前哨淋巴结显像剂^(99)Tc^m-rituximab体外特性和安全限度的实验研究  

Experimental Study of Biological Property and Safety Limitation of Sentinel Lymph Node Imaging Agent ^(99)Tc^m-rituximab

作　　者：王雪鹃[1,2,3] 张岩[1,2,3] 李艳[1,2,3] 翟士桢[1,2,3] 林保和[1,2,3] 杨志[1,2,3] 

机构地区：[1]北京大学临床肿瘤学院 [2]北京肿瘤医院 [3]北京市肿瘤防治研究所核医学科恶性肿瘤发病机制及转化研究教育部重点实验室,北京100142

出　　处：《同位素》2011年第B12期90-94,共5页Journal of Isotopes

基　　金：国家自然科学基金资助项目(81172083)

摘　　要：用99 Tcm标记rituximab(美罗华)评价特异性前哨淋巴结(SLN)示踪剂99 Tcm-rituximab体外特性及其体内应用的安全性。采用聚丙烯酰胺凝胶电泳(SDS-PAGE)检测了99 Tcm-Rituximab的分子完整性;采用间接酶联免疫荧光分析(ELISA)及流式细胞术检测了99 Tcm-rituximab的免疫活性;最后依据中华药典的要求行99 Tcm-Rituximab安全限度及在正常小鼠体内分布实验。结果显示:99 Tcm-rituximab标记率为90%～95%;标记化合物分子完整,免疫活性保留完全,标记化合物无菌无热源。受试小鼠以60mg/kg剂量注射99 Tcm-rituximab(相当于人体用量的500倍),1周内未见小鼠死亡。小鼠体内分布结果显示:99 Tcm-ritux-imab入血后主要通过肾脏排泄,放射性摄取值由1h的(14.01±0.61)%ID/g减少为24h的(3.51±0.48)%ID/g;肝脏亦可见摄取。各器官未见有明显的放射性滞留。因此,99 Tcm-rituximab结构及性能稳定,无急性毒性,使用安全,可应用于临床。To evaluate the biological property and safety limitation of a specific sentinel lymphoscintigraphy imaging agent, 99 Tcm rituximab, 99 Tcm rituximab were analyzed for chemical and radiochemical purity, via SDS-PAGE and ITLC-SG. The immunoreactivity were detected via ELISA and flow cytometry. The safety limitation and biodistribution were tested according to the Chinese Pharmacopeia. The results showed that 99Tcm-rituximab, with a labeling yield of 90-95%, was intact, and processed similar immunoreactivity of rituximab. The final product was bacteria and pyogen free, and was safe to the body. According to the data of biodistribution, most of agent was excreted by the kiney, and the radio uptake decreased from （14.01±0.61） %ID/g at 1 h to （3.51±0.48） %ID/g at 24 h. The liver also uptook the agent. No accumulation was found in the normal tissue. 99Tern rituximab is stable and contains a good immunoreacivity and can be effectively used for clinical study.

关 键 词：99Tcm-rituximab 前哨淋巴结 显像剂 安全限度 

分 类 号：R817.33[医药卫生—影像医学与核医学]