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本文报告氧化苦参碱在动物体内的吸收、分布、排泄和转化的动态情况。静脉注射氧化苦参碱后,大鼠血浆中的药物浓度呈双相指数下降,符合开放式二室模型(T 1/2(a)=5.0min,T 1/2(β)=27.0 min)。氧化苦参碱经不同途径给药,药物在体内的转化有较大的差异。肌肉注射氧化苦参碱后,药物在大鼠组织中的分布以氧化苦参碱为主,尿中排出大量原形药,24小时内排出氧化苦参碱占排出总量的85.3％,说明肌肉注射后药物在体内转化较少。口服后,氧化苦参碱在大鼠或小鼠胃肠道中逐渐转化成苦参碱被吸收,药物在大鼠组织中的分布,苦参碱的含量比氧化苦参碱高,尿排泄也以苦参碱为主,24小时内占排出总量的80.1％,人口服氧化苦参碱后,屎排泄苦参碱比氧化苦参碱高。实验证明,苦参碱可能是平喘作用的有效形式。
This article reports the dynamics of oxymatrine absorption, distribution, excretion and conversion in animals. After intravenous injection of oxymatrine, the drug concentration in rat plasma showed a biphasic exponential decline, in line with the open two-compartment model (T 1/2 (a) = 5.0 min, T 1/2 (β) = 27.0 min) . Oxymatrine by different routes of administration, the drug in vivo conversion have greater differences. Intramuscular injection of oxymatrine, the distribution of drugs in rat tissue to oxymatrine-based, urinary excretion of a large number of prototype drugs, oxytocin within 24 hours accounted for 85.3% of the total discharge, indicating that intramuscular injection Post-drug conversion in the body less. Oral administration, oxymatrine gradually transformed into matrine in rats or mice gastrointestinal tract is absorbed, the distribution of drugs in the rat tissue, matrine content higher than oxymatrine, urinary excretion also Matrine-based, within 24 hours accounted for 80.1% of the total discharge, oral administration of oxymatrine, feces excretion of matrine than oxymatrine high. Experiments show that matrine may be an effective form of antiasthmatic effect.