Antibacterial antiplaque oral composition

• US 5,538,715 A
• Filed: 12/03/1993
• Issued: 07/23/1996
• Est. Priority Date: 01/30/1987
• Status: Expired due to Fees

• Current Assignee: Colgate-Palmolive Company
• Original Assignee: Colgate-Palmolive Company
• Inventors: Nabi, Nuran, Gaffar, Abdul, Afflitto, John, Stringer, Orum
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US08/161,033
• Time in Patent Office: 963 Days
• Field of Search: 424/49-58
• US Class Current: 424/52
• CPC Class Codes: A61K 2800/87 Application Devices; Containers; Packaging
• 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 8/81 obtained by reactions involving only carbon-to-carbon unsaturated bonds
• 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: C08F 230/02 containing phosphorus

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 methy 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.

Claims

1. An oral composition dentifrice for attaching, adhering or bonding a plaque-inhibiting antibacterial agent to oral tooth and gum surfaces comprising in an orally acceptable aqueous humectant vehicle, about 5-30% by weight of a siliceous polishing agent, an effective antiplaque amount in the range of about 0.01-5% by weight of a 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 carboxylic delivery-enhancing functional group and at least one organic retention-enhancing functional group, which delivery-enhancing group enhances delivery of said antibacterial agent to oral tooth and gum surfaces and which retention-enhancing group enhances attachment, adherence or bonding of said antibacterial agent on oral tooth and gum surfaces, and 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, wherein (a) said oral composition dentifrice is free of polyphosphate anticalculus agent in an effective anticalculus amount and (b) said oral composition dentifrice does not contain polyethylene glycol which effectively inhibits the antibacterial activity of said non-cationic antibacterial agent.

6. The oral composition claimed in either of claim 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.

7. The oral composition claimed in claim 6, wherein said antibacterial agent is a halogenated diphenyl ether.

8. The oral composition claimed in claim 7, wherein said halogenated diphenyl ether is 2,4,4'"'"'-trichloro-2'"'"'-hydroxydiphenyl ether.

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

10. The oral composition claimed in claim 9, wherein said phenolic compound is selected from the group consisting of phenol, thymol, eugenol, and 2,2'"'"'-methylene bis(4-chloro-6-bromophenol).

11. The oral composition claimed in either of claim 1 or 2, wherein said antibacterial agent is present in amount of about 0.01-5% by weight.

12. The oral composition claimed in claim 11 wherein said antibacterial agent is present in amount of about 0.25-0.5%.

13. The oral composition dentifrice claimed in either of claim 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 12 carbon atoms, amyl acetate, ethyl acetate, glycerol tristearate and benzyl benzoate.

14. The oral composition dentifrice claimed in claim 13, wherein said solubilizing material is propylene glycol.

15. A composition according to any one of claims 1 to 5 containing an effective anticaries amount of a fluoride ion-providing source.

2. An oral composition dentifrice for attaching, adhering or bonding a plaque-inhibiting antibacterial agent to oral tooth and gum surfaces comprising an orally acceptable aqueous humectant vehicle, about 5-30% by weight of a siliceous polishing agent, an effective amount in the range of 0.01-5% by weight of a substantially water insoluble non-cationic antibacterial agent, an effective amount in the range of about 0.05-5% 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, and about 0.5-50% by weight of a solubilizing material for aid 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, wherein (a) said oral composition dentifrice is free of polyphosphate anticalculus agent in an effective anticalculus amount and (b) said oral composition dentifrice does not contain polyethylene glycol which effectively inhibits the oral antibacterial activity or said non-cationic antibacterial agent.

3. The oral composition according to claim 2, 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.

4. The oral composition according to claim 3, 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.

5. A composition according to claim 4, wherein the copolymer has an average molecular weight of about 70,000.

16. An oral composition dentifrice comprising in an orally acceptable aqueous humectant vehicle, about 5-30% of a siliceous polishing agent, about 0.01-5% of triclosan, about 0.05-5% of a copolymer of maleic acid or anhydride with methyl vinyl ether, and propylene glycol in amount sufficient to dissolve the triclosan in saliva.