药学学报, 2013, 48(6): 940-945
引用本文:
杨付英, 张文萍, 陈和莉, 付 岩, 王欣瑜, 魏世杰, 杨小英, 张宇馨, 党宏万. 盐酸伊立替康纳米粒的药动学和组织分布[J]. 药学学报, 2013, 48(6): 940-945.
YANG Fu-Ying, Zhang Wen-Ping, Chen He-Li, Fu Yan, Wang Xin-Yu, Wei Shi-Jie, Yang Xiao-Ying, Zhang Yu-Xin, Dang Hong-Wan. Pharmacokinetics and tissue distribution of irinotecan hydrochloride nanoparticles[J]. Acta Pharmaceutica Sinica, 2013, 48(6): 940-945.

盐酸伊立替康纳米粒的药动学和组织分布
杨付英1, 张文萍2, 3, 陈和莉1, 付  岩1, 王欣瑜2, 3, 魏世杰2, 3, 杨小英2, 3, 张宇馨2, 3, 党宏万2, 3*
(宁夏医科大学 1. 药学院, 2. 总医院药剂科, 3. 总医院临床药理研究室, 宁夏 银川 750004)
摘要:

考察盐酸伊立替康纳米粒 (irinotecan hydrochloride nanoparticles, CPT-11 NPs) 在大鼠体内药动学和小鼠体内组织分布特性。LC-MS/MS法测定生物样品中伊立替康的浓度, 比较盐酸伊立替康纳米粒和盐酸伊立体康溶液尾静脉给药后的药动学参数与体内分布特点。在药动学研究中, 与盐酸伊立替康溶液相比, 纳米粒组中CPT-11AUC是溶液组的1.47, t1/22.28 h延长到3.95 h。在组织分布研究中, 盐酸伊立替康纳米粒在小鼠血液、结肠和肺中的药量显著提高, 其次是脾、肝、肾及心, 脑中最少。CPT-11 NPs可以提高CPT-11的生物利用度, 并在一定程度上延长该药物在动物体内的循环时间。

关键词:   
Pharmacokinetics and tissue distribution of irinotecan hydrochloride nanoparticles
Abstract:

To investigate the pharmacokinetics of irinotecan hydrochloride (CPT-11) in rats and the tissue distribution of CPT-11 in mice after injection of irinotecan hydrochloride nanoparticles (CPT-11 NPs) via tail veins, separately, a LC-MS/MS method was established to determine the concentration of CPT-11 in whole blood of rats and in different tissues of mice.  The pharmacokinetics and tissue distribution of CPT-11 were compared after the intravenous injection of CPT-11 NPs and CPT-11 solution.  Compared with CPT-11 solution, the elimination half-life of CPT-11 was prolonged from 2.28 h to 3.95 h after the intravenous injection of CPT-11 NPs, and its AUC was 1.47 times than that of CPT-11 solution.  After the injection of CPT-11 NPs in mice, the concentrations of CPT-11 loaded in CPT-11 NPs were significantly higher in the whole blood, colon and lungs than those in CPT-11 solution, but lower in the spleen, liver, kidney and heart, but the least in brain.  CPT-11 NPs could improve CPT-11’s AUC, and help CPT-11 to reach long circulation activity.

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