# US 8,772,337 B2 · Preservative-free prostaglandin-based ophthalmic solution

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 8,772,337 B2
- Document ID: US8772337B2
- Status: Granted
- Kind: B2
- Application number: 12/666,778
- Filed: 2008-07-17
- Published: 2010-08-19
- Granted: 2014-07-08
- Earliest claimed: 2007-07-20
- Assignees: Laboratoires Thea
- Applicants: Frederic Pilotaz; Fabrice Mercier; Henri Chibret
- Inventors: Frederic Pilotaz; Fabrice Mercier; Henri Chibret
- Web page: https://patentgrep.com/patent/US8772337B2

## CPC

- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/5575: having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
- A61P 27/06: Antiglaucoma agents or miotics
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides an ophthalmic solution without an antimicrobial preservative. The solution includes as an active substance at least one prostaglandin and as a solubilizing agent, a surfactant, where the solubilizing agent is polyoxyl-15-hydroxystearate.

## Claims

### Claim 1

An ophthalmic solution without an antimicrobial preservative comprising as an active substance at least one prostaglandin and as a solubilizing agent, a surfactant wherein the solubilizing agent is polyoxyl-15-hydroxystearate.

### Claim 2 (depends on 1)

The solution according to claim 1, wherein the concentration of the solubilizing agent in the solution is between 1 and 20 g/l.

### Claim 3 (depends on 1)

The solution according to claim 1, wherein the prostaglandin concentration in the solution is between 0.02 and 1.5 g/l.

### Claim 4 (depends on 1)

The solution according to claim 1 wherein the prostaglandin is selected from the group consisting of 17-phenyl-13,14 dihydro trinor prostaglandin F2α isopropyl ester (latanoprost), 20-ethyl prostaglandin F2α, (+)-fluprostenol isopropyl ester (travoprost), 17-phenyl trinor prostaglandin F2α amide, 17-phenyl-13,14 dihydro trinor prostaglandin F2α ethyl amide (bimatoprost), tafluprost prostaglandin F2α ethanolamide, bimatoprost (free acid)-d4, bimatoprost-d4, latanoprost ethyl amide, 13,14 dihydro-15-keto-20-ethyl prostaglandin F2α (unoprostone), and 13,14 dihydro-15-keto-20-ethyl prostaglandin F2α isopropyl ester (unoprostone isopropyl ester).

### Claim 5 (depends on 1)

The solution according to claim 1, further comprising an antiglaucoma agent selected from the group consisting of beta-blockers, carbonic anhydrase inhibitors and alpha-adrenergic agonists.

### Claim 6 (depends on 5)

The solution according to claim 5, wherein the antiglaucoma agent forms between 0.1 and 0.5% by weight of the solution.

### Claim 7 (depends on 1)

The solution according to claim 1, further comprising an additive selected from the group consisting of isotonicity agents, antioxidants and buffer systems.

### Claim 8 (depends on 1)

A single-use or multi-dose vial produced in additive-free LDPE containing the ophthalmic solution of claim 1.

### Claim 9 (depends on 1)

A method of treating glaucoma, reducing intraocular pressure, or providing neuroprotection to retinal tissues in a human or animal in need thereof comprising administering to the human or animal a solution according to claim 1.

### Claim 10 (depends on 9)

A method according to claim 9, comprising administering to the human or animal, via the topical route, one drop per day of the solution into each eye.

### Claim 11 (depends on 1)

The solution according to claim 1, wherein the concentration of the solubilizing agent in the solution is between 2 and 10 g/l.

### Claim 12 (depends on 1)

A method of treating glaucoma in an eye of a human in need thereof comprising topically administering to the eye of the human an effective amount of the solution according to claim 1.

### Claim 13 (depends on 1)

A method of reducing intraocular pressure in an eye of a human in need thereof comprising topically administering to the eye of the human an effective amount of the solution according to claim 1.

### Claim 14 (depends on 1)

A method of providing neuroprotection to retinal tissues in an eye of a human in need thereof comprising topically administering to the eye of the human an effective amount of the solution according to claim 1.