| 摘要 |
<p>A composition for reducing intraocular pressure and reducing the formation of aqueous humour by application to the cornea, in topical form, of an effective quantity of an aqueous solution of carbonic anhydrase inhibitor which includes a sulphonamide having the following properties: a. either a pKa of more than 7.0, but not above 7.3, or sufficiently soluble in water to form at least a 3 mM solution with a pH of 8.2, but not sufficiently soluble to form a solution of 1% by weight, b. or an ether partition coefficient of at least 1.0, c. a chloroform partition coefficient of at least 0.01, d. a dissociation constant with respect to carbonic anhydrase of more than 3 x 10-8 molar, e. a first order rate constant for penetration of the sulphonamide through live rabbit cornea of at least 0.005 hour -1, f. which is not harmful to the cornea, and g. which is stable in aqueous solution and in contact with the cornea is described.</p> |
