新型骨显像剂99Tcm-HBIDP的制备与初步生物学性质

    Preparation and Biological Study on a Novel Bone Imaging Agent 99Tcm-HBIDP

    • 摘要: 在SnCl2•2H2O存在下,用Na99TcmO4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99Tcm-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(99TcmO4-)=55.5 MBq、室温反应15min时,99Tcm-HBIDP的标记率大于95%。99Tcm-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。99Tcm-HBIDP的血浆蛋白结合率为(31.41±1.25)%。99Tcm-HBIDP具有良好的体外稳定性。动物分布实验显示:99Tcm-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,99Tcm-HBIDP较99Tcm-ZL在心、肝、脾等器官组织中的摄取低。99Tcm-HBIDP有望成为新型骨显像剂。

       

      Abstract: 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)=100μg, m(HBIDP)=5mg, A(99TcmO4-)=55.5MBq at room temperature for 15min and the radiochemical purity is more than 95% and it is stable within 6h 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.

       

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