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
School of Pharmacy, Ningxia Medical University, Yinchuan 750004, China.
Yao Xue Xue Bao. 2013 Jun;48(6):940-5.
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.
为分别研究盐酸伊立替康（CPT-11）纳米粒（CPT-11 NPs）经尾静脉注射后在大鼠体内的药代动力学以及在小鼠体内的组织分布情况，建立了一种液相色谱-串联质谱（LC-MS/MS）方法来测定大鼠全血及小鼠不同组织中CPT-11的浓度。在静脉注射CPT-11 NPs和CPT-11溶液后，比较了CPT-11的药代动力学和组织分布情况。与CPT-11溶液相比，静脉注射CPT-11 NPs后CPT-11的消除半衰期从2.28小时延长至3.95小时，其曲线下面积（AUC）是CPT-11溶液的1.47倍。在小鼠注射CPT-11 NPs后，CPT-11 NPs中负载的CPT-11在全血、结肠和肺中的浓度显著高于CPT-11溶液中的浓度，但在脾脏、肝脏、肾脏和心脏中的浓度较低，在脑中的浓度最低。CPT-11 NPs可提高CPT-11的AUC，并有助于CPT-11实现长循环活性。
