Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1993-10-22
1995-11-28
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514327, 514424, 514426, 514742, 514947, A61K 3156, A61K 31445, A61K 3140, A61K 3104
Patent
active
054708486
ABSTRACT:
This invention relates to a method for administering systemically active agents through the skin or mucosal membranes of humans and animals and into the bloodstream in a transdermal device or formulation comprising topically administrating with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## or the pharmaceutically acceptable salt thereof wherein W represents oxygen, sulfur or two hydrogen radicals; Z represents --CH.sub.2 --; R represents alkyl optionally substituted with one to three double or triple bonds, --SR"', --OR"', --NHR"', or --COOR.sub.1 ; R"' represents alkyl, alkylthioalkyl, alkoxyalkyl, amino alkyl, optionally substituted with a phenyl, or benzoyl; R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy or --(CH.sub.2).sub.y COOR.sub.1 ; R" represents hydrogen or --(CH.sub.2).sub.y COOR.sub.1 ; R.sub.1, in each instance, independently represents hydrogen or lower alkyl; y, in each instance, is between zero and 3, inclusive; m is between one and 3, inclusive; n is between one and 24, inclusive; and x is zero or one, inclusive;
with the provisos that when R" is hydrogen, then W is two hydrogen radicals and R' is not hydrogen; and when R' is hydrogen, then R" is not hydrogen. It has been found that the penetration enhancers are sufficient to carry physiologically active agents through body membranes and into the bloodstream.
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Minaskanian Gevork
Peck James V.
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