氚标记吲哚美辛在荷瘤鼠血液及瘤体内的药代动力学研究

Study on Pharmacokinetics of ^3H-IN in Tumor-bearing Mice＇s Blood and Tumor

研究氚标记吲哚美辛(3H-IN)在荷瘤小鼠血液及瘤体内的分布及药代动力学特征,进一步探讨其在肿瘤中的蓄积现象。荷Lewis肺癌小鼠灌胃给药后于不同时间点取血和瘤组织,分别测定其放射性计数及药物浓度。结果表明,3H-IN蓄积于肿瘤组织中,并以较高水平维持较长时间,在此期间,瘤体中吲哚美辛药物原形则迅速消除,且浓度远低于血药浓度。小鼠血浆和瘤体内不同时相IN的药物浓度数据用DASver1.0实用药代动力学程序处理,选择二室模型,且权重系数为1/cc拟合药-时曲线,得出主要药代动力学参数。结果提示,3H-IN有很好的瘤组织趋向性,其药物原形并非在肿瘤中蓄积的主要成分。

Pharmacokinetics of ^3H-IN in tumor-bearing Mice＇s blood and tumor are studied, and the accumulated phenomenon of IN in tumor are further discussed. Blood and tumor of mice are taken at different time after being taken ^3 H-IN orally, radioactivities are counted and concentrations of IN are measured in the tissues. The results show that ^3 H-IN accumulate in tumor tissue with high levels for a long time, but at the same time IN prototype is cleared rapidly and it＇s concentrations are far lower than in blood. Pharmacokinetic parameters are calculated by DAS verl. 0 software. The results demonstrate that ^3 H-IN has good affinity to the tumor tissue and the major part accumulated in tumor is not the IN prototype.