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目的:研究间尼索地平对映体在人肝微粒体中的酶促反应动力学,计算其酶促反应动力学参数,并对R型和S型间尼索地平的酶促反应动力学过程进行比较。方法:以尼莫地平为内标,建立液相色谱-质谱联用(LC-MS)方法分别测定体外孵育人肝微粒体后R型、S型间尼索地平含量,采用Linewrave-Burk作图法处理数据,以底物消除法计算酶促动力学参数Km和Vmax。结果:R-间尼索地平Km=71.67μmol·L-1,Vmax=2.513μmol·min-1·mg-1;S-间尼索地平Km=72.86μmol·L-1,Vmax=2.534μmol·min-1·mg-1。结论:该方法简单、可靠,适用于间尼索地平的体外代谢研究,R型和S型间尼索地平的酶促反应动力学过程无明显差异。
OBJECTIVE: To study the enzymatic reaction kinetics of enantiomeric enantiomers of human nisoldipine in human liver microsomes, and to calculate the kinetic parameters of enzymatic reaction. The kinetics of the enzymatic reaction of nisoldipine between R type and S type Compare. Methods: Nimodipine was used as an internal standard to establish a liquid chromatography-mass spectrometry (LC-MS) method to measure the content of nisoldipine in R-type and S-type after in vitro incubation of human liver microsome. Linewrave-Burk Data were processed and substrate kinetic parameters Km and Vmax were calculated by substrate subtraction. Results: Km = 71.67μmol·L-1 and Vmax = 2.513μmol · min-1 · mg-1 for R-nisoldipine, Km = 72.86μmol·L-1 and Vmax = 2.534μmol · min-1 · mg-1. CONCLUSION: This method is simple and reliable and is suitable for in vitro metabolism studies of nisoldipine. There is no significant difference in the kinetic process of nisoldipine between R type and S type.