Pyridylaminoacetic acid compound and polyoxyethylene castor oil-containing pharmaceutical composition
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 method for stabilizing isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof, the method comprising preparing a pharmaceutical composition by combining (i) isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof as a sole active ingredient, (ii) citric acid or a salt thereof, (iii) polyoxyethylene castor oil, and (iv) glycerin, wherein
the content of the isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino) acetate or a salt thereof in the pharmaceutical composition is in a range of 0.001 to 0.003% (w/v),
the content of the citric acid or the salt thereof is in a range of 0.1 to 0.2% (w/v),
the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 0.1 to 3% (w/v),
the content of the glycerin is in a range of 2.2 to 3% (w/v),
the polyoxyethylene castor oil is not polyoxyethylene hardened castor oil,
a number of polymerization of ethylene oxide of the polyoxyethylene castor oil is in a range of 5 to 100, and
the pharmaceutical composition does not comprise sorbic acid.
2 . The method 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 method according to claim 2 , wherein the polyoxyethylene castor oil includes polyoxyl 35 castor oil.
4 . The method according to claim 1 , wherein the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 0.5 to 3% (w/v).
5 . The method according to claim 4 , wherein the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 0.8 to 2% (w/v).
6 . The method according to claim 1 , wherein the content of the polyoxyethylene castor oil in the pharmaceutical composition is in a range of 50 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.
7 . The method according to claim 6 , wherein the content of the polyoxyethylene castor oil in the pharmaceutical composition 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.
8 . The method according to claim 1 , wherein the pharmaceutical composition further comprises edetic acid or a salt thereof.
9 . The method according to claim 1 , wherein the pharmaceutical composition is filled into a container made of polyethylene.
10 . The method according to claim 1 , wherein the pharmaceutical composition is for prevention or treatment of glaucoma or ocular hypertension, or for reduction of intraocular pressure.