氚标记吲哚美辛在荷瘤鼠血液及瘤体内药代动力学研究

Study on Pharmacokinetics of 3H-IN in tumor-bearing mice’s Blood and Tumor

  • 摘要: 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消除迅速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DAS ver1.0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。结果证明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

     

    Abstract: 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. mice are taken out blood and tumor at different time point after being taken 3H-IN orally, radioactivities are counted and concentrations of IN are measured in the tissues above.The results show that 3H-IN accumulated in tumor tissue with high levels for long time,But at the same time IN prototype is cleared rapidly and the concentrations are far lower than in blood, pharmacokinetic parameters were calculated by DAS ver1.0 software. The results demonstrate that 3H-IN has good affinity to the tumor tissue and the major part accumulated in tumor is not the IN prototype.

     

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