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浙江大学学报（医学版）
Journal of ZheJiang University(Medical Science)  1999, Vol. 28 Issue (6): 265-267    DOI: 10.3785/j.issn.1008-9292.1999.06.008
    
Determination of the Stereoselectivity for Phase I Metabolism of S-(-)-and R-(+)-Ofloxacin by RP-HPLC
ZENG Su, LI Yan
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031
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Abstract  

Objective:To determine the stereoselectivity for phase I metabolism of S-(-)-and R-(+)-ofloxacin (OFLX) in vitro.Methods:The curves of reaction time vs.metabolites formed and the parameters of enzymatic kinetics for both enantiomers were determined by using reserve phase high performance liquid chromatography after S-(-)-or R-(+)-OFLX was incubated with rat liver microsome respectively.Results:The formation rate of metabolites for S-(-)-OFLX was faster than that for R (+) OFLX.There were significant differences between two enantiomers for their Vmax,Km and Clint.Conclusion:The phase I metabolism of S-(-)-and R-(+)-OFLX in rat liver microsome possessed stereoselectivity.

Key words： Ofloxacin      Stereoisomerism      Chromatography,high pressure liquid     
Received: 16 February 1998      Published: 25 November 1999
CLC:  R969.1  
  R962  
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ZENG Su
LI Yan
Cite this article:

ZENG Su, LI Yan. Determination of the Stereoselectivity for Phase I Metabolism of S-(-)-and R-(+)-Ofloxacin by RP-HPLC. Journal of ZheJiang University(Medical Science), 1999, 28(6): 265-267.

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https://www.zjujournals.com/med/10.3785/j.issn.1008-9292.1999.06.008     OR     https://www.zjujournals.com/med/Y1999/V28/I6/265


氧氟沙星I相代谢的立体选择性

目的:测定S-(-)-和R-(+)-氧氟沙星(OFLX)体外I相代谢的立体选择性。方法:分别将S-(-)-和R-(+)-OFLX与大鼠肝微粒体孵育后,采用反相高效液相色谱方法,测定代谢物随反应时间的生成曲线和酶动力学参数(最大反应速度、米氏常数,清除率)。结果:S-(-)-OFLX代谢物的生成量和生成速度均大于R-(+)-OFLX,两对映体的酶动力学参数也有显著差异。结论:S-(-)-OFLX和R-(+)-OFLX在大鼠肝微粒体中的I相代谢具有立体选择性。


关键词： 氧氟沙星,  立体异构体,  色谱法,  高压液相 
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