US4305927A
Expired / Lapsed
US
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Method for the management of intraocular pressure
Assignee: Alza Corp
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Filing: 1980-02-08
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Granted: 1981-12-15
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Expires: 2000-02-08
Abstract
Abstract A method for the management of intraocular pressure and for lessening the incidence of side effects associated therewith is disclosed. The method comprises administering continuously controlled low dosage amounts of acetazolamide to produce both a lessening of the side effects and lowering of the intraocular pressure.
Inventors
- 👤 Felix Theeuwes
- 👤 William F. Bayne
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 21:30
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0002; A61K9/0004
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
198 words
In a method for treating ocular hypertension in a warm-blooded animal responsive to acetazolamide and having ocular hypertension, the improvement consisting of orally administering to the animal an osmotic dosage formulation consisting of a wall of semipermeable cellulose acetate surrounding a compartment containing up to 250 mg of acetazolamide, which is released through a passageway in the wall to the animal in a controlled, and continuous rate, and in a therapeutically effective amount up to 20 milligrams per hour over a prolonged period up to 12 hours to produce effective blood levels for lowering intraocular pressure within the average normal range, said method of acetazolamide administration occurring independent of the pH of the animal, producing a hypotensive effect, a blood plasma acetazolamide concentration that is in a steady, substantially constant state and characterized by a low plasma dosage form index of less than 2.5 as exemplified by the ratio of the maximum to minimum plasma concentration of the acetazolamide, said plasma concentration lower than the plasma level obtained by non-osmotic delivery of acetazolamide while concomitantly equally lowering the intraocular pressure and lessening the incidence of side effects of drowsiness, confusion and paresthesias associated with the administration of acetazolamide.
Claim 2
Dependent Claim
198 words
In a method for treating ocular hypertension in a warm-blooded animal responsive to acetazolamide and having ocular hypertension, the improvement consisting of orally administering to the animal an osmotic dosage formulation consisting of a wall of semipermeable cellulose acetate surrounding a compartment containing up to 250 mg of acetazolamide, which is released through a passageway in the wall to the animal in a controlled, and continuous rate, and in a therapeutically effective amount up to 20 milligrams per hour over a prolonged period up to 12 hours to produce effective blood levels for lowering intraocular pressure within the average normal range, said method of acetazolamide administration occurring independent of the pH of the animal, producing a hypotensive effect, a blood plasma acetazolamide concentration that is in a steady, substantially constant state and characterized by a low plasma dosage form index of less than 2.5 as exemplified by the ratio of the maximum to minimum plasma concentration of the acetazolamide, said plasma concentration lower than the plasma level obtained by non-osmotic delivery of acetazolamide while concomitantly equally lowering the intraocular pressure and lessening the incidence of side effects of drowsiness, confusion and paresthesias associated with the administration of acetazolamide.
Claim 3
Dependent Claim
35 words
A method for treating ocular hypertension in a warm-blooded animal according to claim 1 wherein the treating of ocular hypertension consists in lowering the intraocular pressure associated with narrow-angle glaucoma, wide-angle glaucoma, and secondary glaucoma.
Claim 4
Dependent Claim
39 words
A method for treating ocular hypertension in a warm-blooded animal according to claim 1 wherein the plasma concentration of acetazolamide in the animal administered up to 20 milligrams per hour is up to 6 micrograms per milliter of plasma.
Claim 5
Dependent Claim
28 words
A method for treating ocular hypertension in a warm-blooded animal according to claim 1 wherein the method produces an intraocular pressure lowering of up to 15 mm Hg.
Claim 6
Dependent Claim
46 words
A method for treating ocular hypertension in a warm-blooded animal according to claim 1 wherein the wall of semipermeable cellulose acetate consists of 58 to 62% cellulose acetate having an acetyl content of 32%, and 30 to 34% cellulose acetate having an acetyl content of 39.8%.
Claim 7
Dependent Claim
28 words
A method for treating ocular hypertension in a warm-blooded animal according to claim 1 wherein the wall of semipermeable cellulose acetate contains from 7 to 9% polyethylene glycol.
Claim 8
Dependent Claim
128 words
An oral, osmotic delivery device containing acetazolamide, said device having a semipermeable wall consisting essentially of 58 to 65% cellulose acetate having an acetyl content of 31 to 33%, from 30 to 32% cellulose acetate having an acetyl content of 39 to 40%, and from 7 to 9% of polyethylene glycol, said device having a passageway through said wall, the device being constructed so as to release the acetazolamide in a controlled, continuous rate and in a therapeutically effective amount up to 20 milligrams per hour to produce effective blood levels for lowering intraocular pressure within the average normal range and to obtain a low plasma dosage form index of less than 2.5 as exemplified by the ratio of the maximum to minimum plasma concentration of the acetazolamide.
Claim 9
Dependent Claim
128 words
An oral, osmotic delivery device containing acetazolamide, said device having a semipermeable wall consisting essentially of 58 to 65% cellulose acetate having an acetyl content of 31 to 33%, from 30 to 32% cellulose acetate having an acetyl content of 39 to 40%, and from 7 to 9% of polyethylene glycol, said device having a passageway through said wall, the device being constructed so as to release the acetazolamide in a controlled, continuous rate and in a therapeutically effective amount up to 20 milligrams per hour to produce effective blood levels for lowering intraocular pressure within the average normal range and to obtain a low plasma dosage form index of less than 2.5 as exemplified by the ratio of the maximum to minimum plasma concentration of the acetazolamide.
Claim 10
Dependent Claim
35 words
The oral, osmotic delivery device according to claim 7 wherein the 58 to 65% cellulose acetate has an acetyl content of 32%, and the 30 to 32% cellulose acetate has an acetyl content of 39.8%.
References Cited (Backward Citations)
US3916899A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-12-14 | 1985-06-15 | 1985-12-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-12-14 | 1989-06-15 | 1989-12-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-12-14 | 1993-06-15 | 1993-12-15 | $7700.00 | Window Closed / Lapsed |