Enhanced bimatoprost ophthalmic solution

• US 8,338,479 B2
• Filed: 01/09/2009
• Issued: 12/25/2012
• Est. Priority Date: 03/16/2005
• Status: Active Grant

• Current Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Original Assignee: Allergan, Inc. (Canada) (Abbvie Incorporated)
• Inventors: Chang, Chin-Ming, Chang, James N., Schiffman, Rhett M., Jordan, R. Scott, Chang-Lin, Joan-En
• Primary Examiner(s): FAY, ZOHREH A
• Application Number:
  US12/351,383
• Publication Number:
  US 20090149546A1
• Time in Patent Office: 1,446 Days
• Field of Search: 514/530, 514/573
• US Class Current: 514/530
• 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 for the treatment of elevated intraocular pressure comprising about 0.01% w/v bimatoprost and about 200 ppm benzalkonium chloride, at least one buffer and having a pH of about 7.3 wherein said composition is an aqueous liquid which is formulated for ophthalmic administration.

2. The composition of claim 1 wherein the composition is for the treatment of elevated intraocular pressure in patients suffering from glaucoma or ocular hypertension.

3. The composition of claim 1 wherein the concentration of benzalkonium chloride is 200 ppm.

4. The composition of claim 1 which consists essentially of about 0.01% w/v bimatoprost, about 200 ppm benzalkonium chloride, a phosphate buffer, NaCl, citric acid monohydrate, hydrochloric acid, sodium hydroxide and water.

5. The composition of claim 1 wherein the concentration of bimatoprost is 0.01% w/v and the composition is applied once a day.

6. The composition of claim 4 wherein the concentration of citric acid monohydrate is about 0.014% w/v.

7. The composition of claim 4 wherein the concentration of benzalkonium chloride is 200 ppm.

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

9. The composition of claim 1 which comprises about 0.01% w/v bimatoprost, about 200 ppm benzalkonium chloride, 0.014% w/v citric acid monohydrate, a phosphate buffer, and NaCl and having a pH of 7.3.

10. The composition of claim 1 which comprises 0.01 w/v bimatoprost, 200 ppm benzalkonium chloride, a phosphate buffer, NaCl, and water.

15. The composition of claim 1 comprising about 0.01% w/v bimatoprost, about 0.02% w/v benzalkonium chloride, about 0.26% w/v sodium phosphate dibasic heptahydrate, about 0.014% w/v citric acid monohydrate, about 0.8% w/v sodium chloride, and water.

11. A method comprising administering to a human suffering from glaucoma or intraocular hypertension a composition comprising about 0.01% w/v bimatoprost and about 200 ppm benzalkonium chloride, sodium phosphate dibasic, and having a pH of about 7.3.

12. The method of claim 11 wherein the composition comprises 0.01% w/v bimatoprost and is topically administered to an affected eye once a day.

13. The method of claim 11 wherein the composition further comprises about 0.26% w/v sodium phosphate dibasic.

14. The method of claim 11 wherein the composition further comprises NaCl.

16. The method of claim 11 further comprising citric acid monohydrate, about 0.8% w/v sodium chloride, and water.