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Claims for Patent: 4,619,939

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Claims for Patent: 4,619,939

Title: Process for reducing intraocular pressure
Abstract: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 caronic anhydrase inhibitor comprising a sulfonamide having the following properties: a. sufficiently soluble in water to form at least a 3 mM solution at pH 8.2 or a 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 3.times.10.sup.-8 molar; e. first order rate constant for penetration of the sulfonamide through a living rabbit cornea of at least 0.005 hr.sup.-1 ; f. not injurious to the cornea; and g. stable in aqueous solution and in contact with the cornea.
Inventor(s): Maren; Thomas H. (Gainesville, FL)
Assignee: University of Florida (Gainesville, FL)
Application Number:06/729,907
Patent Claims: 1. A method for reducing aqueous humor formation and intraocular pressure consisting of topically applying to the cornea an amount of an aqueous solution of from about 0.1% to about 5%, by weight, of a carbonic anhydrase inhibitor and for a time sufficient to effect a reduction of aqueous humor formation and intraocular pressure, wherein said carbonic anhydrase inhibitor is a pharmaceutically acceptable sulfonamide having the following properties:

(a) sufficiently water soluble to form at least a 3 mM solution at pH 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 3.times.10.sup.-8 molar;

(e) first order rate constant for penetration of said sulfonamide through a living rabbit cornea of at least 0.005 hr.sup.-1 ;

(f) not injurious to the cornea; and

(g) stable in solution and in contact with the cornea.

2. The process of claim 1 wherein said sulfonamide is a heterocyclic sulfonamide.

3. The process of claim 1 wherein said sulfonamide is a thiadiazoline sulfonamide.

4. The process of claim 1 wherein the intraocular pressure is reduced at least 4 mm. Hg and the reduction of aqueous humor formation is 30-80%.

5. The process of claim 2 wherein said sulfonamide is 2-orthochlorophenylthiadiazole-5-sulfonamide.

6. The process of claim 3 wherein said sulfonamide is 2-trifluoroacetylimino-3-methyl-.DELTA..sup.2 -1,3,4-thiadiazoline-5-sulfonamide.

7. The process of claim 3 wherein said sulfonamide is 2-trichloroacetylimino-3-methyl-.DELTA..sup.2 -1,3,4-thiadiazoline-5-sulfonamide.

8. A composition adapted for topical application to the eye in unit dosage form consisting of an aqueous solution of from about 0.1% to about 5%, by weight, of a carbonic anydrase inhibitor sufficient to reduce aqueous humor formation and to reduce intraocular pressure, said carbonic anhydrase inhibitor being a pharmaceutically acceptable sulfonamide having the following properties:

(a) sufficiently soluble in water to form at least a 3 mM solution at pH of 8.2 or a 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 anydrase of not more than 3.times.10.sup.-8 molar;

(e) first order rate constant for penetration of said sulfonamide through a living rabbit cornea of at least 0.005 hr.sup.-1 ;

(f) not injurious to the cornea; and

(g) stable in solution and in contact with the cornea.

9. The composition of claim 8 wherein said sulfonamide is a heterocyclic sulfonamide.

10. The composition of claim 9 wherein said sulfonamide is a thiadiazoline sulfonamide.

11. The composition of claim 9 wherein said sulfonamide is 2-orthochlorophenylthiadiazole-5-sulfonamide.

12. The composition of claim 10 wherein said sulfonamide is 2-trifluoroacetylimino-3-methyl-.DELTA..sup.2 -1,3,4-thiadiazoline-5-sulfonamide.

13. The composition of claim 10 wherein said sulfonamide is 2-trichloroacetylimino-3-methyl-.DELTA..sup.2 -1,2,4-thiadiazoline-5-sulfonamide.
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