Process for reducing intraocular pressure

A - Human Necessities – 61 – K

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A61K 31/425 (2006.01) A61K 31/41 (2006.01) A61K 31/63 (2006.01) C07D 285/135 (2006.01)

Patent

CA 1193546

ABSTRACT OF THE DISCLOSURE Process and composition for reducing intraocular pressure and reducing aqueous humor formation by applying topically to the cornea an effective amount of an aqueous solution of a carbonic anhydrase inhibitor comprising a sulfonamide having the following properties: a. sufficiently soluble in water to form at least a 3mM solution at pH of 8.2 or pKa of not greater than 7.3; b. ether partition coefficient of at least 1.0; c. chloroform partition coefficient of at least 0.01; d. dissociation constant against carbonic anhydrase of not more than 3x10-8 molar; e. first order rate constant for penetration of the sulfonamide through a living rabbit cornea of at least 0.005 hr-1; f. not injurious to the cornea; and g. stable in aqueous solution and in contact with the cornea.

380546

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