EP0129284A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Improved penetrating topical pharmaceutical compositions containing 1-dodecyl-azacycloheptan-2-one
Assignee: Procter and Gamble Co
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Filing: 1984-06-12
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Granted: —
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Expires: 2004-06-12
Abstract
Abstract Improved topical pharmaceutical compositions containing a pharmaceutically-active agent and the penetration enhancing agent 1-dodecylazacycloheptan-2-one are disclosed. This agent is used at selected levels in combination with certain C<sub>3</sub>-C<sub>4</sub> diols or a 1-substituted azacycloalkyl-2-one. This composition provides marked transepidermal and percutaneous delivery of the selected pharmaceutically-active agent. A method of treating certain pathologies and conditions responsive to the selected active, systemically or locally, is also disclosed.
Inventors
- 👤 Eugene Rex Cooper
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-04 08:45
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/22; A61K31/00; A61K31/56; A61K31/57; A61K9/00; A61K9/0012; A61K9/0014
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
152 words
A penetration-enhancing pharmaceutical composition for topical application, characterized in that it comprises: (a) a safe and effective amount of a pharmaceutically-active agent; (b) 0% to 80% by weight of a solvent selected from ethanol and 2-propanol; (c) 0% to 80% by weight water; (d) 15% to 99% by weight of a penetration-enhancing diol or cycloketo compound selected from the group consisting of 1,2-propanediol, 1,3-propanediol, 1 ,2-butanediol, 1,3-butanediol, 1,4-butanediol, 2,3-butanediol; a compound of the formula where R 11 is selected from the group consisting of -H, -CH 3 , - C 2 H 4 0H, -C 3 H 7 , -C 3 H 6 OH, or -CH 2 CHOHCH 2 0H, R 12 is - H , -CH 3 , -C 2 H 5 , -C 3 H 7 , -C 4 H 9 , and m is an integer from 0-2, and mixtures thereof; and (e) 0.9% to 40% by weight 1-dodecylazacycloheptan-2-one.
Claim 2
Dependent Claim
152 words
A penetration-enhancing pharmaceutical composition for topical application, characterized in that it comprises: (a) a safe and effective amount of a pharmaceutically-active agent; (b) 0% to 80% by weight of a solvent selected from ethanol and 2-propanol; (c) 0% to 80% by weight water; (d) 15% to 99% by weight of a penetration-enhancing diol or cycloketo compound selected from the group consisting of 1,2-propanediol, 1,3-propanediol, 1 ,2-butanediol, 1,3-butanediol, 1,4-butanediol, 2,3-butanediol; a compound of the formula where R 11 is selected from the group consisting of -H, -CH 3 , - C 2 H 4 0H, -C 3 H 7 , -C 3 H 6 OH, or -CH 2 CHOHCH 2 0H, R 12 is - H , -CH 3 , -C 2 H 5 , -C 3 H 7 , -C 4 H 9 , and m is an integer from 0-2, and mixtures thereof; and (e) 0.9% to 40% by weight 1-dodecylazacycloheptan-2-one.
Claim 3
Dependent Claim
22 words
A composition according to Claim 1 characterized in that component (d) is present at a level of 20% to 99% by weight.
Claim 4
Dependent Claim
26 words
A compound according to any of Claims 1 or 2 characterized in that component (d) is present at a level of 25% to 96% by weight.
Claim 5
Dependent Claim
25 words
A composition according to any of Claims 1-3 characterized in that the 1-dodecylazacycloheptan-2-one is present at a level of from 1% to 35% by weight.
Claim 6
Dependent Claim
25 words
A composition according to any of Claims 1-4 characterized in that the 1-dodecylazacycloheptan-2-one is present at a level of from 2% to 101 by weight.
Claim 7
Dependent Claim
15 words
A composition according to any of Claims 1-5 characterized in that component (d) is 1,2-propanediol.
Claim 8
Dependent Claim
16 words
A composition according to any of Claims 1-5 characterized in that component (d) is 1-(2-hydroxyethyl)-azacyclo- pentan-2-one.
Claim 9
Dependent Claim
26 words
A composition according to any of Claims 1-7 characterized in that the ratio by weight of component (d) to 1-dodecyl- azacycloheptan-2-one is from 3:1 to 100:1.
Claim 10
Dependent Claim
17 words
A composition according to any of Claims 1-8 characterized in that the pharmaceutically-active agent is a corticosteroid.
Claim 11
Dependent Claim
26 words
A composition according to Claim 9 characterized in that the corticosteroid is present at a level of from 0.01% to 10% by weight of the composition.
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