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99Tcm直接标记洛美沙星方法研究

Direct Labeling Method of Lomefloxacin With 99Tcm

    摘要
  • 摘要: 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 150 μg，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。

     

    Abstract: The purpose of this study was to determine the best conditions in synthesis of 99Tcm lomefloxacin.Lomefloxacin was directly labeled by Na99TcmO4, 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 99Tcm-lomefloxacin was 96.98%. The optimized synthesis conditions of 99Tcm-lomefloxacin were containing 3 mg lomefloxacin, 150 μg SnCl2·2H2O, pH 6, 10 min and 60 ℃. 99Tcm lomefloxacin has an excellent radiochemical characters. 99Tcm-lomefloxacin was fat soluble. These results demonstrated that the direct labeling method of 99Tcm-
    lomefloxacin was easy and efficient.

     

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