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本文以胆固醇为原料,合成和标记了6-~(131)I胆固醇。结果表明,6-~(131)I胆固醇是一种良好和安全的肾上腺扫描剂。鉴于6-~(131)Ⅰ胆固醇的实际应用意义,我们比较系统地研究了6-I胆固醇同位素交换的各种影响因素。如载体浓度对标记率的影响,计算和验证了在不同载体浓度下交换平衡可能达到的极限值。浴温对反应速度的影响以及同位素交换的动力学特征。确定了比放为2mCi/mg的最佳标记条件,并研究了6-~(131)I胆固醇在不同温度和不同辐射剂量下的热稳定性和辐射稳定性。研究表明6-I胆固醇能在空气存在的条件下回流碘化及标记。产品也可在室温下保存。较国外报道的19-~(131)Ⅰ胆固醇具有生产工艺简便,产额高,产品质量稳定,热稳定性和辐射稳定性好,以及便于使用和保存等优点。
In this paper, cholesterol as raw material, synthesis and labeling of 6- 131I I cholesterol. The results show that 6 ~ (131) I cholesterol is a good and safe adrenal scan. In view of the practical application of 6 ~ (131) I cholesterol, we systematically studied various influencing factors of 6-I cholesterol isotope exchange. Such as the effect of carrier concentration on the labeling rate, calculated and verified the limit of exchange equilibrium possible under different carrier concentrations. Effect of bath temperature on reaction rate and kinetic characteristics of isotope exchange. The optimal labeling conditions of specific release of 2mCi / mg were determined and the thermal stability and radiation stability of 6- 131I cholesterol at different temperatures and doses were studied. Studies have shown that 6-I cholesterol reflux iodide and labeling in the presence of air. The product can also be stored at room temperature. Compared with foreign reports of 19- ~ (131) I cholesterol, the invention has the advantages of simple production process, high yield, stable product quality, good thermal stability and radiation stability, and convenient use and preservation.