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Stereoselective toxicokinetics and tissue distribution of ethofumesate in rabbits
Author(s) -
Zhu Wentao,
Dang Ziheng,
Qiu Jing,
Lv Chunguang,
Jia Guifang,
Li Li,
Zhou Zhiqiang
Publication year - 2007
Publication title -
chirality
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.43
H-Index - 77
eISSN - 1520-636X
pISSN - 0899-0042
DOI - 10.1002/chir.20428
Subject(s) - chemistry , stereoselectivity , enantiomer , toxicokinetics , chromatography , pharmacokinetics , high performance liquid chromatography , chiral column chromatography , stereochemistry , pharmacology , organic chemistry , toxicity , catalysis , medicine
The stereoselective toxicokinetics of ethofumesate enantiomers following a single intravenous (i.v.) administration at doses of 30 mg/kg were investigated in rabbits. Plasma concentrations of (+)‐ and (−)‐ethofumesate were analyzed by a validated chiral HPLC method that involved extraction of plasma with organic solvent followed by separation on a cellulose‐Tris‐(3,5‐dimethylphenylcarbamate)‐based chiral column and quantification by UV absorbance at 230 nm. Plasma concentration‐time curves after i.v. administration were best described by an open two‐compartment model. The concentration of the (−)‐enantiomer decreased more rapidly than that of the (+)‐enantiomer. Significant differences in toxicokinetic parameters between the two enantiomers indicated that stereoselective behavior occurred with the (−)‐enantiomer being preferentially metabolized and eliminated. Chirality 19:632–637, 2007 © 2007 Wiley‐Liss, Inc.