Transdermal delivery system comprising buprenorphine

摘要

The invention relates to transdermal therapeutic system for the transdermal administration of buprenorphine, comprising a buprenorphine-containing self-adhesive layer structure comprising
A) a buprenorphine-impermeable backing layer, andB) a buprenorphine-containing pressure-sensitive adhesive layer on said buprenorphine-impermeable backing layer, the adhesive layer comprising
a) at least one polymer-based pressure-sensitive adhesive,b) an analgesically effective amount of buprenorphine base or a pharmaceutically acceptable salt thereof, andc) a carboxylic acid selected from the group consisting of oleic acid, linoleic acid and linolenic acid, levulinic acid and mixtures thereof, in an amount sufficient so that said analgesically effective amount of buprenorphine is solubilized therein to form a mixture, and the carboxylic acid buprenorphine mixture forms dispersed deposits in the said pressure-sensitive adhesive,

wherein said buprenorphine-containing pressure-sensitive adhesive layer is the skin contact layer.

主权项

1. A method of treating pain in a patient comprising applying a transdermal therapeutic system for the transdermal administration of buprenorphine to the skin of the patient, wherein the transdermal therapeutic system comprises a buprenorphine-containing self-adhesive layer structure comprising
a. a buprenorphine-impermeable backing layer, and b. a buprenorphine-containing pressure-sensitive adhesive layer on the buprenorphine-impermeable backing layer, the adhesive layer comprising
i. at least one polymer-based pressure-sensitive adhesive based on polysiloxanes or polyisobutylenes,ii. an analgesically effective amount of buprenorphine base or a pharmaceutically acceptable salt thereof, andiii. a carboxylic acid selected from the group consisting of oleic acid, linoleic acid, linolenic acid, levulinic acid and mixtures thereof, in an amount sufficient so that the analgesically effective amount of buprenorphine is solubilized therein to form a mixture, and the carboxylic acid buprenorphine mixture forms dispersed deposits in the pressure-sensitive adhesive,
wherein the buprenorphine-containing pressure-sensitive adhesive layer is the skin contact layer; and wherein the transdermal therapeutic system is applied on the skin of the patient for about 168 hours;wherein the transdermal therapeutic system provides a size of the buprenorphine-containing pressure-sensitive adhesive layer providing an area of release ranging from about 1 cm2 to about 4.8 cm2 and contains an amount of the buprenorphine from about 1 mg to about 4 mg buprenorphine base or an equimolar amount of a pharmaceutically acceptable salt thereof, andwherein the transdermal therapeutic system provides a mean AUCt per area of release of more than 1,700 pg.hr/ml-cm2 over about 168 hours of administration after a single-dose administration to a subject population.