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Details for Patent: 5,188,821

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Details for Patent: 5,188,821

Title: Antibacterial antiplaque oral composition mouthwash or liquid dentifrice
Abstract:An oral composition mouthwash or liquid dentifrice containing an aqueous vehicle acceptable vehicle, a substantially water-insoluble noncationic antibacterial antiplaque agent, such as 2,4,4'-trichloro-2'-hydroxy-diphenyl ether (triclosan) and an antibacterial-enhancing agent which enhances delivery of said antibacterial agent to, and retention thereof on, oral surfaces.
Inventor(s): Gaffar; Abdul (Princeton, NJ), Nabi; Nuran (North Brunswick, NJ), Afflitto; John (Brookside, NJ), Stringer; Orum (Yardley, PA)
Assignee: Colgate-Palmolive Company (Piscataway, NJ)
Filing Date:Aug 28, 1989
Application Number:07/398,592
Claims:1. In a method of preparing an oral composition mouthwash or liquid 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 aqueous vehicle, an effective amount in the range of about 0.15-5% by weight of substantially water insoluble noncationic antibacterial agent and at least one of a surface active agent, a flavoring oil or a non-toxic alcohol, 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 said antibacterial agent on oral tooth and gum surfaces, wherein said oral composition is free of polyphosphate anticalculus agent in an effective anticalculus amount.

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 mouthwash or liquid dentifrice comprising an aqueous vehicle and 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 flavoring oil or a non-toxic alcohol, the improvement comprising 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 to oral tooth and gum surfaces, and said retention-enhancing agent 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 a halogenated diphenyl ether.

4. The method claimed in claim 3 wherein said halogenated diphenyl ether is 2,4,4'-trichloro-2'-hydroxydiphenyl ether.

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

6. The method claim in either of claims 1 or 2 wherein said composition is a mouthwash and said aqueous vehicle contains a non-toxic alcohol and the weight ratio of water to non-toxic is from about 1:1 to about 20:1.

7. The method claimed in claim 6 wherein said non-toxic alcohol is ethanol.

8. The method claimed in either of claims 1 or 2 wherein said surface active agent is present in amount of about 0.5-5% by weight.

9. The method claimed in either of claims 1 or 2 wherein said flavoring oil is present in amount of about 0.1-5% by weight.

10. 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.

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

12. The method according to claim 11 wherein said delivery-enhancing group is selected from the group consisting of carboxylic, phosphonic, phosphonic, 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 copolymers, graft copolymers and cross-linked polymers and monomers.

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

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

15. The method claimed in claim 14 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.

16. The method claimed in claim 12 wherein the delivery-enhancing group is a carboxylic group or salt thereof.

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

18. The method claimed in claim 17 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.

19. The method claimed in claim 18 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.

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

21. 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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