特异性前哨淋巴结显像剂^(99)Tc^m-rituximab药盒的制备及生物评价  

Preparation and Evaluation of a Freeze-dried Kit of ^(99)Tc^m-rituximab for Sentinel Lymph Node Imaging

作　　者：李艳[1,2,3] 李囡[1,2,3] 翟士桢[1,2,3] 王雪鹃[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85-89,共5页Journal of Isotopes

基　　金：国家自然科学基金资助项目(81071198)

摘　　要：采用2-巯基乙醇修饰Rituximab(利妥昔单克隆抗体),制得其冻干药盒。所制得的冻干药盒性质稳定,可在-20℃冷冻保存3个月以上。利用99 Tcm-葡庚糖酸钠(GH)交换法,标记冻干药盒得到99 Tcm-ritux-imab,标记率和放化纯度均大于90%。生物分布结果显示:SD大鼠经前脚掌皮下注射99 Tcm-rituximab后,前哨淋巴结的摄取值在1～4h内逐渐增加,在4h时达到(2.14±0.46)%ID,前哨淋巴结与注射点的放射性摄取比在4h时达到最大(14.80%±2.11%),且在18h时,这一比值基本保持不变。SPECT显像结果表明,在30min～18h内,大鼠的前哨淋巴结清晰可见,无次级淋巴结显影。本研究提供了一种特异性前哨淋巴结显像剂的药盒化制备方法,该方法操作简便,性能稳定,便于在临床推广应用。99 Tcm-rituximab has been demonstrated to be having favourable properties for sentinel lymph node imaging. The aim of this research was to develop the formulation of the 99 Tcm-rituximab freeze-dried kit. Firstly the rituximab was modified by 2-Mercapitoethanol, with the glucose as the excipient, and 1 mL phosphate buffers to compose the kit, which was dispensed into nitrogen-filled vials and aliquots frozen at -20 ℃. 99 Tcm_Rituximab was prepared from the 99 Tcm-glucose via ligand exchange method. Both of the labeling yield and the radiochemical purity were more than 90%. The results of biodisdistribution of 99Tcm-rituximab in normal rat with front pad injection showed that the accumulation of the sentinel lymph node increased from 1 h （0.93±0.39%ID） to 4 h （2.14±0.46%ID）. The ratio of the uptake of sentinel lymph node to that of the injection site was 14.80±2.11% at 4 h, with no significant change at 18 h （13.03%±3.98%）. The SPECT imaging in rat showed that the sentinel lymph node can be seen clearly without the secondary lymph node imaging 30 min-18 h p. i.. In general, the frozen kit of rituximab was feasible to prepare the sentinel imaging agent 99 Tcm-rituximah, which possesses satisfied properties for sentinel lymph node SPECT imaging.

关 键 词：99Tcm-rituximab 前哨淋巴结 显像剂 

分 类 号：R817.33[医药卫生—影像医学与核医学]