Ophthalmic compositions

• US 20040019130A1
• Filed: 07/29/2002
• Published: 01/29/2004
• Est. Priority Date: 07/29/2002
• Status: Active Grant

• Current Assignee: AST Products Incorporated, Ophthalmic Research Associates, Inc.
• Original Assignee: AST Products Incorporated, Ophthalmic Research Associates, Inc.
• Inventors: Su, Shih-Horng, Ousler, George W. III
• Granted Patent: US 6,806,364 B2
• Time in Patent Office: Days
• US Class Current: 523/105
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/717 Celluloses
• CPC Class Codes: A61K 33/14 Alkali metal chlorides; Alkaline earth metal chlorides
• CPC Class Codes: A61K 33/22 Boron compounds
• CPC Class Codes: A61K 33/30 Zinc; Compounds thereof
• CPC Class Codes: A61K 33/42 Phosphorus; Compounds thereof
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears

Abstract

An aqueous ophthalmic solution containing 0.2 to 2.5 percent by weight a polymeric demulcent, 0.045 to 0.065 percent by weight a calcium salt, and 0.14 to 1.4 percent by weight a phosphate salt. The solution has a viscosity of 20 to 150 centipoise and is buffered to a pH 5.5 to 8.5.

Claims

1. An aqueous ophthalmic solution, the solution comprising:

0.2 to 2.5 percent by weight a polymeric demulcent,

0.045 to 0.065 percent by weight a calcium salt, and

0.14 to 1.4 percent by weight a phosphate salt,

wherein the solution has a viscosity of 20 to 150 centipoise and is buffered to a pH 5.5 to 8.5.

2. The solution of claim 1, wherein the solution is buffered with a phosphate salt.

3. The solution of claim 2, wherein the concentration of the calcium salt is 0.05 to 0.06 percent by weight.

4. The solution of claim 3, wherein the concentration of the polymeric demulcent is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

5. The solution of claim 2, wherein the concentration of the calcium salt is 0.058 percent by weight.

6. The solution of claim 5, wherein the concentration of the polymeric demulcent is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

7. The solution of claim 2, further comprising 0.5 to 1.0 percent by weight glycerol or propyleneglycerol.

8. The solution of claim 2, further comprising 0.5 to 1.0 percent by weight glycerol.

9. The solution of claim 8, wherein the concentration of the calcium salt is 0.05 to 0.06 percent by weight.

10. The solution of claim 9, wherein the concentration of the polymeric demulcent is 0.5 to 0.8, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

11. The solution of claim 2, wherein the polymeric demulcent is a cellulosic polymer.

12. The solution of claim 11, wherein the concentration of the calcium salt is 0.05 to 0.06 percent by weight.

13. The solution of claim 12, wherein the concentration of the cellulosic polymer is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

14. The solution of claim 11, wherein the cellulosic polymer is hydroxy propylmethylcellulose.

15. The solution of claim 14, wherein the concentration of the calcium salt is 0.05 to 0.06 percent weight.

16. The solution of claim 15, wherein the concentration of the hydroxy propylmethylcellulose is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

17. The solution of claim 2, wherein the calcium salt is calcium chloride.

18. The solution of claim 17, wherein the concentration of the calcium chloride is 0.05 to 0.06 percent by weight.

19. The solution of claim 18, wherein the concentration of the polymeric demulcent is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

20. The solution of claim 17, wherein the concentration of calcium chloride is 0.058 percent by weight.

21. The solution of claim 20, wherein the concentration of the polymeric demulcent is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

22. The solution of claim 17, wherein the cellulosic polymer is a cellulosic polymer.

23. The solution of claim 22, further comprising 0.5 to 1.0 percent by weight glycerol.

24. The solution of claim 23, wherein the concentration of the calcium chloride is 0.05 to 0.06 percent by weight.

25. The solution of claim 24, wherein the concentration of the cellulosic polymer is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

26. The solution of claim 23, wherein the cellulosic polymer is hydroxypropyl methylcellulose.

27. The solution of claim 26, wherein the concentration of the calcium chloride is 0.058 percent by weight.

28. The solution of claim 27, wherein the concentration of the hydroxypropyl methylcellulose is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

29. The solution of claim 28, wherein the concentration of the hydroxypropyl methylcellulose is 0.6 percent by weight, the concentration of the phosphate salt is 0.6 to 0.8 percent by weight, and the solution has a viscosity of 70 centipoise and is buffered to a pH of 6.0 to 7.4.

30. The solution of claim 29, further comprising:

0.005 to 0.05 percent by weight glycine,

0.006 to 0.08 percent by weight sodium borate,

0.025 to 0.10 percent by weight magnesium chloride, and

0.001 to 0.01 percent by weight zinc chloride.

31. The solution of claim 1, wherein the polymeric demulcent is a cellulosic polymer.

32. The solution of claim 31, wherein the concentration of the calcium salt is 0.05 to 0.06 percent by weight.

33. The solution of claim 32, wherein the concentration of the cellulosic polymer is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

34. The solution of claim 33, further comprising 0.5 to 1.0 percent by weight glycerol.

35. The solution of claim 31, wherein the cellulosic polymer is hydroxypropyl methylcellulose.

36. The solution of claim 35, wherein the concentration of the calcium salt is 0.05 to 0.06 percent weight.

37. The solution of claim 36, wherein the concentration of the hydroxypropyl methylcellulose is 0.5 to 0.8 percent by weight, the concentration of the phosphate salt is 0.3 to 1.2 percent by weight, and the solution has a viscosity of 50 to 90 centipoise and is buffered to a pH of 6.0 to 8.0.

38. The solution of claim 37, further comprising 0.5 to 1.0 percent by weight glycerol.

39. A method for treating an eye, comprising administering to an eye in need thereof an effective amount of the solution of claim 1.

40. A method for treating an eye, comprising administering to an eye in need thereof an effective amount of the solution of claim 31.

41. A method for treating an eye, comprising administering to an eye in need thereof an effective amount of the solution of claim 34.

42. A method for treating an eye, comprising administering to an eye in need thereof an effective amount of the solution of claim 35.

43. A method for treating an eye, comprising administering to an eye in need thereof an effective amount of the solution of claim 38.