Different pharmacokinetics of nicotine following intravenous administration of nicotine base and nicotine hydrogen tartarate in rats

Title
Different pharmacokinetics of nicotine following intravenous administration of nicotine base and nicotine hydrogen tartarate in rats
Authors
정병화정봉철정석재이민화심창구
Keywords
nicotine; Nicotine base; Nicotine hydrogen tartarate; Cotinine; Pharmacokinetics
Issue Date
2001-12
Publisher
Journal of controlled release : official journal of the Controlled Release Society
Citation
VOL 77, NO 3, 183-190
Abstract
Pharmacokinetics of nicotine was studied in rats following intravenous (i.v.) administration of nicotine base (NB) and nicotine hydrogen tartarate salt (NS) at a nicotine dose of 1 mg/ kg. The area under the plasma concentration–time curve (AUC), mean residence time (MRT), systemic clearance (CL), distribution volume at steady state (V ) and terminal plasma ss half-life (T ) of nicotine were compared between NB and NS. Compared to NS, NB exhibited higher and sustained 1 / 2,b plasma nicotine levels, thereby yielding significantly (P,0.05) larger AUC (66.3 vs. 27.7 mg ml /min), MRT (165.7 vs. 58.3 min), T (144.2 vs. 51.4 min) and a lower CL (18.3 vs. 46.3 ml/min per kg). The V was comparable between the two 1 / 2,b ss compounds. The metabolic conversion to cotinine from NS was threefold larger than that from NB. The plasma protein binding and distribution to blood cells were comparable between the compounds. The apparent partition coefficient (APC) of NS decreased as a function of its concentration, while that of NB remained nearly constant. Particles of different mean sizes were observed for the 1% (w/v) aqueous solutions of NS (388.6 nm) and NB (123.8 nm). Different metabolism and/or elimination between NB and NS appear to be mainly responsible for their different pharmacokinetics. Ó 2001 Elsevier Science B.V. All rights reserved.
URI
http://pubs.kist.re.kr/handle/201004/13793
ISSN
0168-3659
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