US5045317A — Enhancing the cutaneous penetration of pharmacolo…

Claim 1

Independent Claim 179 words

A composition for achieving enhanced cutaneous penetration of a dermally applied pharmacologically active agent, comprising: (a) a therapeutically effective amount of a pharmacologically active agent; and (b) a hydroxy-terminated urethane penetration enhancing 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 10 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 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 up to about 200,000.

Claim 2

Dependent Claim 179 words

A composition for achieving enhanced cutaneous penetration of a dermally applied pharmacologically active agent, comprising: (a) a therapeutically effective amount of a pharmacologically active agent; and (b) a hydroxy-terminated urethane penetration enhancing 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 10 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 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 up to about 200,000.

Claim 3

Dependent Claim 13 words

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

Claim 4

Dependent Claim 57 words

The composition 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 penetration enhancing compound having a molecular weight of from about 220 to about 37,000.

Claim 5

Dependent Claim 57 words

The composition 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 penetration enhancing compound having a molecular weight of from about 1000 to about 15,000.

Claim 6

Dependent Claim 10 words

The composition of claim 4 further containing a topical carrier.

Claim 7

Dependent Claim 28 words

The composition of claim 5 wherein the topical carrier comprises a liquid or nonliquid carrier, a gel, a cream, an ointment, a lotion, an aerosol or an emulsifier.

Claim 8

Dependent Claim 31 words

The composition of claim 6 wherein the hydroxy-terminated urethane penetration enhancing compound is present in an amount of from about 3 wt. % to about 90 wt. % of the composition.

Claim 9

Dependent Claim 31 words

The composition of claim 6 wherein the hydroxy-terminated urethane penetration enhancing compound is present in an amount of from about 10 wt. % to about 25 wt. % of the composition.

Claim 10

Dependent Claim 12 words

The composition of claim 8 wherein the pharmacologically active agent is methotrexate.

Claim 11

Dependent Claim 12 words

The composition of claim 9 wherein the topical carrier is a cream.

Claim 12

Dependent Claim 12 words

The composition of claim 9 wherein the topical carrier is an ointment.

Claim 13

Dependent Claim 13 words

The composition of claim 8 wherein the pharmacologically active agent is a steroid.

Claim 14

Dependent Claim 14 words

A composition of claim 12 wherein the steroid is hydrocortisone or a hydrocortisone derivative.

Claim 15

Dependent Claim 12 words

The method of claim 13 wherein the topical carrier is a cream.

Claim 16

Independent Claim 187 words

A method for achieving enhanced penetration of a pharmacologically active agent, comprising applying to the skin, hair or other epithelial surface a composition containing: (a) a locally administrable topical composition containing a topical carrier; and (b) a hydroxy-terminated urethane compound having the formula: ##STR5## 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 10 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 to 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 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 17

Independent Claim 187 words

A method for achieving enhanced penetration of a pharmacologically active agent, comprising applying to the skin, hair or other epithelial surface a composition containing: (a) a locally administrable topical composition containing a topical carrier; and (b) a hydroxy-terminated urethane compound having the formula: ##STR5## 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 10 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 to 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 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 18

Dependent Claim 13 words

The method of claim 15 wherein each of n and n' is 0.

Claim 19

Dependent Claim 57 words

The method of claim 15 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 penetration enhancing compound having a molecular weight of from about 220 to about 37,000.

Claim 20

Dependent Claim 57 words

The method of claim 15, 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 penetration enhancing compound having a molecular weight of from about 1000 to about 15000.

Claim 21

Dependent Claim 28 words

The method of claim 18, wherein the topical carrier comprises a liquid or nonliquid carrier, a gel, a cream, an ointment, a lotion, an aerosol or an emulsifier.

Claim 22

Dependent Claim 31 words

The method of claim 19 wherein the hydroxy-terminated urethane penetration enhancing compound is present in an amount of from about 3 wt. % to about 90 wt. % of the composition.

Claim 23

Dependent Claim 31 words

The method of claim 19, wherein the hydroxy-terminated urethane penetration enhancing compound is present in an amount of from about 10 wt. % to about 25 wt. % of the composition.

Claim 24

Dependent Claim 12 words

The method of claim 21, wherein the pharmacologically active agent is methotrexate.

Claim 25

Dependent Claim 12 words

The method of claim 21, wherein the topical carrier is a cream.

Claim 26

Dependent Claim 12 words

The method of claim 21 wherein the topical carrier is an ointment.

Claim 27

Dependent Claim 13 words

The method of claim 19, wherein the pharmacologically active agent is a steroid.

Claim 28

Dependent Claim 14 words

The method of claim 25 wherein the steroid is hydrocortisone or a hydrocortisone derivative.

Claim 29

Dependent Claim 12 words

The method of claim 26 wherein the topical carrier is a cream.

Claim 30

Dependent Claim 231 words

A composition for achieving enhanced penetration when applied to hair or nails comprising: (a) an effective amount of a hair or nail medicant or care agent; (b) a topical carrier up to about 75 wt. % of the composition; and (c) a permeation enhancer in an amount from about 5 wt. % to about 25 wt. % of the composition and effective to enhance the penetration of the hair or nail medicant or hair agent, the enhancer being a hydroxy-terminated urethane compound having the formula: ##STR6## 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 10 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 31

Dependent Claim 231 words

A composition for achieving enhanced penetration when applied to hair or nails comprising: (a) an effective amount of a hair or nail medicant or care agent; (b) a topical carrier up to about 75 wt. % of the composition; and (c) a permeation enhancer in an amount from about 5 wt. % to about 25 wt. % of the composition and effective to enhance the penetration of the hair or nail medicant or hair agent, the enhancer being a hydroxy-terminated urethane compound having the formula: ##STR6## 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 10 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 32

Dependent Claim 22 words

The composition as in claim 28 wherein the hair or nail medicant or care agent includes cutaneous growth enhancers, colorants or mascaras.

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	1994-09-02	1995-03-04	1995-09-03	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	1998-09-02	1999-03-04	1999-09-03	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	2002-09-02	2003-03-04	2003-09-03	$7700.00	Window Closed / Lapsed

Enhancing the cutaneous penetration of pharmacologically active agents

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