Pharmaceutical composition containing pyridylaminoacetic acid compound

Patent metadata

Field	Value
Publication number	US-10765750-B2
Application number	US-201916658585-A
Country	US
Kind code	B2
Filing date	Oct 21, 2019
Priority date	Jan 10, 2014
Publication date	Sep 8, 2020
Grant date	Sep 8, 2020

Abstract

The purpose of the present invention is to provide a pharmaceutical composition that comprises a specific compound and exhibits a superior preservation efficacy, the specific compound being stable within the pharmaceutical composition, and to provide methods for improving the stability of the specific compound within the pharmaceutical composition and the preservation efficacy of the pharmaceutical composition. The pharmaceutical composition according to the present invention comprises isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, and further comprises edetic acid or a salt thereof.

First claim

The invention claimed is:

1. A pharmaceutical composition comprising isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof and a nonionic surfactant, which further comprises edetic acid or a salt thereof,
wherein the nonionic surfactant includes polyoxyethylene castor oil,
wherein the pharmaceutical composition does not comprise sorbic acid;
wherein the content of the nonionic surfactant is in a range of 0.001 to 5% (w/v), and
wherein the content of the edetic acid or a salt thereof is in a range of 0.001 to 1% (w/v).

2. The pharmaceutical composition according to claim 1 , wherein the polyoxyethylene castor oil includes polyoxyethylene castor oil selected from the group consisting of polyoxyl 5 castor oil, polyoxyl 9 castor oil, polyoxyl 15 castor oil, polyoxyl 35 castor oil, and polyoxyl 40 castor oil.

3. The pharmaceutical composition according to claim 1 , wherein the content of the nonionic surfactant is in a range of 0.5 to 3% (w/v).

4. The pharmaceutical composition according to claim 1 , wherein the content of the nonionic surfactant is in a range of 1 to 20,000 parts by mass relative to 1 part by mass of isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof.

5. The pharmaceutical composition according to claim 1 , wherein the content of isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof is in a range of 0.0001 to 0.1% (w/v).

6. The pharmaceutical composition according to claim 5 , wherein the content of isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof is in a range of 0.001 to 0.003% (w/v).

7. The pharmaceutical composition according to claim 1 , wherein the content of edetic acid or a salt thereof is in a range of 0.01 to 0.1% (w/v).

8. The pharmaceutical composition according to claim 1 , wherein the content of edetic acid or a salt thereof is in a range of 0.1 to 1,000 parts by mass relative to 1 part by mass of isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof.

9. The pharmaceutical composition according to claim 1 , which further comprises boric acid or a salt thereof, citric acid or a salt thereof, or acetic acid or a salt thereof.

10. The pharmaceutical composition according to claim 1 , which is filled into a container made of polyethylene.

11. The pharmaceutical composition according to claim 1 , for prevention or treatment of glaucoma or ocular hypertension, or for reduction of intraocular pressure.

12. A method for stabilizing isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof comprising adding edetic acid or a salt thereof and polyoxyethylene castor oil into a pharmaceutical composition comprising isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof,
wherein the pharmaceutical composition does not comp rise sorbic acid,
wherein the content of the nonionic surfactant is in a range of 0.001 to 5% (w/v); and
wherein the content of the edetic acid or a salt thereof is in a range of 0.001 to 1% (w/v).

Assignees

• Santen Pharmaceutical Co Ltd

Inventors

• Endo Yoko

Classifications

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• A61K47/183 Primary

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

• A61K47/26

  Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin · CPC title

• A61K9/0048 Primary

  Eye, e.g. artificial tears · CPC title

• A61K47/02

  Inorganic compounds · CPC title