Enhancing transdermal administration of hydrophilic drugs

Details Enhancing transdermal administration of hydrophilic drugs Enhancing transdermal administration of hydrophilic drugs

A - Human Necessities

61

F

A61F 13/00 (2006.01)

Patent

CA 2542753

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.

La présente invention concerne des procédés, des formulations et des systèmes d'administration de médicaments permettant de renforcer le flux d'un médicament hydrophile administré par voie transdermique, grâce à une composition basique renforçant la perméation. Cette composition contient un hydroxyde inorganique, et une base azotée, plus faible. Les bases sont choisies de façon qu'une solution aqueuse à 0,1M de la base azotée présente un pH d'environ 1.0 à environ 6.5 inférieur à celui de la solution aqueuse à 0,1M de l'hydroxyde inorganique. En outre, le rapport molaire de la base azotée sur l'hydroxyde inorganique dans la composition renforçatrice se situe dans une place d'environ 0,5n:1 à environ 20m:1, "n" étant le nombre d'ions hydroxyde par molécule d'hydroxyde inorganique.

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