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EP0164998A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Compositions and methods of enhancing transdermal and transmembrane penetration of topical and systemic agents

Assignee: Allergan Inc
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Filing: 1985-06-04
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Granted: —
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Expires: 2005-06-04
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Abstract

Abstract Composition and methods usefuf for enhancing the transdermal and transmembrane drug delivery of topical and systemic agents. The compositions and methods comprise the active agent together with an effective amount of certain amides of heterocyclic amines as defined herein as penetration enhancers and topically administering a human or animal skin or other membranes the resulting compositions.

Inventors

  • 👤 Dorla Mirejovsky
  • 👤 Harun Takruri

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-06 01:50
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/06; C; C07; C07D; C07D295/00; C07D295/16; C07D295/18; C07D295/182; C07D295/185; A61K47/00; A61K47/06; A61K47/22; A61K9/0012; A61K9/0014

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 73 words
A topical composition for enhancing the transdermal and transmembrane penetration of pharmacologically active substances which comprises an effective amount of said substance and a nontoxic penetrating amount of a compound having the structural formula: in which: m is 4 to 9; R 1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and R is a straight or branched chain alkyl group having from 1 to 20 carbon atoms.
Claim 2
Dependent Claim 73 words
A topical composition for enhancing the transdermal and transmembrane penetration of pharmacologically active substances which comprises an effective amount of said substance and a nontoxic penetrating amount of a compound having the structural formula: in which: m is 4 to 9; R 1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and R is a straight or branched chain alkyl group having from 1 to 20 carbon atoms.
Claim 3
Dependent Claim 13 words
The composition of Claim 1 in which the active substance is an antibiotic.
Claim 4
Dependent Claim 23 words
The composition of CLaim 2 in which m is 4 to 6, R 1 is hydrogen, and R is from 1 to 20.
Claim 5
Dependent Claim 22 words
The composition of Claim 3 in which m is 6, R 1 is hydrogen, and R is undecyl, the compound being hexamethyLeneLauramide.
Claim 6
Dependent Claim 19 words
The composition of CLaim 2 in which the antibiotic is selected from the group consisting of erythromycin and Lincomycin.
Claim 7
Dependent Claim 14 words
The composition of CLaim 1 in which the active substance is an antifungal agent.
Claim 8
Dependent Claim 13 words
The composition of CLaim 1 in which the active substance is a steroid.
Claim 9
Dependent Claim 28 words
A compound of the formula: for use in enhancing the transdermal and transmembrane penetration of a pharmacologically active substance by cooperative topical administration of the compound and substance.
Claim 10
Dependent Claim 28 words
A compound of the formula: for use in enhancing the transdermal and transmembrane penetration of a pharmacologically active substance by cooperative topical administration of the compound and substance.
Claim 11
Independent Claim 75 words
A method for preparing a topical composition for enhancing the transdermal and transmembrane penetration of pharmacologically active substances which comprises admixing a nontoxic penetrating amount of a compound having the structural formula: in which: m is 4 to 9; R 1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and R is a straight or branched chain alkyl group having from 1 to 20 carbon atoms with nontoxic pharmaceutical carriers.
Claim 12
Independent Claim 75 words
A method for preparing a topical composition for enhancing the transdermal and transmembrane penetration of pharmacologically active substances which comprises admixing a nontoxic penetrating amount of a compound having the structural formula: in which: m is 4 to 9; R 1 is hydrogen or an alkyl group having from 1 to 8 carbon atoms; and R is a straight or branched chain alkyl group having from 1 to 20 carbon atoms with nontoxic pharmaceutical carriers.
Claim 13
Dependent Claim 3 words
CLAIMS for AT
Claim 14
Independent Claim 75 words
A method for preparing a topical composition for enhancing the transdermal and transmembrane penetration of pharmacologically active substances which comprises admixing a nontoxic penetrating amount of a compound having the structural formula: in which: m is 4 to 9; R 1 is hydrogen or an aLkyL group having from 1 to 8 carbon atoms; and R is a straight or branched chain aLkyL group having from 1 to 20 carbon atoms with nontoxic pharmaceutical carriers.
Claim 15
Independent Claim 75 words
A method for preparing a topical composition for enhancing the transdermal and transmembrane penetration of pharmacologically active substances which comprises admixing a nontoxic penetrating amount of a compound having the structural formula: in which: m is 4 to 9; R 1 is hydrogen or an aLkyL group having from 1 to 8 carbon atoms; and R is a straight or branched chain aLkyL group having from 1 to 20 carbon atoms with nontoxic pharmaceutical carriers.
Claim 16
Dependent Claim 11 words
The method of Claim 1 wherein said composition is a solution.
Claim 17
Dependent Claim 11 words
The method of CLaim 1 wherein said composition is a cream.
Claim 18
Dependent Claim 11 words
The method of CLaim 1 wherein said composition is an ointment.

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