Ophthalmic solution comprising diquafosol

Patent metadata

Field	Value
Publication number	US-10071113-B2
Application number	US-201615289273-A
Country	US
Kind code	B2
Filing date	Oct 10, 2016
Priority date	Mar 26, 2012
Publication date	Sep 11, 2018
Grant date	Sep 11, 2018

Abstract

Regarding Diquafosol ophthalmic solution comprising a chelating agent at a concentration of 0.0001 to 1% (w/v), formation of insoluble precipitates found in Diquafosol ophthalmic solution during storage of the solution, as well as deterioration of the filtration performance in the course of production (course of filtration sterilization), have been inhibited. Further, in Diquafosol ophthalmic solution comprising a chelating agent, reduction of eye irritation and enhancement of the preservative effectiveness have been confirmed, in comparison to Diquafosol ophthalmic solution comprising no chelating agent. Accordingly, the present invention has been confirmed to provide physicochemical properties that are stable during the courses of production and distribution as well as the course of storage by a patient, and also reduce eye irritation and enhance preservative effectiveness.

First claim

The invention claimed is:

1. A method for treating dry eye comprising applying to corneal epithelium disorder found in a dry-eye patient an aqueous ophthalmic solution consisting of diquafosol or a salt thereof at a concentration of 0.1 to 10% (w/v) and a chelating agent at a concentration of 0.0001 to 1% (w/v) and optionally at least one other agent of a preservative, buffer agent, isotonizing agent, surfactant or pH adjuster, wherein the surfactant is selected from the group consisting of polyoxyl 40 stearate and polyoxyethylene hydrogenated castor oil, wherein the chelating agent is at least one type selected from the group consisting of edetic acid, citric acid, metaphosphoric acid, pyrophosphoric acid, polyphosphoric acid, malic acid, tartaric acid, phytic acid, and salts thereof.

2. The method according to claim 1 , wherein the chelating agent is at least one type selected from the group consisting of edetic acid, citric acid, metaphosphoric acid, polyphosphoric acid, and salts thereof.

3. The method according to claim 1 , wherein the chelating agent is a salt of edetic acid.

4. The method according to claim 1 , wherein the chelating agent is at a concentration of 0.0005 to 0.5% (w/v) in the ophthalmic solution.

5. The method according to claim 1 , wherein the chelating agent is at a concentration of 0.001 to 0.1% (w/v) in the ophthalmic solution.

6. The method according to claim 1 , wherein diquafosol or a salt thereof is at a concentration of 1 to 10% (w/v) in the ophthalmic solution.

7. The method according to claim 1 , wherein diquafosol or a salt thereof is at a concentration of 3% (w/v) in the ophthalmic solution.

8. The method according to claim 1 , wherein the chelating agent is a salt of edetic acid, the chelating agent is at a concentration of 0.001 to 0.1% (w/v) in the ophthalmic solution, and diquafosol or a salt thereof is at a concentration of 3% (w/v) in the ophthalmic solution.

9. The method according to claim 1 , wherein the ophthalmic solution contains the preservative.

10. The method according to claim 1 , wherein the buffer agent is at least one type selected from the group consisting of sodium phosphate, sodium hydrogen phosphate, sodium dihydrogen phosphate, sodium acetate, and epsilon aminocaproic acid.

11. The method according to claim 1 , wherein the isotonizing agent is at least one type selected from the group consisting of sodium chloride, potassium chloride, and concentrated glycerin.

Assignees

• Santen Pharmaceutical Co Ltd

Inventors

• Sakatani Akiko
• Ikei Tatsuo
• Inagaki Koji
• Nakamura Masatsugu
• Hosoi Kazuhiro
• Saito Mikiko
• Sonoda Masaki
• Fukui Yoko
• Kuwano Mitsuaki

Classifications

• A61P27/04

  Artificial tears; Irrigation solutions · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• A61K47/24

  containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title