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目的探讨~(99)Tc~m 标记2-(2-甲基咪唑-1-基)-1-羟基乙烷-1,1-二膦酸(MIDP)用于骨显像的可能性。方法以2-甲基咪唑为原料,经3步反应制得 MIDP。以 SnCl_2为还原剂,加入5 mgMIDP,在 pH 值7.0下加入~(99)Tc~mO_4~-溶液,室温放置8 min 即得~(99)Tc~m-MIDP。于正常小鼠尾静脉注射1.0 MBq(0.2 ml)~(99)Tc~m-MIDP,在不同时间断头处死小鼠。取心、肝、脾、肺、肾、肌肉、骨和血等,称重后测量放射性,计算每克组织百分注射剂量率(%ID/g)及骨中放射性与各组织中放射性的比值,并计算血药清除动力学方程和各参数。新西兰兔静脉注射~(99)Tc~m-MIDP 后于不同时间显像。结果MIDP 的制备总收率为34.3%。~(99)Tc~m-MIDP 的标记率和放化纯均>90%。在3 h 时小鼠骨摄取~(99)Tc~m-MIDP 的量(A_(m,骨))为14.19%ID/g,A_(m,骨)/A_(m,血)为94.60,血药动力学方程为 C=18.849 e~(-0.254 t)+3.568 e~(-0.019 t)。兔显像结果表明,3 h 时即可获得清晰的骨显像图。结论 ~(99)Tc~m-MIDP 制备方便,骨显像清晰,是一种较有希望的新型骨显像剂。
Objective To explore the possibility of using 99 Tc m labeled 2- (2-methylimidazol-1-yl) -1-hydroxyethane-1,1-diphosphonic acid (MIDP) for bone imaging. Methods 2-methylimidazole was used as starting material to prepare MIDP after 3 steps. Add SnCl_2 as reducing agent, add 5 mgMIDP, add ~ (99) Tc ~ mO 4 ~ - solution at pH 7.0, and place ~ 99 Tc m-MIDP at room temperature for 8 min. The normal mice were injected 1.0 MBq (0.2 ml) ~ (99) Tc ~ m-MIDP into the caudal vein and the mice were sacrificed at different times. Heart, liver, spleen, lung, kidney, muscle, bone and blood were weighed, the radioactivity was weighed, the percent of injected dose per gram of tissue (% ID / g) and the ratio of radioactivity in bone to radioactivity in each tissue , And calculate the plasma clearance kinetic equation and the parameters. New Zealand rabbits were intravenously injected with ~ (99) Tc ~ m-MIDP at different times. The overall yield of MIDP was 34.3%. The labeling and radiochemical purity of ~ (99) Tc ~ m-MIDP were> 90%. The amount of ~ (99) Tc ~ m-MIDP was (14.19% ID / g) and the amount of A_ (m, The pharmacokinetic equation was C = 18.849 e ~ (-0.254 t) +3.568 e ~ (-0.019 t). Rabbit imaging results show that 3 h when you can get a clear bone imaging. Conclusion ~ (99) Tc ~ m-MIDP has the advantages of convenient preparation, clear bone imaging and is a promising new bone imaging agent.