Transdermal compositions of 1-oxohydrocarbyl-substituted azacycl

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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514 29, 514 45, 514 53, 514256, 5142322, 5142275, 514247, 536 24, 544123, 544121, 544106, 544 59, A61K 3170, A61K 31715, A61K 31505, A01N 4304

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active

050735446

ABSTRACT:
This invention provides compositions for enhancing penetration of physiologically active agents through the skin or mucosal membranes and for retaining these agents in body tissues, said composition comprising effective amounts of a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms, ##STR2## wherein R" is H or halogen, and salts, e.g. acid or quaternary derivatives, thereof. These compositions are useful in topical or transdermal applications of the physiologically-active agent.

REFERENCES:
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patent: 4440777 (1984-04-01), Zupan
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patent: 4917896 (1990-04-01), Peck et al.
Chem Abs. 98:212,529c, Hawkins, "Conductometric Gas Sensor," 1983.
99:181,394u, Bodor, "Improved Delivery through Biological Membranes," 1983.
66:9530k, Gall, "Adjuvant Activity of Aliphatic Nitrogen Bases," 1967.

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