Rudolphi C, Blaschke G
Institute of Pharmaceutical Chemistry, University of Münster, Germany.
J Chromatogr B Biomed Appl. 1995 Jan 20;663(2):315-26. doi: 10.1016/0378-4347(94)00466-i.
A reversed-phase high-performance liquid chromatographic method to separate meptazinol and its phase I metabolites has been developed using a LiChrosper 100 CN column and a mobile phase of trimethylammoniumacetate buffer (pH 5.5)-acetonitrile-methanol. Quantification of meptazinol and N-desmethylmeptazinol in biological samples was achieved by extraction with organic solvents and chromatographic analysis (detection limit 0.4 and 0.25 micrograms/ml, respectively). Afterwards the enantiomeric ratio of the two compounds was determined on a Chiral AGP column with a mobile phase of phosphate buffer (pH 7.0)-acetonitrile (alpha = 1.29 and 1.49, respectively). In-vitro metabolism data after incubation of the racemic compound and the enantiomers with liver supernatant and microsomes of different species are presented. Finally urinary data of two volunteers after oral application of the racemic drug were determined.
已开发出一种反相高效液相色谱法，使用LiChrosper 100 CN柱和醋酸三甲基铵缓冲液（pH 5.5）-乙腈-甲醇流动相来分离美普他酚及其I相代谢物。通过有机溶剂萃取和色谱分析实现生物样品中美普他酚和N-去甲基美普他酚的定量（检测限分别为0.4和0.25微克/毫升）。之后，在Chiral AGP柱上使用磷酸盐缓冲液（pH 7.0）-乙腈流动相测定这两种化合物的对映体比例（α分别为1.29和1.49）。给出了外消旋化合物和对映体与不同物种的肝脏上清液和微粒体孵育后的体外代谢数据。最后测定了两名志愿者口服外消旋药物后的尿液数据。
