Penetration enhancers for transdermal delivery of systemic agent

Details Penetration enhancers for transdermal delivery of systemic agent Penetration enhancers for transdermal delivery of systemic agent

1986-11-19

1990-04-17

Robinson, Ellis P.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Web, sheet or filament bases; compositions of bandages; or...

514946, 514947, A61F 1300

Patent

active

049178962

ABSTRACT:
This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural 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, carboalkoxy, 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:
patent: 4147785 (1979-04-01), Langham
patent: 4492702 (1985-01-01), Sherlock
patent: 4628055 (1986-12-01), Sherlock
patent: 4666907 (1987-05-01), Fortin et al.
patent: 4694024 (1987-09-01), Weithmann et al.

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