- Compositions and method comprising heterocyclic compounds containing two heteroatoms as membrane penetration enhancers
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A method and compositions for enhancing absorption of topically administered physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for local or systemic use, comprising a therapeutically effective amount of a pharmaceutically active agent and a non-toxic, effective amount of penetration enhancing agent of the formula I: STR1 wherein R is a saturated or unsaturated, straight or branched, cyclic or acyclic hydrocarbon group with from 1 to 19 carbon atoms, alkoxyalkyl, haloalkyl, specifically trifluoromethyl, alkoxy, amino, alkylamino and acylamino; R' and R" are hydrogen, alkyl, trifluoromethyl, alkoxyalkyl, aminoalkyl, alkyl- and acylaminoalkyl, carboxy, carbalkoxy, hydroxyalkyl or lower alkyl ester thereof; X is O or NR1 wherein R1 is hydrogen, alkyl, alkenyl, alkoxyalkyl, carbalkoxyalkyl, aminoalkyl, alkyl- and acylaminoalkyl, hydroxyalkyl or hydroxyalkyloxyalkyl and lower alkyl ester thereof; and n is 2 or 3 are disclosed.
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- Compositions and method comprising heterocyclic compounds containing two heteroatoms
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A method and compositions for topically administering physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for systemic use or to the skin of humans and animals for localized use comprising applying to such skin or membrane a mixture of said physiologically active agent and a non-toxic, effective penetrating amount of penetration enhancing compound having the structural formula I: STR1 wherein: R is a saturated or unsaturated hydrocarbon group with from 5 to 19 carbon atoms; R' and R" are hydrogen, lower alkyl, trifluoromethyl, lower hydroxyalkyl or lower alkyl ester of lower hydroxyalkyl, with the proviso that both R' and R" are not lower hydroxyalkyl; X is O or NR1 ; R1 being hydrogen, lower alkyl, lower alkenyl, lower hydroxyalkyl or lower alkyl ester of lower hydroxyalkyl are disclosed.
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