应用气——质联用等法对青蒿酯钠体内命运的研究

本文报道用气质联用(GC-MS)、高效液相色谱(HPLC),薄层扫描(TLCS)等法研究青蒿酯钠的命运。结果提示:青蒿酯钠在体内可转化为具有α(RT为5.2 min)、β(RT为604 min)两个异构体的双氢青蒿素。已经证明双氢青蒿素的β体更为有效,因此双氢青蒿素可视为青蒿酯钠的有效代谢物,其在体内动力学为一级速率反应,具有一房室模型特征,半衰期t_1/2为10min,表观分布容积Vd为0.36 L/kg。青蒿酯钠等药物具有诱导肝药酶的作用,首过效应明显。

STUDIES ON THE FATE OF ARTESUNATE BY GC-MS, HPLC AND TLCS METHODS.

This paper reports the fate of Artesunate studied by using GCMS, HPLC and TLCS methods.The result of experiments showed that Artesunate may be transformed in vivo in rats, rabbits and dogs into dihydroartemisinine which contains both epimers (α, RT=5.2 rain; β, RT=6.4 min). It has been shown that dihydroartemisinine is even more effective than Artesunate. Therefore, it can be considered as an active metabolite of Artesunate.The results showed a linear relationship between the logarithm of plasma dihydroartemisinine concentration versus time after i. v. administration of Artesunate in dogs. The pharmacokinetic parameters were as follows: T_1/2=10 min; V_d=0.36L/kg.Artesunate and artemisinine derivatives were shown to have inductive effect on hepatomicrosomal enzymes. It showed a very remarkble first pass effect.