Pharmacokinetics and tissue distribution of iv injection of polyphase liposome—encapsulated cisplatin（KM—1） in rats  

大鼠静注多相脂质包裹顺铂(KM-1)后药物动力学及组织分布(英文)

作　　者：王杉[1] 宓捷波[1] 李元宗[1] 常文保[1] 慈云祥[1] 赵敏政[2] 赵云昆[2] 朱利亚[2] 徐光[2] 

机构地区：[1]北京大学化学与分子工程学院 [2]昆明贵金属研究所

出　　处：《Acta Pharmacologica Sinica》2003年第6期589-592,共4页中国药理学报（英文版）

基　　金：Projects supported by Yunnan Science and Technology Committee.

摘　　要：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-14.5mg/kg in rats was fitted with an open three-compartment model. The pharmacokinetic parameters were as follows: Vc=0.10L/kg, T1/2π=0.3h, T1/2α=3.5h, T1/2β=2.7h, AUC=265mg·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.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.

关 键 词：PHARMACOKINETICS liposomes CISPLATIN induced coupled plasma atomic emission spectrometry 

分 类 号：R979.1[医药卫生—药品] R969.1[医药卫生—药学]