# US 8,541,413 B2 · Sustained release eye drop formulations

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- Number: US 8,541,413 B2
- Document ID: US8541413B2
- Status: Granted
- Kind: B2
- Application number: 12/236,877
- Filed: 2008-09-24
- Published: 2009-05-28
- Granted: 2013-09-24
- Earliest claimed: 2004-10-01
- Assignees: Ramscor, Inc.
- Applicants: Vernon G. Wong; Louis L. Wood
- Inventors: Vernon G. Wong; Louis L. Wood
- Web page: https://patentgrep.com/patent/US8541413B2

## CPC

- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 38/13: Cyclosporins
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

This invention provides for biocompatible, biodegradable eye drop pharmaceutical formulations useful for the treatment of ocular indications. In particular, tocopherols and their esters of low water solubility, notably α-tocopheryl acetate, are exceptional vehicles for biocompatible, nonirritating topical eye drop formulations that provide sustained release of active agents.

## Claims

### Claim 1

A method of lowering intraocular pressure in a subject comprising the step of: administering to the eye of a subject in need thereof an eye drop formulation consisting of prostaglandin dissolved, dispersed or suspended in tocopheryl acetate; wherein the administration of a unit dose of a single eye drop has therapeutic effect for seven days and administration is repeated only once every seven days.

### Claim 2

A pharmaceutical eye drops formulation for lowering intraocular pressure consisting of timolol dissolved, dispersed or suspended in tocopheryl acetate; wherein a unit dosage of one drop provides sustained release of timolol for seven days.

### Claim 3

A method of lowering intraocular pressure in a subject comprising the step of: administering to the eye of a subject in need thereof an eye drop consisting of timolol dissolved, dispersed or suspended in tocopheryl acetate; and wherein the administration of a unit dose of a single drop has therapeutic effect for seven days and administration is repeated only once every seven days.

### Claim 4

A pharmaceutical eye drops formulation for lowering intraocular pressure consisting of prostaglandin dissolved, disperse or suspended in tocopheryl acetate; wherein a dosage unit of a single drop provides sustained release of said prostaglandin for seven days.

### Claim 5 (depends on 2)

A dosage dispensing container comprising the pharmaceutical eye drops formulation of claim 2.

### Claim 6 (depends on 4)

A dosage dispensing container comprising the pharmaceutical eye drops formulation of claim 4.