Use of borate-polyol complexes in ophthalmic compositions

• US 5,342,620 A
• Filed: 09/07/1993
• Issued: 08/30/1994
• 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): Page, Thurman K.
• Assistant Examiner(s): Hulina, Amy
• Application Number:
  US08/118,833
• Time in Patent Office: 357 Days
• Field of Search: 424/400, 424/427, 424/658, 424/659, 514/839, 514/840, 514/912, 514/915
• US Class Current: 424/422
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Aqueous ophthalmic compositions containing water-soluble borate-polyol complexes are useful in aqueous ophthalmic compositions containing polyvinyl alcohol. These compositions provide the benefits of a borate buffering system, such as enhanced antimicrobial activity, without the problems associated with the use of borate and pol, such as formation of borate-polyvinyl alcohol complexes which are water-insoluble.

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 a aqueous solvent and adding polyvinyl alcohol thereto, wherein the water-soluble borate-polyol complex is present at a concentration between about 0.5 to about 6.0 wt %.

2. An aqueous ophthalmic composition prepared in accordance with the method of claim 1, comprising polyvinyl alcohol and a water-soluble borate-polyol complex, wherein the water-soluble borate-polyol complex is present at a concentration between about 0.5 to about 6.0 wt %.

3. The aqueous composition of claim 2, wherein the water-soluble borate-polyol complex comprises borate and polyol in a molar ratio between about 1:

1 and about 1;

10.

4. The aqueous composition of claim 2, wherein the water-soluble borate-polyol complex is present at a concentration between about 1.0 and about 2.5 wt %.

5. The aqueous composition of claim 2, wherein the water-soluble borate-polyol complex comprises a polyol selected from the group consisting of sugars, sugar alcohols and sugar acids.

6. The aqueous composition of claim 3, wherein the polyol is selected from the group consisting of mannitol, glycerin, propylene glycol and sorbitol.

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

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

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

1 and about 1;

10.

10. The method of claim 1, wherein the concentration of the water-soluble borate-polyol complex in the final composition is between about 0.5 and about 0.3 wt %.

11. The method of claim 10, wherein the concentration of the water-soluble borate-polyol complex in the final composition is between about 1.0 and about 2.0 wt %.

12. 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.

13. The method of claim 12, wherein the polyol is selected from the group consisting of mannitol, glycerin, propylene glycol and sorbitol.

14. The method of claim 13, wherein the polyol is selected from the group consisting of mannitol and glycerin.

15. The method of claim 14, wherein the polyol is mannitol.