邻碘马尿酸的几种快速标记法
SEVERAL RAPID LABELLING METHODS FOR O-IODOHBPPURIC ACID
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摘要: 本文对~(131)I标记邻碘马尿酸(OIH)的三种快速标记方法——水热熔融法(Hydrothermalmelting method),熔融法和冠醚法进行了系统的研究。水热熔融法操作简单,反应温和而安全,反应时间为15—20min、温度在152—156℃下,标记率可达到99.3%。产品用薄层层析鉴定,~(131)I标记的OIH纯度为99.3%.I~-为0.3—0.5%,OIB(邻碘苯甲酸)为 0.2%。产品经 NaHCO_3或生理盐水溶解,不经任何化学分离可直接使用。水热熔融法的同位素交换反应为均相一级同位素交换反应,服从指数定律,~(131)I与邻碘马尿酸中邻位碘发生同位素交换外,不发生其它取代反应。三种快速标记邻碘马尿酸方法的比较,我们认为水热熔融法具有标记率高、反应时间短、实验方法简单、重复性好的特点,适宜于大批量生产时使用。Abstract: Experimental results of three rapid labelling methods, namely, hydrothermal melting method, melting method and crown ether method are described. Our results indicate clearly that the hydrothermal melting method gives the highest labelling efficiency, radiochemicalContinued on P.135) purity (radioiodohippuran above 99%, radioiodide about 0.3-0.5%, radiobenzoic acid less than 0.2%) and simplicity. The product of hippuran can be used directly for clinical purposes.Reaction temperature,time dependance and pH values of initial material are investigated, and optimum condition are: temperature, 152-156℃; reaction time, 20 min; pH value, 1-2. The mechanism of isotopic exchange reaction is also studied.