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Details for Patent: 5,192,531

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Details for Patent: 5,192,531

Title: Antibacterial antiplaque oral composition
Abstract:An oral composition dentifrice containing an orally acceptable vehicle, about 30-75% by weight of a dentally acceptable water-insoluble polishing agent, a substantially water-insoluble noncationic antibacterial antiplaque agent, such as 2,4,4'-trichloro-2'-hydroxy-diphenyl ether (triclosan) an antibacterial enhancing agent which enhances the delivery of said antibacterial agent to, and retention thereof on, oral surfaces, and a surface active agent and/or a flavoring oil.
Inventor(s): Gaffar; Abdul (Princeton, NJ), Nabi; Nuran (Brunswick, NJ), Afflitto; John (Brookside, NJ), Stringer; Orum (Yardley, PA), Prencipe; Michael (East Windsor, NJ)
Assignee: Colgate-Palmolive Company (New York, NY)
Filing Date:Sep 09, 1991
Application Number:07/758,345
Claims:1. In a method of preparing an oral composition dentifrice free of polyphosphate anticalculus agent in an effective anticalculus amount wherein delivery and retention of a plaque-inhibiting antibacterial agent is enhanced by attaching, adhering or bonding to oral tooth and gum surfaces, which composition comprises an orally acceptable aqueous vehicle, about 30-75% by weight of a dentally acceptable water-insoluble polishing agent, an effective amount in the range of about 0.01-5% by weight of substantially water insoluble noncationic antibacterial agent and at least one of a surface active agent or a flavoring oil, the improvement comprising employing in said composition about 0.05-4% by weight of a water-soluble or swellable antibacterial-enhancing agent, which contains at least one delivery-enhancing functional group and at least one organic retention-enhancing group, wherein said delivery-enhancing group enhances delivery of said antibacterial agent to oral tooth and gum surfaces and said retention-enhancing group enhances attachment, adherence or bonding of surfaces.

2. In a method of attaching, adhering or bonding a plaque-inhibiting antibacterial agent to oral tooth and gum surfaces comprising applying to oral surfaces, an oral composition dentifrice comprising an orally acceptable aqueous vehicle, about 30-75% by weight of a dentally acceptable water insoluble polishing agent, an effective amount in the range of about 0.01-5% by weight of substantially water insoluble noncationic antibacterial agent and at least one of a surface active agent or flavoring oil, the improvement which comprises employing in said composition an effective amount in the range of about 0.05-4% by weight of a water-soluble or swellable antibacterial-enhancing agent which contains at least one delivery-enhancing functional group and at least one organic retention-enhancing group, which delivery-enhancing group enhances delivery of said antibacterial agent or oral tooth and gum surfaces and said retention-enhancing group enhances attachment, adherence or bonding of said antibacterial agent on oral tooth and gum surfaces, wherein said oral composition is free of polyphosphate anticalculus agent in an effective anticalculus amount.

3. The method claimed in either of claims 1 or 2 wherein said antibacterial agent is selected from the group consisting of halogenated diphenyl ethers, halogenated salicylanilides, benzoic esters, halogenated carbanilides and phenolic compounds.

4. The method claimed in claim 3 wherein said antibacterial agent is a halogenated diphenyl ether.

5. The method claimed in claim 4 wherein said halogenated diphenyl ether is 2,4,4'-trichloro-2'-hydroxydiphenyl ether.

6. The method claimed in claim either of claims 1 or 2 wherein said amount of antibacterial agent is about 0.25-0.5%.

7. The method claimed in either of claims 1 or 2 wherein said polishing agent is selected from the group consisting of sodium metaphosphate, tricalcium phosphate, dihydrated dicalcium phosphate, anhydrous dicalcium phosphate, calcium pyrophosphate, magnesium orthophosphate, trimagnesium phosphate, calcium carbonate, aluminum silicate, hydrated alumina, silica, bentonite and mixtures thereof.

8. The method claimed in claim 7 wherein said polishing agent is dicalcium phosphate dihydrate.

9. The method claimed in claim 7 wherein said polishing agent is hydrated alumina.

10. The oral method composition claimed in either or claims 65 or 66 wherein said surface active agent is present in amount of about 0.5-5% by weight.

11. The method claimed in claim 10 wherein said surface active agent is present in amount of about a 1-2.5% by weight.

12. The method claimed in either of claims 1 or 2 wherein said antibacterial-enhancing agent has an average molecular weight of about 100 to about 1,000,000.

13. The method claimed in claim 12 wherein said delivery enhancing group is acidic.

14. The method according to claim 13 wherein said delivery-enhancing group is selected from the group consisting of carboxylic, phosphonic, phosphinic, and sulfonic acids, and their salts, and mixtures thereof and wherein said retention-enhancing group comprises the formula --(X).sub.n --R wherein X is O, N, S, SO, SO.sub.2, P, PO, or Si, R is hydrophobic alkyl, alkenyl, acyl, aryl, alkaryl, aralkyl, heterocyclic, or their inert-substituted derivatives, and n is zero or 1 or more and wherein said antibacterial-enhancing agent is a natural or synthetic polymerizable monomer or a polymer selected from the group consisting of oligomers, homopolymers, copolymers of two or more monomers, ionomers, block copolmers, graft copolymers and cross-linked polymers and monomers.

15. The method claimed in claim 14 wherein said antibacterial-enhancing agent is an anionic polymer containing a plurality of said delivery-enhancing and retention-enhancing groups.

16. The method claimed in claim 15 wherein said anionic polymer comprises a chain containing repeating units each containing at least one carbon atom.

17. The method claimed in claim 16 wherein each unit contains at least one delivery-enhancing group and at least one organic retention-enhancing group bonded to the same or vicinal, or other atoms in the chain.

18. The method claimed in claim 14 wherein the delivery-enhancing group is a carboxylic group of salt thereof.

19. The method claimed in claim 18 wherein the antibacterial-enhancing agent is a copolymer of maleic acid or anhydride with another ethylenically unsaturated polymerizable monomer.

20. The method claimed in claim 19 wherein said other monomer of said copolymer is methylvinyl ether in a 4:1 to 1:4 molar ratio with the maleic acid or anhydride.

21. The method claimed in claim 20 wherein said copolymer has a molecular weight of about 30,000-1,000,000 and is present in amount of about 0.1-2% by weight.

22. The method claimed in claim 21 wherein the copolymer has an average molecular weight of about 70,000.

23. The method claimed in either of claims 1 or 2 wherein said oral composition contains an effective anticaries amount of a fluoride ion-providing source.
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