Use of borate-polyol complexes in ophthalmic compositions

• US 5,505,953 A
• Filed: 02/22/1994
• Issued: 04/09/1996
• Est. Priority Date: 05/06/1992
• Status: Expired due to Term

• Current Assignee: Alcon Research Limited (Nestle SA)
• Original Assignee: Alcon Laboratories Incorporated (Alcon Incorporated)
• Inventors: Chowhan, Masood
• Primary Examiner(s): Marquis, Melvyn I.
• Assistant Examiner(s): Hulina, Amy
• Application Number:
  US08/198,427
• Time in Patent Office: 777 Days
• Field of Search: 424/78.04, 424/659, 424/660, 424/427, 514/839, 514/915
• US Class Current: 424/427
• 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. A method of preparing an aqueous ophthalmic composition, comprising the steps of preparing a water-soluble borate-polyol complex by mixing borate and a polyol together in an aqueous solvent and adding polyvinyl alcohol thereto, wherein the borate-polyol complex is present at a concentration of 0.5 to 6.0 wt % and the molar ratio of borate to polyol is 1:

0.1 to 1;

10.

2. The method of claim 1, wherein the water-soluble borate-polyol complex comprises borate and polyol in a molar ratio of 1:

0.25 to 1;

2.5.

3. The method of claim 1, wherein the concentration of the water-soluble borate-polyol complex in the final composition is 0.5 to 3.0 wt %.

4. The method of claim 3, wherein the concentration of the water-soluble borate-polyol complex in the final composition is 1.0 to 2.0 wt %.

5. The method of claim 1, wherein the water-soluble borate-polyol complex comprises a polyol selected from the group consisting of sugars, sugar alcohols and sugar acids.

6. The method of claim 5, wherein the polyol is selected from the group consisting of mannitol, glycerin, propylene glycol and sorbitol.

7. The method of claim 6, wherein the polyol is selected from the group consisting of mannitol and glycerin.

8. The method of claim 7, wherein the polyol is mannitol.