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Details for Patent: 5,192,530

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Details for Patent: 5,192,530

Title: Antibacterial antiplaque oral composition
Abstract:An oral composition dentifrice comprising an orally acceptable vehicle, about 5-30% by weight of a siliceous polishing agent, a substantially water-insoluble noncationic antibacterial antiplaque agent, such as 2,4,4'-trichloro-2'-hydroxydiphenyl ether (triclosan), and an antibacterial-enhancing agent which enhances the delivery of said antibacterial agent to, and retention thereof on, oral surfaces, wherein said antiplaque agent is substantially completely dissolved in saliva present during tooth and gum cleaning in a solubilizing agent therefor. The solubilizing agent may be a humectant polyol such as propylene glycol, dipropylene glycol and hexylene glycol; a cellosolve such as methyl cellosolve and ethyl cellosolve; a vegetable oil or wax containing at least about 12 carbon atoms in a straight chain such as olive oil, castor oil and petrolatum; or an ester such as ethyl acetate, amyl acetate, glyceryl tristearate and benzyl benzoate.
Inventor(s): Gaffar; Abdul (Princeton, NJ), Nabi; Nuran (No. Brunswick, NJ), Afflitto; John (Brookside, NJ), Stringer; Orum (Yardley, PA)
Assignee: Colgate-Palmolive Company (New York, NY)
Filing Date:Sep 06, 1991
Application Number:07/754,887
Claims:1. In a method of preparing an oral composition dentifrice wherein delivery and retention of a plaque-inhibiting antibacterial agent is enhanced by attaching, adhering or bonding to oral tooth and gum surfaces, comprising an orally acceptable aqueous vehicle, about 5-30% by weight of a siliceous polishing agent and an effective amount in the range of about 0.01-5% by weight of substantially water insoluble noncationic antibacterial agent, the improvement comprising employing in said composition about 0.5-50% by weight of a solubilizing material for said antibacterial agent in amount sufficient to dissolve said antibacterial agent in saliva and permit delivery of said antibacterial agent to soft oral tissues at or near the gum line, and about 0.05-5% 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 to 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.

2. In method of attaching, adhering or bonding a plaque-inhibiting antibacterial agent to oral tooth and gum surfaces comprising applying to oral tooth and gum surfaces comprising applying to oral surfaces an oral composition dentifrice comprising an orally acceptable aqueous vehicle, about 5-30% by weight of a siliceous polishing agent, an effective amount in the range of about 0.01-5% by weight of substantially water insoluble noncationic antibacterial agent, the improvement which comprises employing in said composition about 0.5-50% by weight of a solubilizing material for said antibacterial gent in amount sufficient to dissolve said antibacterial agent in saliva and permit delivery of said antibacterial agent to soft oral tissues at or near the gum line and an effective amount in the range of about 0.05-5% by weight of an 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 to 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.

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 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 solubilizing material is selected from the group consisting of propylene glycol, dipropylene glycol, hexylene glycol, methyl cellosolve, ethyl cellosolve, vegetable oil and wax containing at least about 12 carbon atoms, amyl acetate, ethyl acetate, glycerol tristearate and benzyl benzoate.

8. The method claimed in claim 7 wherein said solubilizing agent is propylene glycol.

9. 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.

10. The method claimed in claim 9 wherein said delivery enhancing group is acidic.

11. The method according to claim 10 wherein said delivery-enhancing group is selected form the group consisting of carboxylic, phosphonic, phosphinic, and sulfonic acids, and their salts, and mixtures thereof and wherein said organic 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 copolymers, graft copolymers and cross-linked polymers and monomers.

12. The method claimed in claim 11 wherein said antibacterial-enhancing agent is an anionic polymer containing a plurality of said delivery-enhancing and retention-enhancing groups.

13. The method claimed in claim 12 wherein said anionic polymer comprising a chain containing repeating units each containing at least one carbon atom.

14. The method claimed in claim 13 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.

15. The method claimed in claim 11 wherein the delivery-enhancing group is a carboxylic group or salt thereof.

16. The method claimed in claim 15 wherein the antibacterial-enhancing agent is a copolymer of maleic acid or anhydride with another ethylenically unsaturated polymerizable monomer.

17. The method claimed in claim 16 wherein said other monomer of said copolymer is methyl vinyl ether in a 4:1 to 1:4 molar ratio with the maleic acid or anhydride.

18. The method claimed in claim 17 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.

19. The method claimed in claim 18 wherein the copolymer has an average molecular weight of about 70,000.

20. 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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