多西他赛磺丁基-<i>β</i>-环糊精包合物的大鼠药代动力学

王猛; 乔红群; 严拯宇

doi:10.11665/j.issn.1000-5048.20130211

多西他赛磺丁基-β-环糊精包合物的大鼠药代动力学

Pharmacokinetics of docetaxel SBE-β-cyclodextrin inclusion complex in rats

摘要

摘要: 采用LC-MS/MS法比较研究多西他赛磺丁基-β-环糊精包合物受试制剂与市售参比制剂静脉注射后，药物在大鼠体内的药代动力学及组织分布。结果显示，大鼠静注10 mg/kg受试制剂及参比制剂后，药代动力学参数分别为t_1/2（3.4±0.9）和（4.0±1.0）h，表观分布容积为（31.999±14.16）和（35.526±7.218）L/kg，AUC_0-∞为(1 690±476)和(1 629±213) μg·h/L，多西他赛在大鼠体内的药代动力学过程均符合二室模型的特征。大鼠静注10 mg/kg受试制剂及参比制剂后，骨髓、肺和脾中含量较高，脑、脂肪和睾丸中含量较低。统计学分析显示，两种制剂在大鼠体内主要药代动力学参数及组织分布无显著性差异（P>0.05）。

Abstract: The pharmacokinetics and tissue distribution of the prepared docetaxel SBE-β-cyclodextrin inclusion complex (test preparation) and the commercial formulation (reference preparation) in rats were studied.After iv administration of test and reference preparations,the concentrations of docetaxel in rats plasma and tissue were determined by LC-MS/MS.The results showed that after a single iv administration of 10 mg/kg test and reference preparation to rats,the pharmacokinetic parameters of docetaxel were as follows:t_1/2 （3.4±0.9）and （4.0±1.0） h,Vz （31.999±14.16）and （35.526±7.218）L/kg,AUC_0-∞ (1 690±476) and (1 629±213) μg ·h/L.It was fit for two-compartment model.And after a single iv administration of 10 mg/kg test and reference preparation in rats,the concentration levels of docetaxel were higher in the bone marrow,lung,and spleen,and lower in the brain,fat and testes.Statistical analysis showed that there was no significant difference (P>0.05) between the test and reference preparations in major pharmacokinetic parameters and tissue distribution data in rats.

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