^(99m)Tc标记雷尼替丁的合成

SYNTHESIS OF ^(99m)Tc—LABELLED RANITIDINE

一、引言雷尼替丁系一种临床用抗溃疡类药物。从其分子结构式上看,不能直接与^(99m)Tc进行络合,应先将其硝基功能团还原,再用双功能偶联剂DTPA偶联(常把DTPA制成环状酸酐,以增强其反应活性);然后在适当条件下进行^(99m)Tc的放射标记。把标记偶联物^(99m)Tc-R-CDTPA添加入一种特定的辅料配方里(配方系由中国药科大学,药剂教研室屠锡德教授提供),压制成一种胃内滞留漂浮片剂,并同时与一种普通片剂作对照研究。

This article describes a double-function conjugation method of^(99)Tc-labelled ranitidine, First of group (NO_2) of ranitidine was reduced with SnCl_2 under the special conditions, and then DTPA anhydride was conjugated with it. The reaction mixture must be purified to separate free DTPA from R-CDTPA by dialysis method. RCDTPA Was labelled with ^(99m)TC. The labelling yield Was determined by paper chromatography, radiochemical purity of ^(99m)Tc-R-CCTPA is more than 99%. The initial results of clinical experiments have shown that the dynamic studies of ranitidine drug in vivo are very satisfied.