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Stereoselective pharmacokinetics of ornidazole after intravenous administration of individual enantiomers and the racemate

All Rights Reserved. Stereoselective pharmacokinetics of ornidazole after intravenous administration of individual enantiomers and the racemate. Chen, Yan; Liu, Xiao Quan; Zhong, Jiao; Zhao, Xiaoping; Wang, Yongsheng; Wang, Guangji (Key Laboratory of Drug Metabolism & Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Peop. Rep. China). Chirality, 18(10), 799-802 (English) 2006 Wiley-Liss, Inc. CODEN: CHRLEP. ISSN: 0899-0042. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The pharmacokinetics of ornidazole (ONZ) were investigated following i.v. administration of racemic mixt. and individual enantiomers in beagle dogs. Plasma concns. of ONZ enantiomers were analyzed by chiral high-performance liq. chromatog. (HPLC) on a Chiralcel OB-H column with quantification by UV at 310 nm. Notably, the mean plasma levels of (-)-ONZ were higher in the elimination phase than those of (+)-ONZ. (-)-ONZ also exhibited greater t1/2, MRT, AUC0-t and smaller CL, than those of its antipode. The area under the plasma concn.-time curve (AUC0-t) of (-)-ONZ was about 1.2 times as high as that of (+)-ONZ. (+)-ONZ total body clearance (CL) was 1.4 times than its optical antipode.There are some commonly used reagents with their cas registry numbers 166734-83-4 and 166734-80-1 in this article. When given sep., there were significant differences in the values of AUC0-￥ and CL between ONZ enantiomers (P < 0.05), indicating that elimination of (+)-ONZ was more rapid than that of (-)-ONZ. No significant differences were found between the ests. of the pharmacokinetic parameters of (+)-ONZ or (-)-ONZ, obtained following administration as the individual and as a racemic mixt. This study demonstrates that the elimination of ONZ enantiomers is stereoselective and chiral inversion and enantiomer/enantiomer interaction do not occur when the enantiomers are given sep. and as racemic mixt. .