关键词:188 Re;药代动力学;裸小鼠;单克隆抗体;肝癌

    摘 要:目的 研究188 Re标记的肝癌单抗片段HAb18F(ab')2 在荷肝癌裸鼠体内的药代动力学，求取药代动力学参数，建立药代动力学模型. 方法 5组裸鼠经尾静脉注入1.85MBq188 Re-HAb18F(ab')2 ，在不同时间点处死裸鼠，测量血及各脏器放射性计数.用3P97药代动力学软件处理188 Re-HAb18F(ab')2 给药后荷瘤鼠各时间点的血液放射性浓度及各主要脏器的放射性浓度，计算药代参数. 结果 188 Re-HAb18F(ab')2 在裸鼠体内药代动力学参数分别为T1/2 2.29h，Vd1.49L，AUC20.49×109 Bq·h·L-1 ，CL0.45×10-3 L·h-1 .

    188 Re-HAb18F(ab')2 特异性聚集于肿瘤中，在瘤体中以较高水平维持较长时间，在正常组织中代谢较快，主要从肾脏中排泄. 结论 188 Re-HAb18F(ab')2 在荷肝癌裸鼠体内药代动力学符合线性一室模型.

    Pharmacokinetics of radioimmunotherapeutic agent188 Re┐HAb18F(ab')2 in hepatoma┐bearing nude mice

    LOU Chao，BIAN Hui-Jie，CHEN Zhi-Nan

    Cell Engineering Research Centre，Fourth Military Medical University，Xi'an710033，China

    Keywords:188 Re;pharmacokinetics;nude mice;monoclonal antibody;hepatoma

    Abstract:AIM To establish the pharmacokinetic model of188 Re-HAb18F(ab')2 and to evaluate its pharmacokinetic pa┐rameters.METHODS The mice was sacrificed at different time after188 Re-HAb18F(ab')2 i.v.injected into hepatoma-bearing nude mice.The blood and organs'radioactivity were measured.The concentrations of188 Re-HAb18F(ab')2 were evaluated with a pharmacokinetic3P97software.RESULTS Parameters of188 Re-HAb18F(ab')2 were T1/2 2.29h ......