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Claims for Patent: 6,159,458

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Claims for Patent: 6,159,458

Title: Sustained release ophthalmic compositions containing water soluble medicaments
Abstract:An ophthalmic composition that provides sustained release of a water soluble medicament is formed comprising a crosslinked carboxy-containing polymer, a medicament, a sugar and water. The composition has a pH of at least 6.7 but a viscosity of from about 1000 to 5000 cps.
Inventor(s): Bowman; Lyle M. (Pleasanton, CA), Pfeiffer; James F. (Oakland, CA)
Assignee: InSite Vision (Alameda, CA)
Application Number:08/963,815
Patent Claims: 1. An ophthalmic composition comprising:

a pharmacologically effective amount of a water soluble ophthalmic medicament, about 0.5 to 2.0% crosslinked carboxy-containing polymer, about 0.5 to 5.0% sugar, and water; said composition having a pH of at least about 6.7 and a viscosity of from about 1000 to 5000 cps.

2. The composition according to claim 1, wherein said crosslinked carboxy-containing polymer comprises 0.6% to 0.9% of the composition.

3. The composition according to claim 1, wherein said polymer is a lightly crosslinked carboxy-containing polymer.

4. The composition according to claim 1, wherein the polymer is comprised of at least 90% acrylic acid monomers and 0.1% to 5% crosslinking agent.

5. The composition according to claim 4, wherein the crosslinking agent is a difunctional crosslinking agent.

6. The composition according to claim 4, wherein said crosslinking agent is selected from the group consisting of divinyl glycol, 2,3-dihydroxyhexa-1,5-diene, 2,5-dimethyl-1,5-hexadiene, divinylbenzene; N,N-diallylacrylamide, N,N-diallymethacrylamide, and mixtures thereof.

7. The composition according to claim 1, wherein said polymer is a polycarbophil.

8. The composition according to claim 1, wherein said polymer has a monodisperse particle size distribution.

9. The composition according to claim 1, wherein said medicament has a log partition coefficient value of 2.0 or greater.

10. The composition according to claim 9, wherein said medicament is a beta-blocker.

11. The composition according to claim 10, wherein said medicament is timolol or levobunolol.

12. The composition according to claim 10, wherein said medicament is contained in an amount of from about 0.005% to about 2.0% of said composition.

13. The composition according to claim 12, wherein medicament comprises 0.1% to 1.0% of said composition.

14. The composition according to claim 13, wherein said medicament is timolol maleate or levobunolol HCl.

15. The composition according to claim 1, further comprising EDTA.

16. The composition according to claim 15, wherein said EDTA comprises 0.09% to 0.11% of the composition.

17. The composition according to claim 1, further comprising benzalkonium chloride.

18. The composition according to claim 17, wherein said benzalkonium chloride comprises 0.005% to 0.015% of said composition.

19. The composition according to claim 1, wherein said pH is within the range of from 7.0 to 7.8.

20. The composition according to claim 1, wherein said composition has an osmolality of from 260 to 340 mOsM.

21. The composition according to claim 1, wherein said composition exhibits a medicament release profile such that no more than 60% of said medicament is released during the first hour after administration.

22. A method for treating an eye, which comprises administering to an eye in need thereof an effective amount of the composition according to claim 1.

23. An ophthalmic composition comprising:

(a) water, (b) a polymer component that consists essentially of one or more crosslinked carboxy-containing polymers, (c) sugar, and (c) timolol; wherein said composition has a pH of at least 7.0 and a viscosity of from about 1500 to 3500 cps.

24. The ophthalmic composition according to claim 23, wherein said timolol is present in the form of timolol maleate and in an amount of from 0.2% to 0.6% and wherein said pH is from 7.0 to 7.8.

25. The ophthalmic composition according to claim 23, wherein said composition exhibits a peak release of timolol no sooner than 30 minutes after administration of the composition.

26. The ophthalmic composition according to claim 25, wherein said peak release of timolol occurs 45 minutes or more after administration.
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