Effects of vehicle on the uptake and elimination kinetics of capsaicinoids in human skin in vivo英文电子书.pdf

Toxicology and Applied Pharmacology 200 (2004) 73– 81 /locate/ytaap Effects of vehicle on the uptake and elimination kinetics of capsaicinoids in human skin in vivo Lynn K. Pershing, a,* Christopher A. Reilly,b Judy L. Corlett, a and Dennis J. Crouchb a Department of Dermatology, University of Utah School of Medicine, Salt Lake City, UT 84132, USA b Center for Human Toxicology, Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, UT 84132, USA Received 5 January 2004; accepted 30 March 2004 Available online 14 May 2004 Abstract While the physiologic and molecular effects of capsaicinoids have been extensively studied in various model systems by a variety of administration routes, little is known about the uptake and elimination kinetic profiles in human skin following topical exposure. The present study evaluated the uptake and elimination kinetics of capsaicinoids in human stratum corneum following a single topical exposure to 3% solutions containing 55% capsaicin, 35% dihydrocapsaicin, and 10% other analogues prepared in three vehicles: mineral oil (MO), propylene glycol (PG), and isopropyl alcohol (IPA). Capsaicinoid solutions were evaluated simultaneously in a random application pattern on the volar forearms of 12 subjects using a small, single 150-Ag dose. Capsaicin and dihydrocapsaicin were recovered from human skin using commercial adhesive discs to harvest stratum corneum from treated sites. Capsaicinoids were extracted from the stratum corneum-adhesive discs and quantified by liquid chromatography/mass spectroscopy (LC/MS). Both caps