US4911920A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Sustained release, comfort formulation for glaucoma therapy
Assignee: Alcon Research LLC
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Filing: 1988-02-05
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Granted: 1990-03-27
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Expires: 2008-02-05
Abstract
Abstract Disclosed are nonstinging, sustained release ophthalmic formulations to control intraocular pressure in antiglaucoma therapy comprising a basic active, a cation exchange resin, and, inter alia, an acidic, mucomimetic polymer. Also disclosed are methods of treatment comprising administering such formulations topically to the eye when indicated for control and lowering of intraocular pressure.
Inventors
- 👤 Rajni Jani
- 👤 Robert G. Harris
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 20:36
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/4164; A61K31/4178; A61K31/13; A61K31/135; A61K31/137; A61K31/138; A61K31/4168; A61K31/74; A61K31/765; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/585; A61K9/00; A61K9/0012; A61K9/0048
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
118 words
A sustained release ophthalmic pharmaceutical composition in the form of an aqueous gel, a pourable aqueous dispersion, or anhydrous salt, for controlling and lowering intraocular pressure comprising: a therapeutically effective amount of betaxolol; an amount of an anionic mucomimetic polymer having carboxylic acid functional groups which comprise from 2 to 7 carbon atoms per functional group and a molecular weight of from 50,000 to 6 million such that the composition in the form of an aqueous gel or pourable aqueous dispersion has a viscosity of about 1 to about 20,000 cps.; and sodium poly(styrenedivinylbenzene) sulfonic acid at a concentration of from about 0.05% to 10.0% by weight, the composition having a pH of from about 3.0 to 8.5.
Claim 2
Dependent Claim
118 words
A sustained release ophthalmic pharmaceutical composition in the form of an aqueous gel, a pourable aqueous dispersion, or anhydrous salt, for controlling and lowering intraocular pressure comprising: a therapeutically effective amount of betaxolol; an amount of an anionic mucomimetic polymer having carboxylic acid functional groups which comprise from 2 to 7 carbon atoms per functional group and a molecular weight of from 50,000 to 6 million such that the composition in the form of an aqueous gel or pourable aqueous dispersion has a viscosity of about 1 to about 20,000 cps.; and sodium poly(styrenedivinylbenzene) sulfonic acid at a concentration of from about 0.05% to 10.0% by weight, the composition having a pH of from about 3.0 to 8.5.
Claim 3
Dependent Claim
13 words
The composition according to claim 1 wherein the composition is an aqueous dispersion.
Claim 4
Dependent Claim
21 words
A composition according to claim 1 wherein the betaxolol is present at a concentration of from about 0.01 to 4.0 wt.%.
Claim 5
Dependent Claim
13 words
A composition according to claim 1 wherein the anionic mucomimetic polymer comprises carbomer.
Claim 6
Dependent Claim
45 words
A composition according to claim 1 wherein the betaxolol is present at a concentration of about 0.25 wt.%, the anionic mucomimetic polymer is carbomer present at a concentration of about 0.20 wt.%, and the sulfonic acid is present at a concentration of about 0.25 wt.%.
Claim 7
Dependent Claim
26 words
The composition of claim 1 wherein the particulate cation exchange resin is in the form of a finely divided powder, said powder consisting of spheroidal particles.
Claim 8
Independent Claim
114 words
A method of treatment for controlling and lowering intraocular pressure which comprises administering topically to the affected eye a pharmaceutical composition which includes: a therapeutically effective amount of betaxolol; an amount of an anionic mucomimetic polymer having carboxylic acid functional groups which comprise from 2 to 7 carbon atoms per functional group and a molecular weight of from 50,000 to 6 million such that the composition in the form of an aqueous gel or pourable aqueous dispersion has a viscosity of about 1 to about 20,000 cps.; and sodium poly(styrene-divinylbenzene) sulfonic acid at a concentration of from about 0.05% to 10.0% by weight, the composition having a pH of from about 3.0 to 8.5.
Claim 9
Independent Claim
114 words
A method of treatment for controlling and lowering intraocular pressure which comprises administering topically to the affected eye a pharmaceutical composition which includes: a therapeutically effective amount of betaxolol; an amount of an anionic mucomimetic polymer having carboxylic acid functional groups which comprise from 2 to 7 carbon atoms per functional group and a molecular weight of from 50,000 to 6 million such that the composition in the form of an aqueous gel or pourable aqueous dispersion has a viscosity of about 1 to about 20,000 cps.; and sodium poly(styrene-divinylbenzene) sulfonic acid at a concentration of from about 0.05% to 10.0% by weight, the composition having a pH of from about 3.0 to 8.5.
Claim 10
Dependent Claim
13 words
The method according to claim 7 wherein the composition is an aqueous dispersion.
Claim 11
Dependent Claim
21 words
A method according to claim 7 wherein the betaxolol is present at a concentration of from about 0.01 to 4.0 wt.%.
Claim 12
Dependent Claim
13 words
A method according to claim 7 wherein the anionic mucomimetic polymer comprises carbomer.
Claim 13
Dependent Claim
47 words
A method according to claim 7 wherein the betaxolol is present at a concentration of about 0.25 wt.%, the anionic mucomimetic polymer is carbomer present at a concentration of about 0.20 wt.%, and the sodium poly(styrene-divinylbenzene) sulfonic acid is present at a concentration of about 0.25 wt.%.
Claim 14
Dependent Claim
26 words
The method of claim 7 wherein the particulate cation exchange resin is in the form of a finely divided powder, said powder consisting of spheroidal particles.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1993-03-26 | 1993-09-25 | 1994-03-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-03-26 | 1997-09-25 | 1998-03-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-03-26 | 2001-09-25 | 2002-03-27 | $7700.00 | Window Closed / Lapsed |