^(99m)锝-羟乙基乙二胺三甲撑膦酸的动物实验研究  

A New Radiopharmaceutical for Bone Imaging: Experimental Study of ^(99m)Tc-HEDTMP

作　　者：胡疏[1] 邓候富[2] 蒋树斌[3] 罗顺忠[3] 雷勇[4] 

机构地区：[1]北京大学深圳医院暨深圳临床医学院核医学科,深圳518036 [2]四川大学华西医院核医学科,成都610041 [3]中国工程物理研究院核物理与核化学研究所,绵阳621900 [4]深圳市第二人民医院核医学科,深圳518035

出　　处：《生物医学工程学杂志》2010年第4期811-815,共5页Journal of Biomedical Engineering

基　　金：国家自然科学基金资助项目(29971027)

摘　　要：合成了化合物99m锝-羟乙基乙二胺三甲撑膦酸(99mTc-HEDTMP)]并初步分析了其生物学性能,探讨其成为新的放射性骨显像剂的可能性。采用亚锡还原法对HEDTMP进行99mTc的标记,其放射化学纯度为97.00%±0.34%,生理盐水稀释前及稀释100倍后室温放置5 h时其放化纯度仍大于95%。动态观察99mTc-HEDTMP在小鼠及兔体内不同时相的生物学资料,表明该显像剂从血液及软组织中清除快,主要经泌尿系统排泄,骨骼摄取较99mTc-亚甲基二膦酸(99mTc-MDP)快且高,并在骨骼内滞留时间较长,便于缩短注射显像剂后等待显像的时间,同时也便于在较为宽松的时间段内完成显像。结果表明99mTc-HEDTMP的标记方法简便,亲骨组织性能良好,有希望成为新型的、极具临床价值的新型骨显像剂,值得进行更为深入的研究。The purpose of this study is to prepare 99mTc-HEDTMP [N-（2-hydroxyethyl） ethlenediamine-1,1,2-tri（methylene phosphonic acid）,a new kind of bone seeking compound;to investigate its biological properties;and to explore the possibility of using it as a potential radiopharmaceutical for skeleton scintigraphy.HEDTMP was labeled with 99mTc by ＂pretinning＂ method,the radiochemical purity was 97.00%±0.34%.99mTc-HEDTMP was found to be stable in 5 hours in vitro with the radiochemical purity over 95% even after being diluted by physiological saline with the factor of dilution 100.The plane bone scanning of rabbits showed that 99mTc-HEDTMP was principally absorbed by skeletal system.Skull,spine and legs could be observed clearly,and were more legible than the images of 99mTc-MDP.Mice trial also indicated the high bone seeking of 99mTc-HEDTMP.The skeletal uptake was 11.92% ID/g,13.19% ID/g,10.14% ID/g,10.04% ID/g,7.71% ID/g separately at 30 minutes,1 hour,3 hours,6 hours and 24 hours after the injection.Kidney seemed to be the major excretory organ.The clearance of blood was quick and the retaining amount in non-target organs was small.These results indicate that 99mTc-HEDTMP can be prepared easily, and its biological properties can be compared favorably with the commonly used bone imaging agent,and it is well worth further researching as a promising potential radiopharmaceutical in nuclide diagnosis for skeleton diseases.

关 键 词：99m锝-羟乙基乙二胺三甲撑膦酸 骨显像剂 生物分布 实验研究 

分 类 号：R817[医药卫生—影像医学与核医学]