TRANSDERMAL ADMINISTRATION OF HYDROPHILIC DRUGS USING PERMEATION ENHANCER COMPOSITION

Methods, formulations, and drug delivery systems are provided for enhancing the flux of a transdermally administered hydrophilic drug using a basic permeation enhancer composition. The enhancer composition contains an inorganic hydroxide and a weaker, nitrogenous base, wherein the bases are selected...

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Hauptverfasser: JACOBSON ERIC, LUO ERIC C, HICKEY ALAN T.J, HSU TSUNG-MIN, GRICENKO NICOLE T
Format: Patent
Sprache:eng
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Zusammenfassung:Methods, formulations, and drug delivery systems are provided for enhancing the flux of a transdermally administered hydrophilic drug using a basic permeation enhancer composition. The enhancer composition contains an inorganic hydroxide and a weaker, nitrogenous base, wherein the bases are selected such that a 0.1M aqueous solution of the nitrogenous base has a pH that is about 1.0 to about 6.5 lower than the pH of a 0.1M aqueous solution of the inorganic hydroxide. Additionally, the molar ratio of the nitrogenous base to the inorganic hydroxide in the enhancer composition is in the range of about 0.5n:1 to about 20n:1, where n is the number of hydroxide ions per molecule of the inorganic hydroxide.