Broly F, Libersa C, Lhermitte M
Laboratoire de Pharmacologie, Faculté de Medecine de Lille, France.
J Chromatogr. 1988 Oct 14;431(2):369-78. doi: 10.1016/s0378-4347(00)83105-9.
A simple high-performance liquid chromatographic assay, using fluorescence detection, is described for determining simultaneously the production of the two major hydroxylated metabolites of mexiletine in human liver microsomes. The detection limits of hydroxymethylmexiletine and p-hydroxymexiletine are 0.35 and 0.08 nmol/ml, respectively. The assay is specific, reproducible and allows the simultaneous kinetic characterization of the reactions in small amounts of liver tissue. The assay may be used to acquire a better knowledge of the kinetic behaviour of mexiletine and of its metabolites, and to investigate if the large inter-individual variations of the mexiletine pharmacokinetics are of metabolic origin, due to variations of its hydroxylation processes.
本文描述了一种简单的高效液相色谱分析法，采用荧光检测，可同时测定人肝微粒体中美西律两种主要羟基化代谢产物的生成量。羟甲基美西律和对羟基美西律的检测限分别为0.35和0.08 nmol/ml。该分析方法具有特异性、可重复性，能够对少量肝组织中的反应进行同时动力学表征。该分析方法可用于更好地了解美西律及其代谢产物的动力学行为，并研究美西律药代动力学的个体间巨大差异是否源于其羟基化过程的变化而具有代谢起源。
