.05 to 3%, preferably 0.05 to 2%, more preferably 0.1 to 2%.
  • Water Soluble Fluoride Ion Source is mainly a hydrocarbon with optional halogen and O-containing substituents and linkages as present in for example ester, ether and OH groups, and when present is generally employed in the instant compositions in approximate weight amounts of 0.05 to 3%, preferably 0.05 to 2%, more preferably 0.1 to 2%.
  • Water-soluble fluoride compounds in the present compositions are present in an amount sufficient to give a fluoride concentration of from about 0.0025% to about 5.0% by weight, preferably from about 0.005% to about 2.0% by weight, to provide anticaries efficacy.
  • Preferred fluorides are sodium fluoride, stannous fluoride, indium fluoride, and sodium monofluorophosphate.
  • Norris et al., U.S. Patent 2.946.735. issued July 26, 1960 and Widder et al., U.S. Patent 3.678.154. issued July 18, 1972 disclose such salts as well as others. Both patents are incorporated herein by reference. Fluorides serve to combat caries as well as to inhibit pyrophosphatase as does the synthetic anionic polycarboxylate.
  • Pharmaceutically Acceptable Carrier serve to combat caries as well as to inhibit pyrophosphatase as does the synthetic anionic polycarboxylate.
  • the carrier for the polyphosphonate and the synthetic anionic polycarboxylate can be any vehicle suitable for use in the oral cavity.
  • Such carriers include the usual components of mouthwashes, toothpastes, tooth powders, prophylaxis pastes, lozenges, gums and the like and are more fully described hereinafter. Dentifrices and mouthwashes are the preferred systems.
  • the abrasive polishing material contemplated for use in the c present invention can be any material which does not excessively abrade dentin.
  • silicas including gels and precipitates, calcium carbonate, dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, calcium polymetaphos- phate, insoluble sodium polymetaphosphate, hydrated alumina, and
  • resinous abrasive materials such as particulate condensation products of urea and formaldehyde, and other such as disclosed by Cooley et al . in U.S. Patent 3,070,510, December 25, 1962, incorporated herein by reference. Mixtures of abrasives may also be used.
  • Silica dental abrasives of various types, can provide the unique
  • Silica abrasive materials are also exceptionally compatible with sources of soluble fluoride and polyphosphonates. For these reasons they are preferred for use herein.
  • the silica abrasive polishing materials useful herein, as well as the other abrasives generally have an average particle size ranging between about 0.1 to 30 microns, preferably 5 and 15 microns.
  • the silica abrasive can be precipitated silica or silica gels such as the silica xerogels described in Pader et al., U.S. Patent No. 3,538,230,
  • silica xerogels marketed under the tradename "Syloid" by the W. R. Grace & Company, Davison Chemical Division.
  • Preferred precipitated silica materials include those marketed by the J. M. Huber Corporation under the tradename, "Zeodent", particularly the silica carrying the designation "Zeodent 119". These silica abrasives are described in U.S. Patent No. 4,340,583, July 29, 1982, incorporated herein by reference.
  • the abrasive in the compositions described herein is present at a level of from about 6% to about 70%, preferably from about 15% to about 25% when the dentifrice is a toothpaste. Higher levels, as high as 90%, may be used if the composition is a toothpowder.
  • Flavoring agents can also be added to dentifrice compositions. Suitable flavoring agents include oil of wintergreen, oil of peppermint, oil of spearmint, oil of sassafras, and oil of clove. Sweetening agents which can be used include aspartame, acesulfame, saccharin, dextrose, levulose and sodium cyclamate. Flavoring and sweetening agents are generally used in dentifrices at levels of from about 0.005% to about 2% by weight.
  • Dentifrice compositions can also contain emulsifying agents.
  • emulsifying agents are those which are reasonably stable and foam throughout a wide pH range, including nonsoap anionic, nonionic, cationic, zwitterionic and amphoteric organic synthetic detergents. Many of these suitable surfactants are disclosed by Gieske et al . in U.S. Patent No. 4,051,234, September 27, 1977, incorporated herein by 5 reference.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention se rapporte à des compositions orales contenant un mélange de certains polyphosphonates et un carboxylate polymère anionique synthétique produisant un effet amélioré contre le tartre dentaire.
PCT/US1993/005521 1992-06-26 1993-06-10 Compositions agissant contre le tartre dentaire WO1994000103A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US90477892A 1992-06-26 1992-06-26
US07/904,778 1992-06-26

Publications (1)

Publication Number Publication Date
WO1994000103A1 true WO1994000103A1 (fr) 1994-01-06

Family

ID=25419760

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1993/005521 WO1994000103A1 (fr) 1992-06-26 1993-06-10 Compositions agissant contre le tartre dentaire

Country Status (2)

Country Link
MX (1) MX9303828A (fr)
WO (1) WO1994000103A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0836469A1 (fr) * 1995-07-05 1998-04-22 The Procter & Gamble Company Composition bactericide
WO2000002527A1 (fr) * 1998-07-09 2000-01-20 Colgate-Palmolive Company Composition orale pouvant lutter avec une efficacite amelioree contre la plaque dentaire
US6677391B1 (en) * 1999-12-08 2004-01-13 The Procter & Gamble Company Tartar control denture adhesive compositions

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0236827A2 (fr) * 1986-03-07 1987-09-16 Blendax GmbH Pâte dentifrice
EP0341662A2 (fr) * 1988-05-09 1989-11-15 The B.F. Goodrich Company Compositions orales pour l'inhibition du tartre et procédé
US5096699A (en) * 1990-12-20 1992-03-17 Colgate-Palmolive Company Anticalculus oral compositions

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0236827A2 (fr) * 1986-03-07 1987-09-16 Blendax GmbH Pâte dentifrice
EP0341662A2 (fr) * 1988-05-09 1989-11-15 The B.F. Goodrich Company Compositions orales pour l'inhibition du tartre et procédé
US5096699A (en) * 1990-12-20 1992-03-17 Colgate-Palmolive Company Anticalculus oral compositions

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0836469A1 (fr) * 1995-07-05 1998-04-22 The Procter & Gamble Company Composition bactericide
EP0836469A4 (fr) * 1995-07-05 1999-09-15 Procter & Gamble Composition bactericide
WO2000002527A1 (fr) * 1998-07-09 2000-01-20 Colgate-Palmolive Company Composition orale pouvant lutter avec une efficacite amelioree contre la plaque dentaire
AU747601B2 (en) * 1998-07-09 2002-05-16 Colgate-Palmolive Company, The Oral composition exhibiting enhanced antiplaque efficacy
US6677391B1 (en) * 1999-12-08 2004-01-13 The Procter & Gamble Company Tartar control denture adhesive compositions

Also Published As

Publication number Publication date
MX9303828A (es) 1994-01-31

Similar Documents

Publication Publication Date Title
EP0563265B1 (fr) Compositions buvables
US5096701A (en) Oral compositions
EP0180435B1 (fr) Compositions orales
US4847070A (en) Anticalculus compositions
US4515772A (en) Oral compositions
US4885155A (en) Anticalculus compositions using pyrophosphate salt
US5338537A (en) Oral compositions
US4684518A (en) Oral compositions
IE56956B1 (en) Oral compositions
IE893314L (en) Oral compositions
WO2018118140A1 (fr) Compositions de soins buccaux
EP0737059A1 (fr) Composition de dentifrice anti-tartre contenant du thymol
EP0249398A2 (fr) Composition orale
EP0311412A2 (fr) Compositions contre les calculs
US5456903A (en) Method of making a tartar control baking soda dentifrice
GB2204487A (en) Oral compositions
US5068100A (en) Anticalculus compositions
AU617987B2 (en) Anticalculus compositions
US5011830A (en) Oral compositions having improved anticalculus properties containing pyrophosphate and an acrylic acid polymer
EP0873747A2 (fr) Compositions orales de traitement de la plaque dentaire et de la gingivite contenant du carbonate de sodium et un sel de bicarbonate
WO1994000103A1 (fr) Compositions agissant contre le tartre dentaire
WO1994000102A1 (fr) Compositions agissant contre le tartre dentaire
US4990328A (en) Anticalculus compositions
US20180168964A1 (en) Oral Care Compositions

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): BR CA FI JP RU

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): AT BE CH DE DK ES FR GB GR IE IT LU MC NL PT SE

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
NENP Non-entry into the national phase

Ref country code: CA

122 Ep: pct application non-entry in european phase