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传统观念认为小檗碱口服吸收差,而近年来,临床口服小檗碱用来治疗心律失常及充血性心衰.为解决其中的矛盾,本实验建立了HPLC方法(最低检测限为2μg·L~(-1))研究Beagle狗po和iv小檗碱的药代动力学、100 mg静脉注射的药—时曲线符合二室模型,K.为10.18 h~(-1),T_(1/2u)为0·15·h~(-1)T_1/2β为12.59·h~(-1),CL为60.70 L·h~(-1),AUC达1979.31 μg·L~(-1)V_d为699.53L。280 mg·kg~(-1)组发生呕吐·仅一狗可计算P—K参数,T_(max)为3.71h,C_(max)为15.46 μg·L~(-1),AUC为777.29μg·h~(-1)·L~(-1).T T_(1/za)0.63 h·T_(1/z)el34.82h,V_a为125.41L,K.为0.02·h~(-1),CL为2.64 L·h~(-1),45 mg·kg~(-1)一次口服以及45 mg·kg~(-1)Bid连续给药1wk的血药浓度都在10μg·L~(-1)以下。700 mg·kg~(-1)组因发生严重呕吐.腹泻,药物吸收差.血浓度在10 μg·L~(-1)以下,不能计算P—K参数.
The traditional concept that oral absorption of berberine poor, and in recent years, clinical oral berberine for the treatment of arrhythmia and congestive heart failure.In order to solve the contradiction, the experiment established the HPLC method (the minimum detection limit of 2μg · L ~ (-1)) to study the pharmacokinetics of po and berberine in Beagle dogs. The drug-time curve of 100 mg intravenous injection conformed to the two-compartment model with K values of 10.18 h -1 and T 1 / 2u) was 0.159 h -1, the T_1 / 2β was 12.59 h -1, the CL was 60.70 L · h -1, and the AUC was 1979.31 μg · L -1 V_d 699.53L. Vomiting occurred in the 280 mg · kg -1 group. P-K parameters were calculated for only one dog with a T max of 3.71 h and a C max of 15.46 μg · L -1 with an AUC of 777.29 μg · H -1 · L -1 · T T 1 / za · 0.63 h · T 1 / z · el 34.82h, V_a was 125.41L and K was 0.02 · h -1 ), CL was 2.64 L · h -1, 45 mg · kg -1 once orally and 45 mg · kg -1 bid for continuous administration of 1 wk for 10 weeks. (-1) or less. Severe vomiting, diarrhea and poor drug absorption were found in 700 mg · kg -1 group, P-K parameters could not be calculated when blood concentration was under 10 μg · L -1.