Enhanced Bimatoprost Ophthalmic Solution

• US 20090149546A1
• Filed: 01/09/2009
• Published: 06/11/2009
• Est. Priority Date: 03/16/2005
• Status: Active Grant

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Jordan, R Scott, Chang, Chin-Ming, Schiffman, Rhett M., Chang-Lin, Joan-En, Chang, James N.
• Granted Patent: US 8,338,479 B2
• Time in Patent Office: Days
• US Class Current: 514/622
• CPC Class Codes: A01N 33/12 Quaternary ammonium compounds
• CPC Class Codes: A61K 31/14 Quaternary ammonium compounds, e.g. edrophonium, choline betaines A61K31/205
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/557 Eicosanoids, e.g. leukotrienes or prostaglandins
• CPC Class Codes: A61K 31/5575 having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: A61P 27/14 Decongestants or antiallergics

Abstract

A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein.

A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein.

Claims

1. A composition comprising from 0.01% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration.

2. The composition of claim 1 which further comprises an effective amount of EDTA.

3. The composition of claim 2 wherein the concentration of benzalkonium chloride is from 150 ppm to 200 ppm.

4. The composition of claim 3 having a pH of 7.4 which consists essentially of 0.015% bimatoprost, 200 ppm benzalkonium chloride, from 0 to 0.03% EDTA, a phosphate buffer, NaCl, and water.

5. The composition of claim 1 wherein the concentration of bimatoprost is from 0.01%.

6. The composition of claim 5 wherein the concentration of bimatoprost is from 0.015% to 0.02%.

7. The composition of claim 6 wherein the concentration of benzalkonium chloride is from 150 ppm to 200 ppm.

8. The composition of claim 7 wherein the concentration of benzalkonium chloride is 200 ppm.

9. The composition of claim 6 which further comprises an effective amount of EDTA.

10. The composition of claim 9 having a pH of 7.4 which comprises 0.015% bimatoprost, 200 ppm benzalkonium chloride, from 0 to 0.03% EDTA, a phosphate buffer, and NaCl.

11. The composition of claim 10 having a pH of 7.4 which consists of 0.015% bimatoprost, 200 ppm benzalkonium chloride, from 0 to 0.03% EDTA, a phosphate buffer, NaCl, and water.

16. The composition of claim 2 comprising from 150 to 250 ppm BAK.

17. The composition of claim 5 comprising 0.01% bitmatoprost, 0.02% benzalkonium chloride, 0.268% sodium phosphate dibasic heptahydrate, 0.014% citric acid monohydrate, 0.81% sodium chloride, sufficient sodium hydride and/or hydrochloric acid to adjust the pH to 7.3, and water.

12. A method comprising administering to a mammal suffering from glaucoma or intraocular hypertension a composition comprising from 0.01% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride.

13. The method of claim 12 comprising from 0.15% to 0.02% bitmatoprost.

14. The method of claim 12 comprising 0.01% bitmatoprost.

15. The method of claim 14 comprising from 0.01% to 0.05% EDTA.