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恒河猴尿液中芦氟沙星及其代谢产物N-去甲基芦氟沙星和芦氟沙星亚砜的高效液相色谱分析及初步药代动力学研究

High-performance liquid chromatography and preliminary pharmacokinetics of rufloxacin and its metabolites, N-desmethylrufloxacin and rufloxacinsulfoxide, in urine of rhesus monkey Macaca mulatta.

作者信息

Vree T B, van den Biggelaar-Martea M, Peeters A, Imbimbo B P

机构信息

Department of Clinical Pharmacy, Academic Hospital Nijmegen Sint Radboud, Netherlands.

出版信息

J Chromatogr. 1992 Jan 3;573(1):168-72. doi: 10.1016/0378-4347(92)80493-a.

Abstract

A gradient high-performance liquid chromatographic method for the quantification of rufloxacin and two of its metabolites in urine, N-desmethylrufloxacin and rufloxacinsulfoxide, has been developed and validated. Monkey urine samples were diluted ten times with distilled water and 20 microliters were injected onto a Cp Spher 5-ODS column, 5 microns particle size. The mobile phase was a mixture of 4% acetonitrile and 96% buffer at time 0, which changed linearly over 37 min to 26% acetonitrile and 74% buffer. Detection was achieved at 246 nm. The limit of detection of the three compounds was 0.50 microgram/ml. An example of a pharmacokinetic study of rufloxacin and its metabolites in monkeys is shown.

摘要

已开发并验证了一种梯度高效液相色谱法,用于定量测定尿液中的芦氟沙星及其两种代谢物N-去甲基芦氟沙星和芦氟沙星亚砜。将猴尿样品用蒸馏水稀释10倍,取20微升注入粒径为5微米的Cp Spher 5-ODS柱。流动相在时间0时为4%乙腈和96%缓冲液的混合物,在37分钟内线性变化为26%乙腈和74%缓冲液。在246纳米处进行检测。三种化合物的检测限为0.50微克/毫升。给出了芦氟沙星及其代谢物在猴体内的药代动力学研究示例。

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