TOPICAL ANTIGLAUCOMA COMPOSITION CONTAINING CARBONIC ANHYDRASE INHIBITOR AND BETA-BLACKER

摘要

PROBLEM TO BE SOLVED: To obtain the subject composition, capable of enhancing the compliance of a patient with no or slight adverse effects and effective in treating glaucoma and intraocular hypertension by including a -blocker and a carbonic anhydrase inhibitor (CAI) therein. SOLUTION: This composition is obtained by including one or more - blockers represented by formula I [R'1 is a (substituted)ring or a (substituted) aliphatic parts; R'2 and R'3 are each H or a (substituted)alkyl] and one or more carbonic anhydrase inhibitors represented by formula II [R1 is H, a 1-4C alkyl, OH, etc.; R2 is H, a 1-8C alkyl, OH, etc.; R3 is H, a halogen, a 1-4C alkyl, etc.; G is SO2 , C(=O), etc.] at (1:1) to (1:40) weight ratio. The composition is preferably an aqueous one and the pH thereof is 5.0-7.8. Furthermore, 0.05-2.0 wt.% anionic mucomimetic polymer having carboxylic acid functional groups or 0.05-10.0 wt.% drug transport substrate capable of selectively adsorbing or binding to a drug molecule or both can be contained in the composition in order to further sustain the release.