【摘要】 目的:评价多相脂质体顺铂（KM-1）在大鼠体内的药物动力学及组织分布,并与游离顺铂比较。方法:用电感耦合等离子光谱法（ICP-AES）测定给药后大鼠血清及组织中铂的含量。结果:大鼠尾静脉给予4.5mg/kg剂量的KM-1后,血清-时间曲线符合开放三室模型。主要药动参数为:V_c=0.10L/kg,T_1/2π=0.3h,T_1/2α=3.5h,T_1/2β=2.7h,AUC-265mg·h·L^-1,CL（s）=0.02g·L^-1·h^-1。多相脂质体顺铂从血清中的消除速率小于游离顺铂。药物在组织中的分布以肝、脾器官中的含量最高。结论:该药物具有一般脂质体的基本特性,在血液循环中停留的时间比游离药物长,且易被网状内皮系统丰富的组织器官吸收。更多还原

【Abstract】 AIM: The pharmacokinetics and biodistribution of cisplatin encapsulated in polyphase liposome（KM-1） were compared with those of free drug in rats. METHODS: The platinum levels in serum and normal organs, after a single dose of iv injection of free or encapsulated cisplatin to rats, were determined by induced coupled plasma atomic emission spectrometry. RESULTS: Serum platinum concentration-time curve after a single iv dose of KM-1 4.5mg/kg in rats was fitted with an open three-compartment model. The pharmacokinetic parameters were as follows: V_c=0.10 L/kg, T_1/2π=0.3 h, T_1/2α=3.5 h, T_1/2β=2.7 h, AUC=265 mg·h·L^-1, and CL（s） =0.02g·L^-1·h^-1. KM-1 was cleared from the circulation much more slowly than free cisplatin. Liver and spleen had the highest concentration of platinum after KM-1 treatment. CONCLUSION: KM-1 remained in the bloodstream longer than its free drug, and was taken mainly by the reticuloendothelial system.更多还原