Pharmacokinetics of barnidipine hydrochloride, a new dihydropyridine calcium channel blocker, in the rat, dog and human

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
T TeramuraK Hashimoto

Abstract

1. The pharmacokinetics of a new calcium antagonist barnidipine hydrochloride, a stereochemically pure enantiomer, was studied after intravenous and oral dosing to the rat and dog, and oral to man. 2. After intravenous dosing, plasma concentrations of barnidipine hydrochloride declined bi-exponentially with the terminal half-lives of 0.6 h in the rat and 4.1 h in the dog. The blood clearance was 5.2 l/h/kg in the rat and 3.3 l/h/kg in the dog, and was comparable with hepatic blood flow in both species. 3. After oral dosing, plasma concentrations of barnidipine hydrochloride peaked rapidly (0.3-0.4 h in the rat and dog, 1.0-1.6 h in man). Cmax and AUC rose non-linearly with increasing doses in all three species. 4. The absolute bioavailability was low (11-18% in the rat and 6-9% in the dog), suggesting a marked first-pass metabolism.

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Citations

Jan 25, 2003·Journal of Biochemical and Biophysical Methods·Nobuo Inotsume, Masahiro Nakano
Dec 30, 1998·Journal of Chromatography. B, Biomedical Sciences and Applications·M PawulaK N Cheng
Feb 12, 1998·Environmental Health Perspectives·J G SarverK Bachmann
Jul 5, 2005·Expert Opinion on Investigational Drugs·D F Cummins
Sep 1, 2006·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·Toshiro NiwaAkira Takagi

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