^(153)Sm-羟乙基乙二胺三甲撑膦酸(HEDTMP)的动物实验研究  

Experimental study of a new radiopharmaceutical, ^(153)Sm-HEDTMP

作　　者：胡疏[1] 邓候富[1] 蒋树斌[2] 雷勇[1] 罗顺忠[2] 

机构地区：[1]四川大学华西医院核医学科 [2]中国工程物理研究院核物理与化学研究所

出　　处：《中华核医学杂志》2002年第6期356-359,共4页Chinese Journal of Nuclear Medicine

基　　金：国家自然科学基金资助项目 (2 9971 0 2 7)

摘　　要：目的　初步探讨1 53Sm 羟乙基乙二胺三甲撑膦酸 (HEDTMP)的生物学性能。方法　分别以99Tcm 亚甲基二膦酸盐 (MDP)和1 53Sm 乙二胺四甲基膦酸 (EDTMP)作对照 ,进行1 53Sm HEDTMP新西兰兔、Wistar大鼠骨显像和昆明小白鼠体内分布实验。结果　①1 53Sm HEDTMP动物骨显像提示有较高的骨摄取 ,颅骨、脊柱、四肢显示清晰 ,与99Tcm MDP及1 53Sm EDTMP的骨显像效果相似。②1 53Sm HEDTMP有快速的血清除与骨摄取 ,注射后 30min骨摄取为 19.13%ID g,3h为 2 4 .5 4 %ID g ,2 4h为 18.95 %ID g;示踪剂主要经肾脏排泄 ,非靶脏器放射性残留低。③1 53Sm HEDTMP的骨摄取和靶 非靶比值比1 53Sm EDTMP高。结论　1 53Sm HEDTMP显示出良好的生物学性能 ,有希望成为新的放射性骨治疗剂。ObjectiveTo investigate the biological properties of 153Sm-N-(2-hydroxyethyl) ethylene diamine -1,1,2-tri (methylene phosphonic acid, HEDTMP), a new kind of bone seeking compound; and to see if this radiopharmaceutical could be explored for target therapy of bone metastases. MethodsWith 99Tcm-methylene diphosphonate (MDP) and 153Sm-ethylene diamine tetramethylene phosphonic acid (EDTMP) being used as control agents, respectively, the plane bone scanning on New Zealand rabbits and Wistar rats and the biodistribution experiment of 153Sm-HEDTMP on Kunming mice were performed. Results①The plane bone scanning on rabbits and rats showed that 153Sm-HEDTMP was principally absorbed by skeletal system. Skull, spine and leg bones could be observed as clearly as the images by 99Tcm-MDP and 153Sm-EDTMP. ②Mice trial also indicated the high bone seeking of 153Sm-HEDTMP. The skeletal uptake was 19.13, 24.54 and 18.95%ID/g at 30 min, 3 and 24 h, respectively, after the injection. Kidney seemed to be the major excretory organ. The clearance from blood was quick and the retaining amount in non-target organs was small.③The bone uptake and target to non-target ratio of 153Sm-HEDTMP were higher than that of 153Sm-EDTMP. Conclusion 153Sm-HEDTMP showed its fine biological properties which could be compared favorably with the commonly used bone radioactive agents, and it is well worth further research as a promising potential radiopharmaceutical in nuclidic treatment for bone metastases.

关 键 词：^153Sm-羟乙基乙二胺三甲撑膦酸 骨转移癌 治疗 动物实验 HEDTMP 化学合成 药代动力学 放射性核素显像 

分 类 号：R817.1[医药卫生—影像医学与核医学]