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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。
OBJECTIVE: To evaluate the pharmacokinetics and tissue distribution of multi-phase liposomal cisplatin (KM-1) in rats and to compare it with free cisplatin. Methods: ICP-AES was used to determine the content of platinum in the serum and tissues of rats after administration. RESULTS: The serum-time curve of KM-1 at the dose of 4.5 mg / kg in tail vein of rats was in accordance with the open three-compartment model. The main pharmacokinetic parameters were as follows: Vc = 0.10L / kg, T 1 / 2π = 0.3h, T 1/2 1/2 3.5h, T 1/2/2.7h, AUC 265mg · h · L ~ (-1), CL (s) = 0.02g · L -1 · h -1. The elimination rate of heterogeneous liposomal cisplatin from serum was less than that of free cisplatin. Drugs in the distribution of the liver, spleen organs in the highest content. Conclusion: The drug has the basic characteristics of the general liposomes, stay in the blood circulation longer than the free drug, and easily absorbed by the reticuloendothelial system rich in tissues and organs.