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本文报道~3H-五味子酯甲在小鼠体内的药物动力学。给与小鼠静脉注射~3H-五味子酯甲23mg/kg后分析其药时曲线,属于开放型二室模型,其动力学参数为;t_1/2 α0.133h,t_1/2 β 18.14h,K_(12)4.24h~(-1),K_(21)0.274小时~(-1),Kel 0.735h~(-1),Vc 8.2ml/kg,Vd155.7ml/kg,C_16.027ml/h。灌胃组药时曲线为单室模型,其动力学参数为:t_(1/2)Ka5.8小时,t_(1/2)Ke20.6h,T_(max)14.1h,C_(max)20213dpm/ml,C_14.21ml/h,F45.36%。从动力学参数看,静脉给药分布相半衰期仅7.98分钟,而消除相t_(1/2)为18.14小时,说明药物在血液中分布迅速、消除缓慢。小鼠灌胃给药后14.1小时才达到高峰,72小时内的生物利用度仅为45.36%,说明该药物在胃肠道吸收差,只有近一半的药物能被机体吸收利用,提示有必要改进剂型。小鼠体内药物分布实验表明,五味子酯甲主要分
This paper reports the ~ 3H-Schisandra ester A pharmacokinetics in mice. The pharmacokinetic parameters of ~ 3H-Schisandrins A (23 mg / kg) given to mice were analyzed and the pharmacokinetic parameters were t_1 / 2 α0.133h, t_1 / 2 β 18.14h, K_ (12) 4.24h ~ (-1), K_ (21) 0.274h ~ (-1), Kel 0.735h ~ (-1), Vc 8.2ml / kg, Vd155.7ml / kg, C_16.027ml / h. The pharmacokinetic parameters of t_ (1/2) Ka5.8h, t_ (1/2) Ke20.6h, T_ (max) 14.1h, C_ (max) 20213dpm /ml,C_14.21ml/h,F45.36%. From the kinetic parameters, intravenous drug delivery phase half-life of only 7.98 minutes, and eliminate phase t_ (1/2) was 18.14 hours, indicating rapid distribution of drugs in the blood, eliminate slowly. The mice reached the peak 14.1 hours after intragastric administration, with a bioavailability of only 45.36% within 72 hours, indicating that the drug absorbed poorly in the gastrointestinal tract and that only about half of the drug was absorbed by the body, suggesting that improvement was necessary Formulation. In vivo drug distribution in mice showed that Schisandra ester A main points