小鼠尾静脉注射^(125)I标记的抗CEA人鼠嵌合抗体rch24的药代动力学研究  

The pharmacokinetics of ^(125)I-rch24 in mice JI Bo,WANG Jian,YANG Zhi,et al

作　　者：纪渤[1] 王建[1] 杨志[2] 路逵阳[3] 

机构地区：[1]徐州医学院第二附属医院ICU,江苏徐州221006 [2]北京大学临床肿瘤学院核医学科,北京100036 [3]徐州医学院附属医院普外科,江苏徐州221002

出　　处：《徐州医学院学报》2005年第1期29-32,共4页Acta Academiae Medicinae Xuzhou

基　　金：江苏省高校自然科学研究项目(02KJD320032);徐州市医学重点人才基金项目

摘　　要：目的探讨125I-rch24在小鼠体内的药代动力学过程。方法7只BABL/c小鼠,溴代琥珀酰亚胺(NBS)法标记的抗体125I-rch24尾静脉注射,于注射后不同时间尾根部取血,测定放射性计数,绘制血清除曲线,计算药代动力学参数。结果①125I与CEA人鼠嵌合抗体rch24结合,采用纸层析法测定的标记率为95.5%±02%;②标记抗体的放射化学纯度至14天后为92.6%,35天后为89.3%;③经计算机模拟,为双指数曲线,标记抗体的血液分布、清除符合二房室模型。结论正常小鼠尾静脉注射标记抗体125I-rch24后的药代动力学过程符合二房室模型,静脉注射适宜用于结肠癌放射免疫导向手术。Objective To investigate the pharmacokinetics of ~125 I labeled anti-CEA human-mouse chimeric antibodies rch24 (~125 I-rch24).?Methods Seven mice were injected with ~125 I-rch24 through the tail vein.After that,blood samples taken from the tip of the tail at regular intervals,were processed to determine the radioactivity,draw the plasma clearance curve and calculate the pharmacokinetics parameters.?Results ①The binding ratios of ~125 I-rch24 measured by using ITLC-SG, were 95.5%±0.2%. ②The radiochemical purity of the radiolabeled antibodies was 92.6% on 14 days and 89.3% on 35 days after radiolabeling.③By computer simulating,the plasma distribution and clearance of ~125 I-rch24 was found to be best fitted by a two-compartment model with a distribution half-life (T_~1/2 α) of 5.544 h and an elimination half-life (T_~1/2 β) of 247.5 h.?Conclusion The venous administration of ~125 I labeled anti-CEA antibodies rch24 is suitable for radioimmunoguided procedure for colonic carcinoma treatment.

关 键 词：静脉注射 ^125I标记 药代动力学 正常小鼠 嵌合抗体 CEA 抗C 人鼠 纸层析法 NBS 

分 类 号：R969.1[医药卫生—药理学] R392[医药卫生—药学]