Enhanced bimatoprost ophthalmic solution

• US 8,309,605 B2
• Filed: 12/10/2010
• Issued: 11/13/2012
• 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
• Application Number:
  US12/965,514
• Publication Number:
  US 20110124737A1
• Time in Patent Office: 704 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 method of lowering elevated intraocular pressure in a patient with open-angle glaucoma or ocular hypertension which comprises applying to the eyes of the patient an aqueous solution comprised of:

about 0.01% w/v bimatoprost;

about 200 ppm benzalkonium chloride;

the solution having a pH of about 7.3;

a phosphate buffer; and

,

water.

2. The method of claim 1 wherein the bimatoprost is present in a concentration of 0.01% w/v and the phosphate buffer is dibasic sodium phosphate.

3. The method of claim 1 further comprising 0.03% EDTA.

4. The method of claims 1 or 2 wherein the patient applies the aqueous solution at least once a day.

5. The method of claim 4 wherein the patient applies the aqueous solution once a day.

6. A method of lowering intraocular pressure in a patient suffering from elevated intraocular pressure which comprises applying to the eyes of the patient an aqueous solution comprising:

0.01% w/v bimatoprost;

about 200 ppm benzalkonium chloride;

the solution having a pH of about 7.3;

a citric acid buffer; and

,

water.

7. The method of claim 6 wherein the method is applied to patients suffering from glaucoma.

8. The method of claim 6 wherein the citric acid buffer is present in a concentration of about 0.01% w/v.

9. The method of claim 6 wherein the method is applied once a day.

10. The method of claim 7 wherein the glaucoma is open angle glaucoma.

11. The method of claim 6 wherein the solution comprises 200 ppm benzalkonium chloride.

12. A method of treating glaucoma in a patient comprising the following steps:

applying at least once a day a formulation comprising;

about 0.01% w/v bimatoprost;

benzalkonium chloride in the amount of about 200 ppm;

at least one buffering agent selected from the group consisting of dibasic sodium phosphate heptahydrate, citric acid monohydrate and EDTA;

and wherein the formulation has a pH of about 7.3.

13. The method of claim 12 wherein the formulation is an aqueous solution.

14. The method of claim 12 wherein the buffering agent is dibasic sodium phosphate heptahydrate.

15. The method of claim 12 wherein the buffering agent is citric acid monohydrate.

16. The method of claim 12 wherein the buffering agent is EDTA.

17. The method of claim 13 further comprising purified water.

18. A method of lowering elevated intraocular pressure in a patient with open-angle glaucoma or ocular hypertension which comprises applying to the eyes of the patient an aqueous solution comprising:

0.01% w/v bimatoprost;

0.02% w/v benzalkonium chloride;

at least two buffering agents selected from the group consisting of dibasic sodium

phosphate heptahydrate, citric acid monohydrate and EDTA;

hydrochloric acid and sodium hydroxide to adjust the solution to a pH of about 7.3;

sodium chloride; and

,

purified water.

19. The method of claim 18 wherein one of the buffering agents is citric acid monohydrate.

20. The method of claim 18 wherein the solution is applied to the patient'"'"'s eyes at least once a day.

21. The method of claim 18 wherein one of the buffering agents is dibasic sodium phosphate heptahydrate.