苦参碱的代谢动力学研究

Pharmacokinctic Study of Matrine

家兔实验表明:iv苦参碱,血药浓度—时间曲线呈双指数型,符合开放式二室模型。T1/2α为1.37min,T1/2β为76.58min,CI为23.59ml/min/kg,Vd为2.61L/kg。12h尿及胆汁的原形药累积排出量分别为给药量的9.39％及0.37％。大鼠实验表明:ig苦参碱,组织中含量多少,依次为肾、肝、肺、脑、心及血。48h尿、24h粪及12h胆汁的原形药累积排出量分别为给药量的53.7％、0.36％和0.27％。

The pharmacokinetic study of matrine was carried out by means of colorimetry. Matrine was injected intravenously into rabbits and the curve of blood concentration vs time was described using an open two-comparement model. The pharmacokinetic parameters were A, 62.57μg/ml; B, l4.22μg/ml; α, 0.5045min^(-1); β, 0.00905min^(-1); T1/2α, 1.37min; T1/2β, 76.58min; Cl, 23.59ml/min/kg; Vc, 0.52L/kg; Vd, 2.61L/kg. The content of matrine in rat' various tissue, after administered orally, was in turn the kidney, liver, lung, brain, heart and blood. It indicated that the drug could distribute extensively to tissues, even passing through the blood-brain barrier. Matrine was given orally to rats, The cumulative quantity of exeretion of unchange drugs was 53.73% of the total dose in urine in 48h, 0.36% in feces in 24h and 0.27% in bile in 12h, and that,after administered intravenously, in rabbits was 9.39% of the total dose in urine and 0.37,% in bile in 12h.