Ophthalmic solution comprising Diquafosol

Patent metadata

Field	Value
Publication number	US-11166974-B2
Application number	US-202016819974-A
Country	US
Kind code	B2
Filing date	Mar 16, 2020
Priority date	Mar 26, 2012
Publication date	Nov 9, 2021
Grant date	Nov 9, 2021

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. An aqueous ophthalmic solution consisting of an active agent of diquafosol or a salt thereof at a concentration of 0.1 to 10% (w/v) a chelating agent at a concentration of 0.0001 to 1% (w/v) and optionally at least one distinct agent of a preservative, buffer agent, isotonizing agent or pH adjuster, wherein the solution is applicable to corneal epithelium disorder found in a dry-eye patient.

2. The ophthalmic solution according to claim 1 , wherein the chelating agent is at least one 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.

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

4. The ophthalmic solution according to claim 1 , wherein the chelating agent is a salt of edetic acid.

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

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

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

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

9. The ophthalmic solution according to claim 1 , wherein the chelating agent is a salt of edetic acid and 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.

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

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

• A61K47/183

  Amino acids, e.g. glycine, EDTA or aspartame · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• A61K31/7084 Primary

  Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide · CPC title

• A61P27/04

  Artificial tears; Irrigation solutions · CPC title