Sorbitan esters as skin permeation enhancers
AssigneeTheratech, Inc.
InventorsSonia Heiber, Dinesh Patel, Charles D. Ebert
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Abstract
Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a sorbitan ester in addition to the selected pharmacologically active agent, and may also contain a C.sub.1 -C.sub.4 aliphatic alcohol. Methods and transdermal drug delivery systems for using the compositions are also provided.
Claims21
A method for enhancing the rate of penetration of a pharmacologically active agent through the skin, comprising applying to a selected area of intact skin:
- (a) a therapeutically effective amount of the pharmacologically active agent;
- and (b) a permeation enhancer consisting essentially of a sorbitan ester having the structural formula ##STR2## wherein R.sub.1 has the formula --O(CO)R', R' is selected from the group consisting of saturated, mono-unsaturated, di-unsaturated, or tri-unsaturated aliphatic hydrocarbon substituents of 7 to 21 carbon atoms optionally containing 1 to 3 hydroxyl groups, and R.sub.2 and R.sub.3 are independently selected from the group consisting of hydroxyl and --O(CO)R'.
A method for enhancing the rate of penetration of a pharmacologically active agent through the skin, comprising applying to a selected area of intact skin:
- (a) a therapeutically effective amount of the pharmacologically active agent;
- and (b) a permeation enhancer consisting essentially of a sorbitan ester having the structural formula ##STR3## wherein R.sub.1 has the formula --O(CO)R', R' is selected from the group consisting of saturated, mono-unsaturated, di-unsaturated, or tri-unsaturated aliphatic hydrocarbon substituents of 7 to 21 carbon atoms optionally containing 1 to 3 hydroxyl groups, and R.sub.2 and R.sub.3 are independently selected from the group consisting of hydroxyl and--O(CO)R', and a C.sub.1 -C.sub.4 aliphatic alcohol.
A composition of matter for the transdermal administration of a pharmaceutically active agent, comprising:
- (a) a therapeutically effective amount of the pharmacologically active agent;
- and (b) a permeation enhancer consisting essentially of a sorbitan ester having the structural formula ##STR4## wherein R.sub.1 has the formula --O(CO)R', R' is selected from the group consisting of saturated, mono-unsaturated, di-unsaturated, or tri-unsaturated aliphatic hydrocarbon substitutuents of 7 to 21 carbon atoms optionally containing 1 to 3 hydroxyl groups, and R.sub.2 and R.sub.3 are independently selected from the group consisting of hydroxyl and --O(CO)R'.
A composition of matter for the transdermal administration of a pharmacologically active agent comprising:
- (a) a therapeutically effective amount of the pharmacologically active agent;
- and (b) a permeation enhancer consisting essentially of a sorbitan ester having the structural formula ##STR6## wherein R.sub.1 has the formula --O(CO)R', R' is selected from the group consisting of saturated, mono-unsaturated, di-unsaturated, or tri-unsaturated aliphatic hydrocarbon substituents of 7 t 21 carbon atoms optionally containing 1 to 3 hydroxyl groups, and R.sub.2 and R.sub. are independently selected from the group consisting of hydroxyl and --O(CO)R', and a C.sub.1 -C.sub.4 aliphatic alcohol.
Dependencies are inferred from the claim text.