^(99)Tc^m直接标记洛美沙星方法研究

Direct Labeling Method of Lomefloxacin With ^(99)Tc^m

采用Na99TcmO4对洛美沙星进行了直接标记,并对标记条件进行了优化,确定99Tcm标记洛美沙星的最佳条件,并测定了标记物的体外稳定性和脂水分配系数。结果表明,最佳标记条件为洛美沙星3 mg,SnCl2.2H2O 150μg,pH=6,温度为60℃,标记时间为10 min,所得标记物的标记率>95%,放化纯度可达96.98%;标记物体外稳定性良好,可在0.01 mol/L pH7.4的PBS中室温放置6 h,其放化纯度仍>95%;99Tcm-洛美沙星为脂溶性化合物。以上结果表明,99Tcm直接标记洛美沙星的方法操作简单,标记率较高。标记物不需分离纯化,体外稳定性好。

The purpose of this study was to determine the best conditions in synthesis of ^99Tc^m lomefloxacin. Lomefloxacin was directly labeled by Na^99Tc^mO4 , the effects on labeling yield by lomefloxacin, stannous chloride, pH and temperature were evaluated, the labeling yield, stability, and lipid/water partition coefficient were analyzed. The results showed that the labeling yield was more than 95% and the radiochemical purity of ^99Tc^m lomefloxacin was 96.98% . The optimized synthesis conditions of ^99Tc^m lomefloxacin were containing 3 mg lomefloxacin, 150μg SnCl2·2H2O, pH 6, 10 min and 60℃. ^99Tc^mlomefloxacin has an excellent radiochemical characters.^99Tc^m lomefloxacin was fat-soluble. These results demonstrated that the direct labeling method of ^99Tc^m lomefloxacin was easy and efficient.