【摘要】 研究碘[131I]-美妥昔单抗注射液的人体药代动力学特征,为临床给药方案及临床应用提供依据。将按纳入标准、排除标准和剔除标准选择的患原发性肝细胞肝癌受试者24例平均分为低、中、高剂量组,各组每位受试者经插管注入相应的注射液,分别在不同时刻采集静脉血及收集尿液,测定样品的放射性计数率(min-1);采用纸层析确定各血样血清中药物的比例,依此校正各血样中药物的放射性计数率;用DASver1.0(Drug And Statistics for Windows)药代动力学程序拟合、计算血液药代动力学参数;鉴定尿液中放射性物质的组成,计算各时间段尿液放射性占注入剂量的百分率(%ID),以分析注射液在尿液的清除动力学特点。研究表明:该注射液血液药代动力学符合动力学二室模型,其在人体内分解代谢产物主要以游离131I的形式通过肾脏排泄,注入后120h内排出尿液的放射性占注入剂量的47.70%~51.16%。因此,该注射液的药代动力学特征满足临床要求,推荐临床的给药剂量为每kg人体27.75MBq注射液。更多还原

【Abstract】 To study pharmacokinetics of injection of iodine-131 labelling MEI-TUO-XI monoclonal antibody (hepatoma monoclonal antibody HAb18 F(ab’)2) in vivo. 24 cases of primary hepatocelluar carcinoma (PHC) were equally divided into the low dose group, middle dose group and high dose group. After the relevant injection was administrated into the hepatic artery of each case, intravenous blood and urine samples were separately collected at different time for determination of the radioactive count ratio (min-1). The proportion of 131I-HAb18 F(ab’)2 in serum of each blood sample was determined, and the radioactive count ratio (min-1) of druggery for each blood sample was revised according to the proportion. The pharmacokinetic parameters were calculated using DAS ver1.0 (Drug And Statistics for Windows) program. The component of urine radiomaterial was determined and the percentages of urine radioactivity in administration dosage were calculated. The catabolism of the injection with time accorded with dynamics two-compartment model. The catabolism product was mainly free-131I and was excreted via kidney; the urine radioactivity was 47.70%-51.16% of administration dosage during 120 h after administration of drug. Therefore, the pharmacokinetics of the injection can satisfy the clinical demands.The drug dose recommended for clinical use was 27.75 MBq of the injection for each kg of human body.更多还原