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US5051260A Expired / Lapsed US ⏱️ 0.0 years remaining

Method and composition for enhancing the cutaneous penetration of pharmacologically active agents

Assignee: University of California, San Diego
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Filing: 1990-09-20
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Granted: 1991-09-24
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Expires: 2010-09-20
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Abstract

Abstract Method and compositions for enhancing the cutaneous penetration of topically or transdermally delivered pharmacologically active agents. The compositions include various urethane compounds as permeation enhancers, the urethane compounds formed from reaction of a monomeric organic diisocyanate with a hydroxy- or hydroxy/alkoxy-terminated linear alkylene or polyalkylene glycol or polyether.

Inventors

  • 👤 Samuel Chess
  • 👤 Jerry L. McCullough
  • 👤 Gerald D. Weinstein

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 19:09
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/16; A61K47/18; A61K9/00; A61K9/0012; A61K9/0014; C; C08; C08G; C08G18/00; C08G18/06; C08G18/28; C08G18/40; C08G18/48; C08G18/4825; C08G18/4833

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 177 words
A method of moisturizing skin, comprising applying to skin surface a composition containing (a) a locally administrable topical composition containing a topical carrier; and (b) a hydroxy-terminated urethane compound having the formula: ##STR4## wherein: R is an alkylene or alkenylene radical containing from one to about 20 carbon atoms; or a cycloalkylene or cycloalkenylene radical containing from about 5 to about carbon atoms, or a mononuclear or fused ring arylene radical containing from about 6 to about 10 carbon atoms, unsubstituted or substituted with one or more lower alkyl, lower alkoxy, lower alkoxy-substituted lower alkyl, nitro or amino groups or halogen atoms; R 1 is the same or different alkylene or alkenylene radical; m is an integer selected so as to provide an (O--R 1 ) moiety having a molecular weight of from about 40 to about 6,000; and n and n' are the same or a different integer of from 0 to 30, inclusive, correlated with m so as to provide a hydroxy-terminated urethane compound having a molecular weight of from about 220 to about 200,000.
Claim 2
Independent Claim 177 words
A method of moisturizing skin, comprising applying to skin surface a composition containing (a) a locally administrable topical composition containing a topical carrier; and (b) a hydroxy-terminated urethane compound having the formula: ##STR4## wherein: R is an alkylene or alkenylene radical containing from one to about 20 carbon atoms; or a cycloalkylene or cycloalkenylene radical containing from about 5 to about carbon atoms, or a mononuclear or fused ring arylene radical containing from about 6 to about 10 carbon atoms, unsubstituted or substituted with one or more lower alkyl, lower alkoxy, lower alkoxy-substituted lower alkyl, nitro or amino groups or halogen atoms; R 1 is the same or different alkylene or alkenylene radical; m is an integer selected so as to provide an (O--R 1 ) moiety having a molecular weight of from about 40 to about 6,000; and n and n' are the same or a different integer of from 0 to 30, inclusive, correlated with m so as to provide a hydroxy-terminated urethane compound having a molecular weight of from about 220 to about 200,000.
Claim 3
Dependent Claim 13 words
The method of claim 1, wherein each of n and n' is 0.
Claim 4
Dependent Claim 55 words
The method of claim 1, wherein m is an integer selected so as to provide an --O--R 1 -- moiety having a molecular weight of from about 40 to about 6000, correlated with n and n' so as to provide a hydroxy-terminated urethane compound having a molecular weight of from about 220 to about 37,000.
Claim 5
Dependent Claim 55 words
The method of claim 1, wherein m is an integer selected so as to provide an --O--R 1 -- moiety having a molecular weight of from about 400 to about 2000, correlated with n and n' so as to provide a hydroxy-terminated urethane compound having a molecular weight of from about 1000 to about 15,000.
Claim 6
Dependent Claim 28 words
The method of claim 1, wherein the topical carrier comprises a liquid or nonliquid carrier, a gel, a cream, an ointment, a lotion, an aerosol or an emulsifier.
Claim 7
Dependent Claim 20 words
The method of claim 5, wherein the locally administrable topical composition comprises a cosmetic, a sunscreen or an insect repellant.
Claim 8
Dependent Claim 29 words
The method of claim 6, wherein the hydroxy-terminated urethane compound is present in an amount of from about 3 wt. % to about 90 wt. % of the composition.
Claim 9
Dependent Claim 29 words
The method of claim 6 wherein the hydroxy-terminated urethane compound is present in an amount of from about 10 wt. % to about 25 wt. % of the composition.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1994-09-23 1995-03-25 1995-09-24 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1998-09-23 1999-03-25 1999-09-24 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2002-09-23 2003-03-25 2003-09-24 $7700.00 Window Closed / Lapsed

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