A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
167/159, 71/23,
A61K 47/00 (2006.01) A01N 25/00 (2006.01) A01N 37/44 (2006.01) A01N 43/36 (2006.01) A01N 43/40 (2006.01) A01N 43/46 (2006.01) A61K 31/395 (2006.01) A61K 47/22 (2006.01) C05G 3/00 (2006.01) C09B 67/00 (2006.01)
Patent
CA 1334647
This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula Image wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or -CH2-; wherein R represents alkyl optionally substituted with one to three double or triple bonds, -SR''', -OR''', -NHR''', -CH3, or COOR1, and wherein R1 represents hydrogen or lower alkyl; wherein R''' represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group; wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, -(CH2)yCOOR1 and with y being between zero and 3, inclusive; and wherein R'' represents hydrogen or -(CH2)yCOOR1 such 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; and wherein m is between one and 5, preferably 2, 3, or 4, while n is between 1 and 24, preferably between 5 and 12, and x is zero or 1, inclusive. It has been found that both open and closed-chain embodiments of the penetration enhancer are sufficient to carry physiologically active agents through body membranes and into the bloodstream.
600789
Minaskanian Gevork
Peck James Vanolden
Gowling Lafleur Henderson Llp
Whitby Research Inc.
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