BAPTA-AM脂质体注射液在大鼠和Beagle犬体内的药动学比较

目的：比较研究BAPTA-AM脂质体注射液在大鼠和Beagle犬体内的药动学过程。方法：通过LC-MS/MS方法测定大鼠、Beagle犬血浆中BAPTA-AM的浓度,采用非房室模型计算BAPTA-AM注射液在大鼠、Beagle犬体内的药动学参数。结果：大鼠尾静脉注射1.5、3.0、6.0mg/kgBAPTA-AM脂质体注射液后,体内消除半衰期分别为（255±140）、（290±260）、（376±257）min,AUC0-∞分别为（831±251）、（1467±528）、（3650±1664）μg.L^-1.min;Beagle犬静脉注射0.5、1.0、2.0mg/kgBAPTA-AM脂质体注射液后,体内3个剂量的消除半衰期分别为（362±305）、（347±278）、（432±292）min,AUC0-∞分别为（400±118）、（569±139）、（1185±640）μg.L-1.min。结论：静脉注射给药后,BAPTA-AM脂质体注射液在大鼠和Beagle犬体内代谢较快,分布较广,在两种动物内的药动学过程无统计学差异。

Comparison of the pharmacokinetics of BAPTA-AM liposome injection in rats and Beagle dogs

AIM：To compare the pharmacokinetics of BAPTA-AM liposome injection in rats and Beagle dogs.METHODS：The concentration of BAPTA-AM in plasma was quantified by LC-MS/MS after intravenous injection.The pharmacokinetic parameters were calculated by the non-compartment model.RESULTS：The elimination half-life in rats after intravenous injection 1.5,3.0 and 6.0 mg/kg BAPTA-AM liposome were （255±140）,（290±260）and （376±257）min respectively,and the AUC0-∞ were（831±251）,（1467±528）and（3650±1664） μg·L-1·min,respectively.The elimination half-life in dogs after intravenous injection 0.5,1.0 and 2.0 mg/kg BAPTA-AM liposome were （362±305）,（347±278）and （432±292）min respectively,and the AUC0-∞ were （400±118）,（569±139）and （1185±640） μg·L^-1·min,respectively.CONCLUSION：After intravenous injection,BAPTA-AM liposome is metabolized rapidly and distributed abroad in rat and Beagle dog.There is no difference in the pharmacokinetic between rats and dogs.