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目的 :用 1 2 5 I标记抗 AFP多克隆抗体治疗 12例原发性肝癌患者 ,观察其药代动力学特征。方法 :用改良氯胺 - T法制备 1 2 5 I-抗 AFP抗体 ,标记率为 6 5 %～ 83% ,比放射性为 5 5 .5～ 74MBq/ m g (Ig G)。全部病例采用 Seldinger插管技术 ,经肝动脉注射给药。给药后在不同时间点采集外周静脉血测放射活性。所得数据用计算机程序 PK - GRAPH模拟出 1 2 5 I-抗 AFP抗体的药代动力学模型、血放射性 -时间曲线和计算出各种动力学参数。结果 :全组病例的药代动力学模式为二室模型 ;t1 /2α为 (1.85± 1.79) h,t1 /2β为 (15 6 .46± 6 5 .11) h。血清 AFP>40 0μg/ L和 AFP阴性病人药动学参数无显著性差异 ,不同的抗体用量以及是否经肝动脉用碘油抗癌药乳剂作 TAE对药动学参数均无显著性影响 (P >0 .0 5 )。结论 :1 2 5 I-抗 AFP抗体经肝动脉给药 ,在肝癌病人体内有较长的清除半衰期。
Objective : To treat 12 cases of primary liver cancer patients with 1 2 5 I-labeled anti-AFP polyclonal antibody and observe its pharmacokinetic characteristics. Methods: The 1 25 I-anti-AFP antibody was prepared with the modified chloramine-T method. The labeling rate was 65 to 83% and the specific radioactivity was 5 5 to 74 MBq/g (Ig G). All cases were treated with Seldinger cannulation and administered via hepatic artery injection. Peripheral venous blood was collected at different time points after administration to measure radioactivity. The obtained data were used to simulate the pharmacokinetic model of 1 2 5 I-anti-AFP antibody, blood radioactivity-time curve and calculate various kinetic parameters using computer program PK-GRAPH. Results: The pharmacokinetic model of the whole group was a two-compartment model; t1 /2α was (1.85± 1.79) h, and t1 /2β was (15 6 .46± 6 5.11) h. There was no significant difference in pharmacokinetic parameters between serum AFP>40 μg/L and AFP-negative patients. There were no significant differences in pharmacokinetic parameters between different doses of antibodies and whether TAE was used as a hepatic artery with lipiodol anticancer drug emulsion (P). >0 .0 5 ). Conclusion : 1 25 I-anti-AFP antibody administered via the hepatic artery has a long elimination half-life in patients with liver cancer.