高效液相色谱法拆分盐酸哌醋甲酯的主要代谢产物盐酸哌醋甲酸

Enantioseparation of d-,l-Threo-Ritalinic Acids, the Metabolites of d-, l-Threo-Methylphenidates, by High Performance Liquid Chromatography

首次发展了一种新型快速的采用高效液相色谱直接拆分血液中手性药物盐酸哌醋甲酯(methylphenidate,MPH)的主要代谢产物盐酸哌醋甲酸(ritalinicacid,RA)的方法。实验中采用α1 酸性糖蛋白手性分离柱,以0 4%(体积分数)的醋酸水溶液(含体积分数0 1%的DMOA,pH3 4)为流动相,成功地对体外试验中RA的含量进行了分析,结果表明在人和狗的血浆中d MPH的代谢速度明显的快于l MPH。

A novel high performance liquid chromatographic method was developed and validated for the quantitative analysis of enantiomeric ritalinic acid (RA), the metabolites of d,lthreomethylphenidates (MPH), in human plasma and enzyme buffer solution. An α1acid glycoprotein column was used with mobile phase of 04% (v/v) acetic acid solution containing 01% (v/v) dimethyloctylamine (pH 34). The assay was successfully applied for in vitro analysis of enantiomeric ritalinic acids produced in human and dog plasma and dog liver. The results demonstrate that the esterase in human plasma metabolize dMPH faster than lMPH. 