WO2006053150B1 - Pharmaceutical compositions for topical application on the treatment of age-related macular degeneration and ocular hypertension - Google Patents

Abstract

A topically applied pharmaceutical composition for the prevention or treatment of age-related macular degeneration, ocular hypertension, glaucoma or any eye disease resulting from increase intraocular pressure, comprised of a solution of 17-β-estradiol suspended or dissolved in a vehicle, and the method of treatment using same.

Claims

AMENDED CLAIMS Received by the International Bureau on 07 July 2006 (07.07.2006)REPLACEMENT PAGE

1. A method for treating or preventing age-related macular degeneration comprising administering topically to an area in proximity to an eye a composition comprising an estrogen analogue selected from the group consisting of 17-β-estradiol, 17-β-estradiol glucuromide, 17-β- estradiol hemisuccinate, 17-β-estradiol phosphate, 17-β-estradiol sulfate and their salts and esters in a pharmaceutically acceptable vehicle.

2. The method of claim 1 , wherein said estrogen analogue is selected from 17-β-estradiol, and its salt, phosphate, and ester derivatives at the 3 position.

3. The method of claim 2, wherein said estrogen analogue is selected from 17-β-estradiol-3- phosphate, 17-β-estradiol-3-phosphate disodium salt, and 17-β-estradiol-3-sulfate.

4. The method of claim 3, wherein said estrogen analogue is selected from 17-β-estradiol-3- phosphate.

5. The method of claim 4, wherein said 17-β-estradiol-3 -phosphate comprises from about .001 to about 1.0 weight percent of said composition. REPLACEMENT PAGE

6. The method of claim 5, wherein the composition of said vehicle comprises, on a weight percent basis:

0.2 - 0.9% sodium chloride

0.05 - 1.0% anhydrous sodium phosphate

0.001 - 0.05% poloxamer NF

0.05 - 1.0% polyethylene glycol

0.05 - 1.0% disodium edetate

0.05 - 2.0% povidone

0.05 - 1.0% hydroxyethyl celluose NF

7. The method of claim 6, wherein said vehicle comprises, on a weight percent basis:

Dibasic sodium phosphate, USP 0.3 %

Sodium Chloride, USP 0.6%

Edetate disodium, USP 0.1%

Povidone, USP 0.37%

Poloxamer NF 0.004%

PEG 0.12%

Hydroxyethyl Cellulose NF 0.2%

Purified water, USP, q.s to 100%

HCl or NaOH to adjust pH to pH 6-8.

8. A method for treating or preventing ocular hypertension comprising administering topically to an area in proximity to an eye a composition comprising an estrogen analogue selected from the group consisting of 17-β-estradiol, 17-β-estradiol glucuromide, 17-β-estradiol hemisuccinate, 17-β-estradiol phosphate, 17-β-estradiol sulfate and their salts and esters in a pharmaceutically acceptable vehicle, comprising, on a weight percent basis:

0.2 - 0.9% sodium chloride

0.05 - 1.0% anhydrous sodium phosphate

0.001 - 0.05% poloxamer NF

0.05 - 1.0% polyethylene glycol

0.05 - 1.0% disodium edetate

0.05 - 2.0% povidone

0.05 - 1.0% hydroxyethyl celluose NF REPLACEMENT PAGE

9. The method of claim 8, wherein said estrogen analogue is selected from 17-β-estradiol-3- phosphate, 17-β-estradiol-3-phosphate disodium salt, and 17-β-estradiol-3-sμlfate.

10. The method of claim 9, wherein said estrogen analogue is 17-β-estradiol-3-phosphate.

11. The method of claim 10, wherein said vehicle comprises, on a weight percent basis:

Dibasic sodium phosphate, USP 0.3 %

Sodium Chloride, USP 0.6%

Edetate disodium, USP 0.1%

Povidone, USP 0.37% ^"

Poloxamer NF 0.004%

PEG 0.12%

Hydroxyethyl Cellulose NF 0.2%

Purified water, USP, q.s to 100%

HCl or NaOH to adjust pH to pH 6-8.