Ophthalmic delivery system

• US 5,776,445 A
• Filed: 08/07/1996
• Issued: 07/07/1998
• Est. Priority Date: 06/20/1994
• Status: Expired due to Fees

• Current Assignee: Smadar Cohen
• Original Assignee: Ben Gurion University of The Negev, Teva Pharmaceutical Industries Limited
• Inventors: Cohen, Smadar, Lobel, Esther
• Primary Examiner(s): AZPURU, CARLOS A
• Application Number:
  US08/689,218
• Time in Patent Office: 699 Days
• Field of Search: 424/78.04, 514/779, 514/912
• US Class Current: 424/78.04
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears

Abstract

The present invention relates to formulations particularly well suited for use as delivery systems in the delivery of an active agent to the eye. The formulations comprise an alginate having a particular proportion of guluronic acid.

Claims

1. An ophthalmic formulation comprising:

a therapeutically effective amount of at least one active agent, and 0.5 to 5 weight percent of a dissolved sodium alginate comprising at least 50% guluronic acid,

said sodium alginate undergoing a change from a dissolved phase to a gel phase upon contacting lacrimal fluid.

2. The ophthalmic formulation of claim 1, wherein the sodium alginate comprises at least 60% guluronic acid.

5. The ophthalmic formulation of claim 1, wherein the sodium alginate comprises from 50-95% guluronic acid and from 5-50% mannuronic acid.

6. The ophthalmic formulation of claim 1 wherein at least one of the active agents is a therapeutic agent for the eye.

7. The ophthalmic formulation of claim 1, wherein active agents are selected from the group consisting of:

a glaucoma agent, an anti-inflammatory agent, an anti-bacterial agent, an anti-viral agent and an anti-cataract agent.

8. The ophthalmic formulation of claim 1, wherein active agents are selected from the group consisting of:

a beta-adrenergic blocker, a cholinergic agent, an alpha-adrenergic agonist and a steriodal or a non-steroidal anti-inflammatory agent.

9. The ophthalmic formulation of claim 1, wherein active agents are selected from the group consisting of pilocaipine, acyclovir, epinephrine, ciprofloxacin, sodium chromoglycate, dexamethasone and timolol.

3. An ophthalmic formulation comprising:

a therapeutically effective amount of at least one active agent, and 0.5 to 5 weight percent of a dissolved sodium alginate whose composition comprises no more than 50% mannuronic acid, said sodium alginate undergoing a change from a dissolved phase to a gel phase upon contacting lacrimal fluid.

4. The ophthalmic formulation of claim 3, wherein the sodium alginate comprises no more than 40% mannuronic acid.

10. A method of treating diseases of the eye comprising:

administering a controlled release ophthalmic formulation to the eye, said ophthalmic formulation comprising;

a therapeutically effective amount of at least one active agent, and 0.5 to 5 weight percent of a dissolved sodium alginate comprising at least 50% guluronic acid, said sodium alginate undergoing a change from a dissolved phase to a gel phase after administering to the eye and contacting lacrimal fluid.

11. The method of claim 10, wherein the sodium alginate comprises at least 60% guluronic acid.

12. A method of treating diseases of the eye comprising:

administering a controlled release ophthalmic formulation to the eye, said ophthalmic formulation comprising;

0.5 to 5 weight percent of a dissolved sodium alginate comprising at least 50% guluronic acid, said sodium alginate undergoing a change from a dissolved phase to a gel phase after administering to the eye and contacting lacrimal fluid.