葛根素及葛根提取物在大鼠体内药代动力学研究

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目的 考察葛根素及葛根提取物在大鼠体内的药代动力学差异.方法 大鼠分别灌胃给予葛根素(500 mg/kg)或葛根提取物(相当于葛根素500 mg/kg),在不同时间点采血,以对羟基苯甲酸为内标,应用高效液相色谱法测定葛根素血药浓度,采用DAS 2.0软件计算药动学参数.结果 葛根素及葛根提取物在大鼠体内药动学过程均符合二室模型,比较二者主要药动学参数:提取物组较葛根素组的AUC_(0-t)、C_(max)显著降低,T_(max)、t_(1/2z)、CL/F及V_z/F显著增加.结论 葛根素及葛根提取物的主要药动学参数具有显著性差异,葛根提取物中复杂成分的存在能影响其有效成分葛根素的体内药动学行为.“,”Purpose To compare pharmacokineics of puerarin and crude extract in rats.Methods Rats received 500 mg/kg puerarin and puerarin crude extract by oral administration respectively.Hydroxybenzoic acid was selected as internal standard and the plasma concentration of the puerarin and crude extract was analyzed by HPLC.The pharmacokinetics parameters were calculated with DAS2.0.Results The pharmacokinetics of puerarin and puerarin crude extract was both best fitted with two-compartment models in rats after oral administration,and the pharmacokinetics main parameters of the two formulations were different:the AUC_(0-t) and C_(max) of puerarin were much greater than those of puerarin crude extract,but T_(max),t_(1/(2z)),CL/F and V_z/F were much lesser than those of puerarin crude extract.Conclusion The complex components in pueraria crude extract can affect the pharmacokinetics of puerarin in rat in vivo.
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