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~3H-氧甲基山豆根碱的药物代谢动力学研究

Pharmacokinetic Studies on Tritium-O-methyldauricine

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【作者】 代宗顺; 李志敏; 李健; 胡崇家;

【Author】 Dai Zhongshun, Li Zhimin, Li Jian, Hu ChongjiaDepartment of Pharmacology, Faculty of Premedical andPreclinical Sciences, Wuhan Medical College, Wuhan

【机构】 武汉医学院基础医学部临床药理研究室; 北京四○一研究所; 武汉医学院药理教研室; 武汉医学院药理教研室;

【摘要】 本文报道3H-氧甲基山豆根碱的药物代谢动力学。大白鼠一次灌胃给药后,血浆药物浓度对时问的曲线符合开放式二室模型。其主要参数是:t1/2Ka=0.203hr t1/2a=0.481hr,t1/2β=9.429hr, K12=0.582hr-1, K21=0.799hr-1, K10=0.132hr-1, Tmax=0.61hr, Cmax=0.461μg/m1。收集48小时内大白鼠的粪、尿测得排出的放射性分别为21.59%和1.97%

【Abstract】 The pharmacokinetics of tritium-O-methyldauricine was studied in rats. The logarithm of drug concentration in plasma versus time curve after oral administration was fitted to a two-compartment open model with first order elimination. The pharmacokinetic parameters are as follows: Distribution half-life 0.48hr, Elimination half-life 9.43hr, Absorption half-life 0.2hr, Elimination rate constant 0.132/hr, Posi-tive transfer rate constant 0.582/hr, Converse transfer rate constant 0.799/hr, Peak concentration 0.461ng/ml, Time of peak concentration 0.6lhr. After oral administration, the radioactivities excreted in urine and faeces within 48 hours were determined directly ia rats. The radioactivities excreted in faeces and urine were 21.59% and 1.97% respectively.

  • 【文献出处】 武汉医学院学报 , 编辑部邮箱 ,1984年05期
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