~(99m)Tc-平阳霉素的制备研究

  • 摘要: 平阳霉素(PYM)的化学结构与博莱霉素的A_5组分相同。本文目的是制备~(99m)Tc-PYM以供临床评价。 我们采用改进的氯化亚锡还原方法,不通氮气,研究了pH值、搅拌时间、Sn~(2+)和PYM含量等对制备~(99m)Tc-PYM的影响,同时研究了这些标记条件(除搅拌时间外)与产品在荷瘤小鼠体内分布的关系。 实验获得最佳标记条件为 pH=5.0—6.2,每毫升高鍀酸钠溶液含氯化亚锡为 0.1—0.4μg,PYM为 0.5 mg或 0.5 mg以上。标记率可达到(96.7±0.3)%,高于过去通氮达到的 94%。产品注射1.5小时后,除肾外,肿瘤摄取居第一位,比已发表的肿瘤摄取居第二、三位的结果要好,因此认为此标记条件制成的~(99m)Tc-PYM可供临床试用研究肿瘤阳性显像。

     

    Abstract: The chemical structure of Pingyangmycin (PYM) is identical with that ofBleomycin A_5. We prepared ~(99m)Tc-PYM for clinical evaluation. Using the im-proved stannous chloride reducing method with no N_2, the effects of pH, stirringtime, Sn~(2+) and PYM concentrations were studied. The relations between theselabeling conditions (except stirring time) and the biodistribution in the tumor-bearing mice are here reported. The results indicate that the optimum conditions for ~(99m)Tc-PYM labelingare: pH 5. 0-6.2, SnCl_2 concentration of 0. 1-0. 4 μg/ml and PYM 0. 5mg/ml ormore than 0. 5mg/ml. The labeling yield of 96. 7(±0. 3)% is higher than before(94% with N_2). It was found that 1.5 hours after injection the tumor uptake wasthe highest (except kidney tissue). and better than those described in previousreports. Therefore we suggest that the ~(99m)Tc-PYM prepared with these labelingconditions may be offered on clinical trial for tumor positive imaging.

     

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