EP0036351A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Ophthalmic compositions of carbonic anhydrase inhibitors for topical application in the treatment of elevated intraocular pressure
Assignee: Merck and Co Inc
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Filing: 1981-03-03
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Granted: —
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Expires: 2001-03-03
Abstract
Abstract Although dibasic carbonic anhydrase inhibitors (CAI.) can be administered systemically by oral or intravenous routes, attempts to administer them topically were inadvisable because of their elevated pH. The mono-alkali metal salts in the treatment of intraocular hypertension especially the sodium and potassium salts, of dibasic salt-forming C.A.I. are as effective in lowering intraocular pressure as dialkali metal salts of dibasic C.A.I. while having a pH more in harmony with ocular pH. They are found particularly useful when administered in conjunction with an ophthalmologically acceptable water-soluble polymer such as hydroxypropylcellulose in an aqueous carrier.
Inventors
- 👤 Robert L. Smith
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 22:25
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/28; A61P; A61P27/00; A61P27/02; A61K9/00; A61K9/0012; A61K9/0048; A61K9/0051
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
33 words
An ophthalmic composition for lowering intraocular pressure comprising an intraocular pressure reducing amount of a mono alkali metal salt of a dibasic carbonic anhydrase inhibitor and an ophthalmologically acceptable carrier for topical application.
Claim 2
Dependent Claim
33 words
An ophthalmic composition for lowering intraocular pressure comprising an intraocular pressure reducing amount of a mono alkali metal salt of a dibasic carbonic anhydrase inhibitor and an ophthalmologically acceptable carrier for topical application.
Claim 3
Dependent Claim
26 words
A composition according to Claim 1 where the alkali metal salt of the carbonic anhydrase inhibitor is from 0.1 to 15% by weight of said composition.
Claim 4
Dependent Claim
29 words
A composition according to Claim 1 where the carbonic anhydrase inhibitor is selected from the group consisting of 4,5-dichloro-m-benzenedisulfonamide; N-[5 - (aminosulfonyl)-3-methyl-l,3,4-thiadiazol-2(3H)-ylidene]acetamide; N-[5-(aminosulfonyl)-3-methyl-I,3,4-thiadiazol-2(3H)-ylidene]-acetamide; p-sulfamoylbenzoic acid; N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]propanamide; N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]butanamide and 5-benzenesulfonamido-l,3,4-thiadiazol-2-sulfonamide.
Claim 5
Dependent Claim
43 words
An ophthalmologically acceptable water solid polymeric insert comprising an intraocular pressure lowering amount of a mono potassium or mono sodium salt of a carbonic anhydrase inhibitor selected from the group consisting of 4,5-dichloro-m-benzene-disulfonamide; N-[5-(aminosulfonyl)-3-methyl- l,3,4-thiadiazol-2(3H)-ylidene]acetamide; N-[5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene]-acetamide; p-sulfamoylbenzoic acid; N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]propanamide; N -[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]butanamide and 5-benzenesulfonamido-1,3,4-thiadiazol-2-sulfonamide.
Claim 6
Dependent Claim
43 words
An ophthalmologically acceptable water solid polymeric insert comprising an intraocular pressure lowering amount of a mono potassium or mono sodium salt of a carbonic anhydrase inhibitor selected from the group consisting of 4,5-dichloro-m-benzene-disulfonamide; N-[5-(aminosulfonyl)-3-methyl- l,3,4-thiadiazol-2(3H)-ylidene]acetamide; N-[5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene]-acetamide; p-sulfamoylbenzoic acid; N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]propanamide; N -[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]butanamide and 5-benzenesulfonamido-1,3,4-thiadiazol-2-sulfonamide.
Claim 7
Dependent Claim
30 words
A composition according to Claim 1 where there is included an additional intraocular pressure lowering amount of an ophthalmic medicament that functions by a mechanism other than carbonic anhydrase inhibition.
Claim 8
Dependent Claim
13 words
A composition according to Claim 5 where the additional ophthalmic medicament is timolol.
References Cited (Backward Citations)
No citation records indexed.
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