新型骨显像剂^(99)Tc^m-HBIDP的制备与初步生物学性质  

Preparation and Biological Study on a Novel Bone Imaging Agent ^(99)Tc^m-HBIDP

作　　者：王立勤[1,2] 邱玲[2] 林建国[2] 南蓓蓓[1,2] 罗世能[2] 马海霞[1] 黄洁[1] 

机构地区：[1]西北大学化工学院,陕西西安710069 [2]江苏省原子医学研究所,卫生部核医学重点实验室,江苏省分子核医学重点实验室,江苏无锡214063

出　　处：《核化学与放射化学》2012年第2期93-101,共9页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目(20801024);江苏省自然科学基金资助项目(BK2009077);江苏省卫生厅科研项目(H200963)

摘　　要：在SnCl2.2H2O存在下,用Na 99 TcmO4标记1-羟基-2-(1-丁基-1H-咪唑-2-基)亚乙基-1,1-双膦酸(HBIDP)。研究了99 Tc m-HBIDP的最优标记条件、理化性质及其在正常小鼠体内分布。结果表明,当pH=6、m(SnCl2.2H2O)=100μg、m(HBIDP)=5mg、A(99 TcmO4-)=55.5MBq、室温反应15min时,99 Tcm-HBIDP的标记率大于95%。99 Tcm-HBIDP在pH为7.0和7.4时,脂水分配系数lg P分别为-2.17和-2.28。99 Tcm-HBIDP的血浆蛋白结合率为(31.41±1.25)%。99 Tcm-HBIDP具有良好的体外稳定性。动物分布实验显示:99 Tcm-HBIDP在骨组织中有较高摄取,并能保持较长时间;其在软组织中的摄取相对较低,并能较快的清除。此外,99 Tcm-HBIDP较99 Tcm-ZL在心、肝、脾等器官组织中的摄取低。99 Tcm-HBIDP有望成为新型骨显像剂。To obtain a maximum radiolabeling yield,the labeling parameters for 99Tcm-HBIDP were optimized.Chemical and physical properties and biodistribution studies in mice for 99Tcm-HBIDP were performed.The optical labeling parameters are found as follows：pH=6,m（SnCl2·2H2O）=100 μg,m（HBIDP）=5 mg,A（99TcmO-4）=55.5 MBq at room temperature for 15 min and the radiochemical purity is more than 95% and it is stable within 6 h in vitro at room temperature.The octanol-water partition coefficients of 99Tcm-HBIDP（lg P） are-2.17 and-2.28 at the pH value of 7.0 and 7.4,respectively.The plasma protein binding ratio of 99Tcm-HBIDP is（31.41±1.25）%.In the biodistribution studies,99Tcm-HBIDP exhibits a relatively high uptake in bone and much lower uptake in soft tissues and shows rapid clearance from soft tissues.Besides,the uptake of 99Tcm-HBIDP in heart,liver and spleen is much lower than that of 99Tcm-ZL.These preliminary studies indicate that 99Tcm-HBIDP has significant potential as a novel bone imaging agent.

关 键 词：99Tcm-HBIDP 标记 理化性质 动物分布 骨显像剂 

分 类 号：R817[医药卫生—影像医学与核医学]