Use of borate-polyol complexes in ophthalmic compositions

• US 6,365,636 B1
• Filed: 06/20/2000
• Issued: 04/02/2002
• Est. Priority Date: 05/06/1992
• Status: Expired due to Fees

• Current Assignee: Alcon Research Limited (Nestle SA)
• Original Assignee: Alcon Manufacturing Limited (Alcon Incorporated)
• Inventors: Dassanayake, Nissanke L., Chowhan, Masood
• Primary Examiner(s): Dudash, Diana
• Assistant Examiner(s): HAGHIGHATIAN, MINA
• Application Number:
  US09/597,310
• Time in Patent Office: 651 Days
• Field of Search: 422/28, 424/657, 424/658, 424/659, 424/660, 424/427, 424/422, 510/112, 514/840, 514/839, 514/912, 514/915, 514/772.3
• US Class Current: 514/64
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: Y10S 134/901 Contact lens

Abstract

Water-soluble borate-polyol complexes are useful as buffers and/or antimicrobials in aqueous ophthalmic compositions, including those containing polyvinyl alcohol. These compositions have greater antimicrobial activity than comparable compositions containing typical borate buffers and unexpectedly increase the antimicrobial efficacy of other antimicrobial agents when used in combination. In addition, use of the borate-polyol complexes avoids the incompatibility problem typically associated with the combination of borate buffer and polyvinyl alcohol; therefore, the compositions disclosed herein may also contain polyvinyl alcohol.

Claims

1. In a method of disinfecting a contact lens by means of soaking the lens in an aqueous disinfectant solution containing a disinfecting amount of an antimicrobial agent, the improvement which comprises including 0.5 to 6.0 wt % of a water-soluble borate-polyol complex in the disinfectant solution, said complex containing borate and polyol in a molar ratio of 1:

0.1 to 1;

10, whereby the antimicrobial activity of the disinfectant solution is enhanced.

2. A method according to claim 1, wherein the antimicrobial agent is selected from the group consisting of monomeric and polymeric quaternary ammonium compounds and their ophthalmically acceptable salts, monomeric and polymeric biguanides and their ophthalmically acceptable salts, and combinations thereof.

3. A method according to claim 2, wherein the borate-polyol complex is included in the composition in a concentration of 1.0 to 2.5 wt %, and the molar ratio of borate to polyol is 1:

0.25 to 1;

2.5.

4. A method according to claim 3, wherein the polyol is selected from the group consisting of mannitol, glycerin, propylene glycol and sorbitol.

5. A method according to claim 4, wherein the polyol is mannitol.

6. A method according to claim 5, wherein the antimicrobial agent comprises a polymeric quaternary ammonium compound.

7. A method according to claim 6, wherein the polymeric quaternary ammonium compound is polyquaternium-1.

8. A method according to claim 7, wherein the concentration of polyquaternium-1 in the composition is 0.001 wt %.

9. A method according to claim 2, wherein the antimicrobial agent comprises a polymeric biguanide.

10. A method according to claim 9, wherein the polymeric biguanide is polyhexamethylene biguanide.

11. A method according to claim 1, wherein the polyol is selected from the group consisting of mannitol, glycerin, propylene glycol and sorbitol.

12. A method according to claim 11, wherein the polyol comprises mannitol.

13. A method according to claim 11, wherein the polyol comprises glycerin.

14. A method according to claim 11, wherein the polyol comprises propylene glycol.

15. A method according to claim 11, wherein the polyol comprises sorbitol.

16. A method according to claim 15, wherein the antimicrobial agent comprises a polymeric quaternary ammonium compound.

17. A method according to claim 16, wherein the polymeric quaternary ammonium compound comprises polyquaternium-1.

18. A method according to claim 15, wherein the antimicrobial agent comprises a polymeric biguanide.

19. A method according to claim 18, wherein the polymeric biguanide comprises polyhexamethylene biguanide.

20. An aqueous solution for disinfecting contact lenses, comprising:

a disinfecting amount of an ophthalmically acceptable antimicrobial agent;

an amount of a borate-polyol complex sufficient to enhance the antimicrobial efficacy of the antimicrobial agent, said complex containing borate and polyol in a molar ratio of 1;

0.1 to 1;

10; and

water.

21. A solution according to claim 20, wherein the molar ratio of borate to polyol is 1:

0.25 to 1;

2.5.

22. A solution according to claim 20, wherein the polyol is mannitol.

23. A solution according to claim 20, wherein the antimicrobial agent is selected from the group consisting of polymeric quaternary ammonium compounds and polymeric biguanides.

24. A solution according to claim 23, wherein the antimicrobial agent is a polymeric quaternary ammonium compound.

25. A solution according to claim 24, wherein the polymeric quaternary ammonium compound is polyquaternium-1.

26. A solution according to claim 25, wherein the solution contains polyquaternium-1 in a concentration of 0.001 wt %.

27. A solution according to claim 20, wherein the antimicrobial agent is a polymeric biguanide.

28. A solution according to claim 27, wherein the polymeric biguanide is polyhexamethylene biguanide.