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Details for Patent: 5,292,526

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Details for Patent: 5,292,526

Title: Antibacterial antiplaque anticalculus oral composition
Abstract:An oral composition such as a dentifrice, mouthwash, lozenge or chewing gum containing a polyphosphate anticalculus agent, such as tetraalkali metal pyrophosphate and antibacterial antiplaque agent compatible therewith. The antiplaque agent is a substantially water-insoluble noncationic antibacterial agent such as 2,4,4'-trichloro-2'-hydroxydiphenyl ether (Triclosan). Antiplaque effectiveness is optimized by the presence of 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 Co. (New York, NY)
Filing Date:Oct 23, 1992
Application Number:07/966,104
Claims:1. An oral composition comprising an orally acceptable aqueous-humectant dentifrice or toothpaste vehicle, a dentally acceptable water-insoluble polishing agent, a water-soluble or swellable anti-bacterial enhancing agent which is effective to enhance the anti-bacterial effect of a substantially water-insoluble non-cationic antibacterial 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, and an effective anticalculus amount of a linear molecularly dehydrated polyphosphate, wherein the polyphosphate is present in amount such that the weight ratio of polyphosphate ion to anti-bacterial agent ranges from in excess of 0.72:1 to less than 4:1 said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "A.E.A", or antibacterial enhancing agent incrementally, to a clear solution micro-emulsion of said antibacterial agent typically dissolved in admixtures of humectant and surface active agent, until the solution becomes cloudy, and may be characterized as a macroemulsion.

2. An oral composition comprising an orally acceptable aqueous-humectant dentifrice or toothpaste vehicle, a dentally acceptable water-insoluble polishing agent, a water-insoluble or swellable anti-bacterial-enhancing agent which is effective to enhance the anti-bacterial effect of a substantially water-insoluble non-cationic antibacterial 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, the said composition containing a mixture of potassium and sodium salts at least one of which is present in an effective anticalculus amount as a polyphosphate anticalculus agent, the ratio of potassium to sodium in the said composition being in the range of up to less than 3:1 said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "A.E.A", or antibacterial enhancing agent incrementally, to a clear solution micro-emulsion of said antibacterial agent typically dissolved in admixtures of humectant and surface active agent, until the solution becomes cloudy, and may be characterized as a macroemulsion.

3. An oral composition comprising an orally acceptable aqueous-humectant dentifrice or toothpaste vehicle, a dentally acceptable water-insoluble polishing agent, substantially water insoluble non-cationic anti-bacterial agent in an amount which retards the oral growth of plaque of from 0.25% to less than 0.5% by weight and a water-soluble or swellable anti-bacterial-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 said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "A.E.A", or antibacterial enhancing agent incrementally, to a clear solution micro-emulsion of said antibacterial agent typically dissolved in admixtures of humectant and surface active agent, until the solution becomes cloudy, and may be characterized as a macroemulsion.

4. An oral composition comprising an orally acceptable aqueous-humectant dentifrice or toothpaste vehicle, a dentally acceptable water-insoluble polishing agent, a substantially water insoluble non-cationic anti-bacterial agent, in an amount which retards the oral growth of plaque of from 0.25% to 0.35% and 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 said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "A.E.A", or antibacterial enhancing agent incrementally, to a clear solution micro-emulsion of said antibacterial agent typically dissolved in admixtures of humectant and surface active agent, until the solution becomes cloudy, and may be characterized as a macroemulsion.

5. An oral composition comprising an orally acceptable aqueous-humectant dentifrice or toothpaste vehicle, a dentally acceptable water-insoluble siliceous polishing agent, about 0.25% to less than 0.5% by weight 9 f a substantially water-insoluble non-cationic anti-bacterial agent to retard oral growth of plaque and a water-soluble or swellable anti-bacterial-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 said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "A.E.A", or antibacterial enhancing agent incrementally, to a clear solution micro-emulsion of said antibacterial agent typically dissolved in admixtures of humectant and surface active agent, until the solution becomes cloudy, and may be characterized as a macroemulsion.

6. An oral composition comprising in an orally acceptable aqueous humectant dentifrice or toothpaste vehicle, a dentally acceptable water-insoluble polishing agent, an effective anticalculus amount of linear molecularly dehydrated polyphosphate salt anticalculus agent present in a mixture of sodium and potassium salts wherein the ratio of potassium to sodium in said composition is up to less than 3:1, and effective antiplaque amount to retard the oral growth of plaque of a substantially water insoluble non-cationic antibacterial agent and about 0.05-4% by weight of an 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 said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "A.E.A", or antibacterial enhancing agent incrementally, to a clear solution micro-emulsion of said antibacterial agent typically dissolved in admixtures of humectant and surface active agent, until the solution becomes cloudy, and may be characterized as a macroemulsion.

7. A composition according to claim 6 wherein the ratio of potassium to sodium is from 0.37:1 to 1.04:1.

8. An oral composition comprising an orally acceptable aqueous-humectant dentifrice or toothpaste vehicle, a dentally acceptable water-insoluble polishing agent, an effective amount of a linear, molecularly dehydrated polyphosphate, an effective amount to retard the growth of plaque in the range of about 0.01-5% by weight of a substantially water insoluble non-cationic antibacterial agent and about 0.05-4% by weight of 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 polyphosphate is present in an amount wherein the weight ratio of said antibacterial enhancing agent to said polyphosphate ion ranges from about 1:6 to about 2.7:1 said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "A.E.A", or antibacterial enhancing agent incrementally, to a clear solution micro-emulsion of said antibacterial agent typically dissolved in admixtures of humectant and surface active agent, until the solution becomes cloudy, and may be characterized as a macro-emulsion.

9. The oral composition claimed in claim 8 wherein said antibacterial agent is selected from the group consisting of halogenated diphenyl ethers, halogenated salicylanilides, benzoic esters, halogenated carbanilides and phenolic compounds.

10. The oral composition claimed in claim 9 wherein said antibacterial agent is a halogenated diphenyl ether.

11. The oral composition claimed in claim 10 wherein said halogenated diphenyl ether is 2,4,4'-trichloro-2'-hydroxyphenyl ether.

12. The oral composition claims in any of claims 8 to 11 wherein said amount of antibacterial agent is about 0.25-0.5%.

13. The oral composition claimed in any of claims 8 to 11 wherein said linear molecularly dehydrated polyphosphate salt is an alkali metal pyrophosphate.

14. The oral composition claimed in claim 13 wherein said alkali metal pyrophosphate is tetrasodium pyrophosphate.

15. The oral composition claimed in any of claims 8 to 11 wherein said polyphosphate is present in amount of about 1-2.5% by weight.

16. The oral composition claimed in any of claims 8 to 11 wherein the weight ratio of antibacterial enhancing agent to polyphosphate ion is about 1.7:1 to about 2.3:1.

17. The oral composition claimed in claim 16 wherein said weight ratio is about 1:9 to about 2:1.

18. The oral composition claimed in any of claims 8 to 11 wherein said vehicle comprises water, humectant and a gelling agent.

19. The oral composition according to any of claims 8 to 11 wherein said antibacterial-enhancing agent has an average molecular weight of about 100 to about 1,000,000.

20. The oral composition according to claim 19 wherein said delivery-enhancing group is acidic.

21. The oral composition according to claim 20 wherein said delivery-enhancing group is selected from the group consisting of carboxylic, phosphoric, phosphinic, and sulfonic acids, and 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, aryl, alkaryl, alkenyl, acyl, aralkyl, heterocyclic, or inert-substituted derivatives thereof, and n is zero or 1 or more and wherein said antibacterial-enhancing agent is a natural or synthetic 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.

22. The oral composition claimed in claim 21 wherein said antibacterial-enhancing agent is an anionic polymer containing a plurality of said delivery-enhancing and retention-enhancing groups.

23. The oral composition claimed in claim 22 wherein said anionic polymer comprises a chain containing repeating units each containing at least one carbon atom.

24. The oral composition claimed in claim 23 wherein the unit contains at least one delivery-enhancing group and at least one retention-enhancing group bonded to the same, vicinal, or other atoms in the chain.

25. The oral composition claimed in claim 24 wherein the delivery-enhancing group is a carboxylic group of salt thereof.

26. An oral composition comprising in an orally acceptable aqueous humectant dentifrice or toothpaste vehicle, a dentally acceptable water-insoluble polishing agent, an effective anticalculus amount of a linear molecularly dehydrated polyphosphate, an effective antiplaque amount of a substantially water insoluble noncationic antibacterial agent, in the range of about 0.01-5% by weight, and about 0.05-4% by weight of an anionic copolymer of maleic acid or anhydride with another ethylenically unsaturated polymerizable monomer, which copolymer enhances delivery and attachment, adherence or bonding of said antibacterial agent on oral tooth and gum surfaces, wherein said polyphosphate is present in amount wherein the weight ratio of said antibacterial enhancing agent to said polyphosphate ranges from about 1:6 to about 2.7:1 said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "A.E.A", or antibacterial enhancing agent incrementally, to a clear solution micro-emulsion of said antibacterial agent typically dissolved in admixtures of humectant and surface active agent, until the solution becomes cloudy, and may be characterized as a macroemulsion.

27. The oral composition claimed in claim 26 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.

28. The oral composition claimed in either of claims 26 or 27 wherein said copolymer has a molecular weight of about 30,000-1,000,000.

29. The oral composition claimed in claim 28 wherein the copolymer has an average molecular weight of about 70,000.

30. The oral composition claimed in any of claims 8 to 11 containing a fluoride-providing source.

31. The oral composition claimed in claim 1 wherein said weight ratio ranges from 1:1 to 3.5:1.

32. The oral composition claimed in claim 31 wherein said ratio ranges from about 1.6:1 to 2.7:1.

33. The oral composition claimed in claim 2 wherein said ratio is in the range from 0.37:1 to 1.04:1.
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