Otsuka Pharmaceutical Company, Limited

Yoshinao Onishi

Yoshihiro Nishioka

Shigekazu Fujita

Shinji Aki

Shun-ichiro Sumida

Shinichi Ishikawa

Shun-Ichiro Sumida

Disclosed is a technique for preventing the decomposition of latanoprost (a thermally unstable substance) contained in an eye-drop solution to stabilize the eye-drop solution. Specifically disclosed is an eye-drop preparation comprising latanoprost and carteolol hydrochloride. By adding carteolol hydrochloride to an eye-drop solution containing latanoprost which is a thermally unstable substance and is likely to be adhered on the surface of a container, it becomes possible to prevent the decomposition of latanoprost in the eye-drop solution and also prevent the loss of latanoprost caused by the adsorption of latanoprost on the surface of a container.

Eye-drop preparation and use thereof

The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects. 

Amine salt of carbostyril derivative

The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double H bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects. 

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Tokushima, Japan

Yoshinao Onishi