Formulations with hydrophobic permeation enhancers
AssigneeAlza Corporation
InventorsEun Soo Lee, Su Il Yum, Michel J. N. Cormier
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Abstract
This invention is directed to a novel formulation for effectively utilizing hydrophobic permeation enhancers for the increased permeability of active agents through the skin or mucosa along with reduction of the lag time between application of the active agent and attainment of a therapeutically effective agent flux, with little or no irritation to the host. The invention is directed to compositions containing a hydrophobic permeation enhancer, which permeation enhancer has been micronized and stabilized in an inert carrier such as water. These compositions can be combined with a biologically active agent to provide enhanced permeability of the active agent to the skin or mucosa.
Claims7
A formulation for the transdermal delivery of corticosteroid at a therapeutically effective rate to the skin of a host and with little or no irritation to the host, which formulation comprises:
- (a) corticosteroid;
- (b) 0.1-50 wt % of a hydrophobic permeation enhancer selected from the group consisting of glycerol monolaurate, glycerol monooleate, glycerol monolinoleate, sorbitan monolaurate, sorbitan dilaurate, sorbitan trilaurate, sorbitan monooleate, sorbitan dioleate, and sorbitan trioleate, the permeation enhancer being in microparticles of from about 0.01 to about 1000 microns in diameter;
- (c) 0.1-5 wt % of a micronization stabilizer selected from the group consisting of sodium deoxycholate, sodium cholate, sodium dodecylsulfate, and sodium benzoate;
- and
- (d) an inert carrier.
Dependencies are inferred from the claim text.