Penetration enhancers for transdermal delivery of systemic agents

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United States of America Patent

PATENT NO 5470848
SERIAL NO

08139684

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Abstract

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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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Patent Owner(s)

Patent OwnerAddress
DISCOVERY THERAPEUTICS INC2028 DABNEY ROAD SUITE E-17 RICHMOND VA 23230-3311

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Minaskanian, Gevork 8 Havenwood, Irvine, CA 92714 43 408
Peck, James V 2524 Bowdoin Pl., Costa Mesa, CA 92626 43 483

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