.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 5,180,578

« Back to Dashboard

Details for Patent: 5,180,578

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 Company (Piscataway, NJ)
Filing Date:Feb 19, 1991
Application Number:07/657,885
Claims:1. In a method of preparing an oral composition wherein delivery and retention of a plaque-inhibiting antibacterial agent is enhanced by attaching, adhering or bonding to oral surfaces comprising an orally acceptable aqueous vehicle, an effective amount in the range of about 0.01-5% by weight of substantially water insoluble noncationic antibacterial agent and polyphosphate anticalculus amount in an effective anticalculus amount present as a mixture of potassium and sodium salts, the improvement comprising employing potassium and sodium in said composition in a ratio of up to less than 1:1 and employing about 0.5-5% 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 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.

2. In a method of attaching, adhering or bonding a plaque-inhibiting antibacterial agent to oral tooth and gum surfaces which comprises applying on oral surfaces an oral composition comprising an orally acceptable aqueous vehicle, an effective amount in the range of about 0.01-5% by weight of substantially water insoluble noncationic antibacterial agent and polyphosphate anticalculus amount in an effective anticalculus amount present as a mixture of potassium and sodium salts, the improvement comprising employing potassium and sodium in said composition in a ratio of up to less than 1:1 and employing 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.

3. A method according to either of claims 1 or 2 wherein the ratio of potassium to sodium is from 0.37:1 to 1.04:1.

4. In a method of preparing an oral composition wherein delivery and retention of a plaque-inhibiting antibacterial agent is enhanced by attaching adhering or bonding to oral surfaces comprising an orally acceptable aqueous vehicle and an effective amount in the range of about 0.01-5% by weight of substantially water insoluble noncationic antibacterial agent the polyphosphate anticalculus agent about 0.5-4% 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 and employing said polyphosphate 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.

5. In a method of attaching, adhering or bonding a plaque-inhibiting antibacterial amount of an antibacterial agent comprising applying to oral surfaces an oral composition comprising an orally acceptable aqueous vehicle and an effective amount in the range of about 0.1-5% by weight of substantially water insoluble noncationic antibacterial agent, the improvement comprising employing polyphosphate anticalculus agent, and 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 and wherein said polyphosphate is 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.

6. The method claimed in either of claims 4 or 5 wherein said antibacterial agent is a halogenated diphenyl ether.

7. The method claimed in claim 6 wherein said halogenated diphenyl ether is 2,4,4'-trichloro-2'-hydroxydiphenyl ether.

8. The method claimed in either of claims 4 or 5 wherein said amount of antibacterial agent is about 0.25-0.5%.

9. The method according to either of claims 4 and 5 wherein said linear molecularly dehydrated polyphosphate salt is an alkali metal pyrophosphate.

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

11. The method according to either of claims 4 or 5 wherein said polyphosphate is present in amount of about 1-2.5% by weight.

12. The method according to either of claims 4 or 5 wherein the weight ratio of antibacterial enhancing agent to polyphosphate ion is about 1.7:1 to about 2.3:1.

13. The method claimed in claim 12 wherein said weight ratio is about 1:9 to about 2:1.

14. The method according to either of claims 4 or 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 dentrifrice.

15. The method claimed in either of claims 4 or 5 wherein said antibacterial-enhancing agent has an average molecular weight of about 100 to about 1,000,000.

16. The method claimed in claim 15 wherein said delivery enhancing group is acidic.

17. The method according to claim 16 wherein said delivery-enhancing group is selected from the group consisting of carboxylic, phosphonic, phosphinic, and sulfonic acids, and their salts, and mixtures thereof and wherein said antibacterial-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, inomomers, block copolymers, graft copolymers and cross-linked polymers and monomers.

18. The method claimed in claim 17 wherein said antibacterial-enhancing agent is na anionic polymer containing a plurality of said delivery-enhancing and retention-enhancing groups.

19. The method claimed in claim 18 wherein said anionic polymer comprising a chain containing repeating units each containing at least one carbon atom.

20. The method claimed in claim 19 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.

21. The method claimed in claim 17 wherein the delivery-enhancing group is a carboxylic group or salt thereof.

22. The method claimed in claim 21 wherein the antibacterial-enhancing agent is a copolymer of maleic acid or anhydride with another ethylenically unsaturated polymerizable monomer.

23. The method claimed in claim 22 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.

24. The method claimed in claim 23 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.

25. The method claimed in claim 24 wherein the copolymer has an average molecular weight of about 70,000.

26. The method claimed in either of claims 4 or 5 wherein said oral composition contains an effective anticaries amount of a fluoride ion-providing source.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc