Antibacterial antiplaque, anticalculus oral composition

• US 5,686,064 A
• Filed: 01/28/1994
• Issued: 11/11/1997
• Est. Priority Date: 01/30/1987
• Status: Expired due to Fees

• Current Assignee: Colgate-Palmolive Company
• Original Assignee: Colgate-Palmolive Company
• Inventors: Gaffar, Abdul, Afflitto, John, Nabi, Nuran, Stringer, Orum
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US08/187,984
• Time in Patent Office: 1,383 Days
• Field of Search: 424/49-58
• US Class Current: 424/57
• CPC Class Codes: A61K 8/24 Phosphorous; Compounds thereof
• CPC Class Codes: A61K 8/347 Phenols
• CPC Class Codes: A61K 8/42 Amides
• CPC Class Codes: A61K 8/8164 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 a carboxyl radical, and containing at least one other carboxyl radical in the molecule, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers, e.g. poly (methyl vinyl ether-co-maleic anhydride)
• CPC Class Codes: A61Q 11/00 Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
• CPC Class Codes: Y10S 526/936 Physiological use, e.g. pharmaceutical, veterinary, dental

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.

Claims

1. An oral composition comprising an orally acceptable aqueous humectant dentifrice or toothpaste vehicle, a dentally acceptable polishing agent, an effective antiplaque amount to retard the oral growth of plaque of a substantially water insoluble non-cationic antibacterial agent in the range of about 0.001-5% by weight, about 0.05-4% by weight of an antibacterial-enhancing agent which contains at least one delivery-enhancing functional group and at least one retention-enhancing group, wherein said delivery-enhancing group is present to enhance delivery of a substantially water insoluble non-cationic antibacterial agent to oral tooth and gum surfaces and said retention-enhancing group is present to enhance attachment, adherence or bonding of the antibacterial agent on oral tooth and gum surfaces, the anti-bacterial-enhancing agent being free from or substantially free from water soluble alkali metal or ammonium synthetic anionic linear polymer polycarboxylate salt having a molecular weight of 1,000 to 1,000,000 and an effective anticalculus amount of linear molecularly dehydrated polyphosphate said dentifrice or toothpaste having an optimized antiplaque effectiveness by presentation of said non-cationic antibacterial agent in a macroemulsion formed by adding said "AEA", 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, 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 having an average molecular weight of about 100 to about 1,000,000, which contains at least one delivery-enhancing phosphonic 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 "AEA", 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. The oral composition claimed in claim 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 oral composition claimed in claim 2 wherein said antibacterial agent is a halogenated diphenyl ether.

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

6. The oral composition claimed in claim 2 wherein said antibacterial agent is a phenolic compound.

7. The oral composition claimed in claim 6 wherein said antibacterial agent is a phenolic compound selected from the group consisting of phenol, thymol, eugenol and 2,2'"'"'-methylene bis (4-chloro-6-bromophenol).

8. The oral composition claimed in claim 5 wherein said amount of antibacterial agent is about 0.25-0.5%.

9. The oral composition claimed in claim 5 wherein said linear molecularly dehydrated polyphosphate salt is an alkali metal pyrophosphate.

10. The oral composition claimed in claim 9 wherein said alkali metal pyrophosphate is tetrasodium pyrophosphate.

11. The oral composition claimed in claim 5 wherein said polyphosphate is present in mount of about 1-2.5% by weight.

12. The oral composition claimed in claim 5 wherein the weight ratio of antibacterial enhancing agent to polyphosphate ion is about 1.7:

1 to about 2.3;

1.

13. The oral composition claimed in claim 12 wherein said weight ratio is about 1:

9 to about 2;

1.

14. The oral composition claimed in claim 5 wherein said vehicle comprises water, humectant and a gelling agent, said oral composition contains a dentally acceptable water-insoluble polishing agent and is a dentifrice.

15. The oral composition claimed in claim 5 wherein said vehicle comprises water and a non-toxic alcohol and said oral composition is a mouthwash.

16. The oral composition claimed in claim 5 wherein said organic retention-enhancing group comprises a formula --(X)_n --R wherein X is O, N, S, SO, SO₂, 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 phosphonic monomer or phosphonic 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.

17. The oral composition claimed in claim 16 wherein said antibacterial-enhancing agent is poly (beta-styrenephosphonic acid), poly (alpha-strenephosphonic acid) polymer, or copolymer of either styrenephosphonic acid with the other or with another ethylenically unsaturated polymerizable monomer.

18. The oral composition claimed in claim 16 wherein said antibacterial enhancing agent has a molecular weight of about 1,000 to about 30,000.

19. The oral composition claimed in any of claims 2, 4, 5 and 8 to 18 containing a fluoride-providing source.