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目的:研究延胡索乙素单体及延胡索提取物中延胡索乙素在大鼠肝微粒体中的酶促反应动力学,考察单体及提取物中延胡索乙素在大鼠肝微粒体代谢的差异。方法:采用高效液相法测定单体及延胡索提取物中延胡索乙素在体外代谢系统中代谢,计算酶动力学参数。结果:延胡索乙素单体在大鼠肝微粒体内代谢反应的最大反应速率Vmax、米氏常数Km和肝内消除率CLint分别为(4.19±0.87)μmol/L.(min.mg)、(172.68±19.24)μmol/L、(0.024±0.008)L.(min.mg);延胡索提取物中延胡索乙素在大鼠肝微粒体内代谢反应的最大速率Vmax、米氏常数Km和肝内消除率CLint分别为(0.12±0.02)μmol/L.(min.mg)、(5.44±1.74)μmol/L、(0.022±0.006)L.(min.mg)。结论:延胡索提取物中的延胡索乙素与延胡索乙素单体在大鼠肝微粒体中的代谢动力学有差别,这种差别可能是提取物中其它成份对代谢酶的作用引起的。
OBJECTIVE: To study the enzymatic kinetics of tetrahydropalmatine in rat liver microsomes of tetrahydropalmatine and tetrahydropalmatine extract, and to investigate the differences of the metabolism of tetrahydropalmatine in rat liver microsomes. Methods: The HPLC method was used to determine the metabolites of tetrahydropalmatine in the in vitro metabolic system and the enzyme kinetic parameters. Results: The maximal reaction rate (Vmax), Km (Mm) and CLint (hepatic clearance rate) of tetrahydropalmatine monohydrate in rat liver microsomes were (4.19 ± 0.87) μmol / L ± 19.24) μmol / L and (0.024 ± 0.008) L (min.mg). The maximal rate of metabolic reaction of tetrahydropalmatine in rat liver microsomes Vmax, Km and CLint (0.12 ± 0.02) μmol / L (min.mg), (5.44 ± 1.74) μmol / L, (0.022 ± 0.006) L. (min.mg), respectively. CONCLUSION: There is a difference in the pharmacokinetics of tetrahydropalmatine and tetrahydropalmatine in rat liver microsomes. This difference may be caused by the action of other components in the extract on metabolic enzymes.