EP0105635A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Nonirritating aqueous ophthalmic compositions comfort formulation for ocular therepeutic agents
Assignee: Alcon Vision LLC
•
Filing: 1983-09-06
•
Granted: —
•
Expires: 2003-09-06
Abstract
Abstract Xanthine derivatives are described which decrease the stinging associated with the application of ophthalmic acidic anti-inflammatory agents.
Inventors
- 👤 Wesley Wehsin Han
- 👤 Robert Eugene Roehrs
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-27 21:57
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; A61K31/52; A61P; A61P27/00; A61P27/02; A61P29/00
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
99 words
An aqueous nonsteroidal ophthalmic composition comprising an effective amount of an acidic anti-inflammatory agent which is an arylcarboxylic acid, heteroarylcarboxylic acid, arylalkanoic acid, heteroarylalkanoic acid, or a pharmaceutically acceptable salt thereof or a mixture thereof and an amount of a xanthine derivative having the general formula:- where R 1 , R 2 and R 3 are each independently selected from a hydrogen atom, a methyl or ethyl group, and at least two of R 1 , R 2 and R 3 are methyl or ethyl groups, or a mixture thereof effective to reduce discomfort upon application of the composition.
Claim 2
Dependent Claim
99 words
An aqueous nonsteroidal ophthalmic composition comprising an effective amount of an acidic anti-inflammatory agent which is an arylcarboxylic acid, heteroarylcarboxylic acid, arylalkanoic acid, heteroarylalkanoic acid, or a pharmaceutically acceptable salt thereof or a mixture thereof and an amount of a xanthine derivative having the general formula:- where R 1 , R 2 and R 3 are each independently selected from a hydrogen atom, a methyl or ethyl group, and at least two of R 1 , R 2 and R 3 are methyl or ethyl groups, or a mixture thereof effective to reduce discomfort upon application of the composition.
Claim 3
Dependent Claim
39 words
A composition as claimed in claim 1 wherein the derivative is present in an amount in the range of from the amount by which the derivative is soluble in the water contained in the composition to 0.05% weight/ volume.
Claim 4
Dependent Claim
24 words
An aqueous ophthalmic composition as claimed in claim 1 or claim 2 wherein the xanthine compound is theophylline, caffeine, theobromine or a mixture thereof.
Claim 5
Dependent Claim
41 words
An aqueous ophthalmic composition as claimed in any one of the preceding claims wherein the anti-inflammatory agent is mefenamic acid, flufenamic acid, clonixin, flufenisal, 4-(t-butyl)benzeneacetic acid, ibufenac, ibuprofen, alclofenac, fenoprofen, naproxen, indomethacin, tolmetin, flurbiprofen, ketoprofen, namoxyrate, suprofen, or a mixture thereof.
Claim 6
Independent Claim
106 words
A method for reducing the stinging and discomfort of an aqueous ophthalmic composition containing an effective amount of an acidic anti-inflammatory agent selected from arylcarboxylic acid, heteroarylcarboxylic acid, arylalkanoic acid or heteroarylalkanoic acid, a pharmaceutically acceptable salt thereof or a mixture thereof comprising adding to the composition a xanthine derivative having the general formula : where R1, R 2 and R 3 are each independently selected from a hydrogen atom, a methyl or ethyl group, and at least two of R 1 , R 2 and R 3 are methyl or ethyl groups, or a mixture thereof effective to reduce discomfort upon application of the composition.
Claim 7
Independent Claim
106 words
A method for reducing the stinging and discomfort of an aqueous ophthalmic composition containing an effective amount of an acidic anti-inflammatory agent selected from arylcarboxylic acid, heteroarylcarboxylic acid, arylalkanoic acid or heteroarylalkanoic acid, a pharmaceutically acceptable salt thereof or a mixture thereof comprising adding to the composition a xanthine derivative having the general formula : where R1, R 2 and R 3 are each independently selected from a hydrogen atom, a methyl or ethyl group, and at least two of R 1 , R 2 and R 3 are methyl or ethyl groups, or a mixture thereof effective to reduce discomfort upon application of the composition.
Claim 8
Dependent Claim
39 words
A method as claimed in claim 5 wherein the xanthine derivative is present in an amount in the range of from the amount by which the derivative is soluble in the water contained in the composition to 0.05% weight/volume.
Claim 9
Dependent Claim
19 words
A method as claimed in claim 5 wherein the xanthine compound is theophylline, caffeine, theobromine or a mixture thereof.
Claim 10
Dependent Claim
36 words
A method as claimed in claim 5 wherein the ocular therapeutic agent is mefenamic acid, flufenamic acid, clonixin, flufenisal, 4-(t-butyl)benzeneacetic acid, ibufenac, ibuprofen, alclofenac, fenoprofen, naproxen, indomethacin, tolmetin, flurbifren, ketoprofen, namoxyrate, suprofen, or a mixture thereof.
Claim 11
Dependent Claim
26 words
An aqueous nonsteroidal ophthalmic composition as claimed in any one of Claims .1 to 4 which is in the form of a solution, suspension or gel.
Claim 12
Independent Claim
47 words
A method for the preparation of an ophthalmic composition as claimed in any one of claims 1 to 4 in which the desired amounts of the active ingredients are dissolved in the required amount of water, with stirring, to ensure that all of the ingredients are dissolved.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.