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Details for Patent: 5,051,260

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Details for Patent: 5,051,260

Title: Method and composition for enhancing the cutaneous penetration of pharmacologically active agents
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.
Inventor(s): Chess; Samuel (Newport Beach, CA), McCullough; Jerry L. (Irvine, CA), Weinstein; Gerald D. (Irvine, CA)
Assignee: The Regents of the University of California (Alameda, CA)
Filing Date:Sep 20, 1990
Application Number:07/556,982
Claims:1. 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.sup.1 is the same or different alkylene or alkenylene radical;

m is an integer selected so as to provide an (O--R.sup.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.

2. The method of claim 1, wherein each of n and n' is 0.

3. The method of claim 1, wherein m is an integer selected so as to provide an --O--R.sup.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.

4. The method of claim 1, wherein m is an integer selected so as to provide an --O--R.sup.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.

5. 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.

6. The method of claim 5, wherein the locally administrable topical composition comprises a cosmetic, a sunscreen or an insect repellant.

7. 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.

8. 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.
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