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应用还原型电化学极谱检测高效液相色谱法研究了青蒿酯的临床药代动力学。四位志愿者静脉注射青蒿酯(3.3—4.4mg/kg)后测得之青蒿酯及其活性代谢产物双氢青蒿素的主要药动学参数见表1。结果表明,静脉注射青蒿酯后原型药的血浆药-时曲线符合双指数函数,其血浆药物浓度在分布相衰减很快;到达消除相时,与其活性代谢产物双氢青蒿素比较已可忽略不计,故可认为在整个血浆药物浓度时程中双氢青蒿素占据主导地位。
The clinical pharmacokinetics of artesunate was studied by reduction-type electrochemical polarography and high performance liquid chromatography. The main pharmacokinetic parameters of artemisinin and its active metabolite, dihydroartemisinin, measured in four volunteers after intravenous injection of artesunate (3.3-4.4 mg / kg) are shown in Table 1. The results showed that the plasma drug-time curve of prototype drug after intravenous injection of artemisinin was in line with the double exponential function, and the plasma drug concentration attenuated quickly in the distribution phase. When reaching the elimination phase, the plasma metabolite dihydroartemisinin Neglected, it can be assumed that dihydroartemisinin predominates throughout the course of plasma drug concentration.