【摘要】 采用改良的氯胺T法,先用稳定的NaI与紫杉醇(Paclitaxel)作用,再以放射性Na125I标记紫杉醇,建立125I标记紫杉醇的方法。采用纸层析及HPLC测定标记产物的标记率、纯化后的放化纯度,采用纸层析法测定标记产物在不同温度及不同的储存溶剂中的体外稳定性,红外光谱鉴定产物。结果显示,采用改良氯胺T法标记率约63.1%±5.7%,放化纯度约96.3%±1.3%;标记物储存于4℃生理盐水或乙醇储存体系中241、20 h,放化纯度分别>95%和约90%;在血浆中稳定性也较好,在4、37℃放置24 h,放化纯度分别为92.3%±0.4%、89.5%±0.6%。以上结果表明,改良氯胺T法标记紫杉醇具有方法简便、标记率高、标记产物稳定性较好的特点,能够满足放射性示踪实验的要求。更多还原

【Abstract】 The modified Ch-T labeling method has been investigated.Firstly,the paclitaxel was reacted with non-radioactive NaI.Then the mixture was radiolabeled with 125I by modified Ch-T method.The radiolabeling yield was analyzed by thin paper chromatography and HPLC.After purified,the radiochemical purity and stability of the radiolabeled compounds were tested in vitro under different conditions,such as temperature or solvent and the final labeled compound was identified by infrared spectra.The radiolabeled yield of the compound produced by the modified Ch-T method was compared with those produced by the nitric acid oxidization method and the common Ch-T method.The radiolabeling yield of the labeled compound produced by the modified Ch-T method was about 63.1%±5.7% and the radiochemical purity was about 96.3%±1.3%.After 24 hours stored in NS or alcohol system at 4℃,the radiochemical purity of the product was above 95%,and 90% after 120 h.The labeled product was also stable in serum,after 24 h stored at 4 ℃ and 37 ℃,the radiochemical purities were 92.3%±0.4% and 89.5%±0.6% respectively.The modified Ch-T method was simple and convenient.The radiolabeling yield was high and the labeled compound was stable.It was qualified for the isotopic tracing experiment in vivo.更多还原