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中国临床药理学与治疗学 ›› 2010, Vol. 15 ›› Issue (6): 663-667.

• 定量药理学 • 上一篇    下一篇

BAPTA-AM脂质体注射液在大鼠和Beagle犬体内的药动学比较

郑枫1, 刘文英1, 魏伟2   

  1. 1中国药科大学药物分析教研室, 南京 210009, 江苏;
    2合肥恒星医药研究所, 合肥 230088, 安徽
  • 收稿日期:2010-04-14 修回日期:2010-06-13 出版日期:2010-06-26 发布日期:2020-09-16
  • 作者简介:郑枫,男,博士,讲师,研究方向:体内药物分析。Tel: 025-83271251 E-mail: cpuanalyst@126.com

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

ZHENG Feng1, LIU Wen-ying1, WEI Wei2   

  1. 1 Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, Jiangsu, China;
    2 Hefei Healstar Medicine Research Institute, Hefei 230088, Anhui, China
  • Received:2010-04-14 Revised:2010-06-13 Online:2010-06-26 Published:2020-09-16

摘要: 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、6.0 mg/kg BAPTA-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、2.0 mg/kg BAPTA-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。

关键词: BAPTA-AM, 脂质体, 大鼠, Beagle犬, 药代动力学

Abstract: 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.

Key words: BAPTA-AM, Liposome, Rat, Beagle dog, Pharmacokinetics

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