Qiu Ling, Cheng Wen, Lin Jianguo, Zhang Shu, Luo Shineng
Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China.
Curr Radiopharm. 2013 Mar;6(1):28-35. doi: 10.2174/1874471011306010005.
A novel zoledronate derivative, 1-hydroxy-4-(2-butyl-1H-imidazol-1-yl)butane-1,1- diyldiphosphonic acid (BIBDP) was prepared and labeled with (99m)Tc successfully in a high radiochemical purity and good stability in vitro. The biodistribution in mice shows that (99m)Tc-BIBDP has high specificity and efficacy in bone uptake with a maximum of 12.14 ± 0.53 %ID/g at 120 min. Kinetics of blood clearance showed that distribution half life (T(1/2α)), elimination half life (T(1/2β)) and total clearance rate (CL) of (99m)Tc-BIBDP were 4.67 min, 91.9 min and 1.21 %ID/g·min(-1), respectively. Moreover, (99m)Tc-BIBDP has higher uptake in the bone and faster clearance from soft tissues than (99m)Tc-MDP and (99m)Tc-ZL. A plain and clear bone image was obtained at 1 h with SPECT bone imaging. The present findings indicate that (99m)Tc- BIBDP holds great potential for bone imaging.
制备了一种新型唑来膦酸衍生物1-羟基-4-(2-丁基-1H-咪唑-1-基)丁烷-1,1-二膦酸(BIBDP)，并成功用(99m)Tc进行标记，体外放射性化学纯度高且稳定性良好。小鼠体内生物分布显示，(99m)Tc-BIBDP在骨摄取方面具有高特异性和高效性，120 min时最大摄取量为12.14±0.53%ID/g。血液清除动力学表明，(99m)Tc-BIBDP的分布半衰期(T(1/2α))、消除半衰期(T(1/2β))和总清除率(CL)分别为4.67 min、91.9 min和1.21%ID/g·min(-1)。此外，与(99m)Tc-MDP和(99m)Tc-ZL相比，(99m)Tc-BIBDP在骨中的摄取更高，从软组织中的清除更快。SPECT骨显像在1 h时获得清晰的骨图像。目前的研究结果表明，(99m)Tc-BIBDP在骨显像方面具有巨大潜力。
