Pyridylaminoacetic acid compound and polyoxyethylene castor oil-containing pharmaceutical composition

Abstract

The purpose of the present invention is to provide: a pharmaceutical composition that comprises the pyridylaminoacetic acid compound of the present invention, said pyridylaminoacetic acid compound being stable within the pharmaceutical composition; and a method for improving the stability of the pydridylaminoacetic acid compound within the pharmaceutical composition. The pharmaceutical composition comprises: (6{[4-(pyrazol-1-yl)benzyl](pyridine-3-ylsulfonyl)aminomethyl}pyridine-2-ylamino)isopropyl acetate or a salt thereof; and polyoxyethylene castor oil. The polyoxyethylene castor oil preferably comprises a 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.

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 polyoxyethylene castor oil, wherein the content of the 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), and the polyoxyethylene castor oil is not polyoxyethylene hardened castor oil. 
     
     
         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 polyoxyethylene castor oil includes polyoxyl 35 castor oil. 
     
     
         4 . The pharmaceutical composition according to  claim 1 , wherein the content of the polyoxyethylene castor oil is in a range of 0.001 to 5% (w/v). 
     
     
         5 . The pharmaceutical composition according to  claim 1 , wherein the content of the polyoxyethylene castor oil is in a range of 0.5 to 3% (w/v). 
     
     
         6 . The pharmaceutical composition according to  claim 1 , wherein the content of the polyoxyethylene castor oil is in a range of 0.8 to 2% (w/v). 
     
     
         7 . The pharmaceutical composition according to  claim 1 , wherein the content of the polyoxyethylene castor oil is in a range of 1 to 20,000 parts by mass relative to 1 part by mass of the isopropyl 6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof. 
     
     
         8 . The pharmaceutical composition according to  claim 1 , wherein the content of the polyoxyethylene castor oil is in a range of 200 to 2,000 parts by mass relative to 1 part by mass of the 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 edetic acid or a salt thereof. 
     
     
         10 . 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. 
     
     
         11 . The pharmaceutical composition according to  claim 1 , which does not comprise sorbic acid. 
     
     
         12 . The pharmaceutical composition according to  claim 1 , which is filled into a container made of polyethylene. 
     
     
         13 . The pharmaceutical composition according to  claim 1 , for prevention or treatment of glaucoma or ocular hypertension, or for reduction of intraocular pressure. 
     
     
         14 . The pharmaceutical composition according to  claim 1 , which further comprises edetic acid or a salt thereof, and
 boric acid or a salt thereof, citric acid or a salt thereof, or acetic acid or a salt thereof, and glycerol, and   water,   wherein the pharmaceutical composition does not comprise sorbic acid, the polyoxyethylene castor oil includes polyoxyl 35 castor oil, and   the content of the polyoxyethylene castor oil is 0.5 to 3% (w/v) in the pharmaceutical composition.   
     
     
         15 . The pharmaceutical composition according to  claim 1 , which further comprises edetic acid or a salt thereof, and
 boric acid or a salt thereof, citric acid or a salt thereof, or acetic acid or a salt thereof, and glycerol, and   sodium hydroxide and/or hydrochloric acid, and   water,   wherein the pharmaceutical composition does not comprise sorbic acid,   the polyoxyethylene castor oil includes polyoxyl 35 castor oil, and   the content of the polyoxyethylene castor oil is 0.5 to 3% (w/v) in the pharmaceutical composition.   
     
     
         16 . The pharmaceutical composition according to  claim 1 , which further comprises edetic acid or a salt thereof, and
 boric acid or a salt thereof, citric acid or a salt thereof, or acetic acid or a salt thereof, and glycerol, and   benzalkonium chloride, and   water, wherein the pharmaceutical composition does not comprise sorbic acid,   the polyoxyethylene castor oil includes polyoxyl 35 castor oil, and   the content of the polyoxyethylene castor oil is 0.5 to 3% (w/v) in the pharmaceutical composition.   
     
     
         17 . The pharmaceutical composition according to  claim 1 , which further comprises edetic acid or a salt thereof, and
 boric acid or a salt thereof, citric acid or a salt thereof, or acetic acid or a salt thereof, and glycerol, and   benzalkonium chloride, and   sodium hydroxide and/or hydrochloric acid, and   water,   wherein the pharmaceutical composition does not comprise sorbic acid, the polyoxyethylene castor oil includes polyoxyl 35 castor oil, and   the content of the polyoxyethylene castor oil is 0.5 to 3% (w/v) in the pharmaceutical composition.