诊断用碘[^(131)I]苄胍中试生产工艺研究  

A Study on the Process of Pilot Production of ^(131)I-MIBG for Diagnosis

作　　者：邵武国 秦红斌 马红利 杨云 刘常宝 李海涛 SHAO Wu- guo;QIN Hong- bin;MA Hong- li;YANG Yun;LIU Chang- bao;LIHai- tao(High Technology Atomic Co. , LTD, Beijing 102413)

机构地区：[1]原子高科股份有限公司,北京102413

出　　处：《标记免疫分析与临床》2018年第5期727-731,共5页Labeled Immunoassays and Clinical Medicine

摘　　要：目的探索最佳的诊断用碘[^(131)I]苄胍注射液中试生产工艺参数。方法采用Cu SO4催化法进行碘苄胍的^(131)I标记,纸色层法测定标记物的标记率,评价标记物的体外稳定性。结果优选的碘[^(131)I]苄胍的中试生产工艺参数为:抗坏血酸95~100mg、Cu SO4·5H2O 6~8mg、碘苄胍40~50mg、Na^(131)I溶液55.5~74GBq;反应液经0.3mol/L H2SO4溶液调节p H至1~3后于110~120℃下反应35min。碘[^(131)I]苄胍标记率和收率分别95%~99%、70%~75%。稳定性结果显示,标记物在干冰保存条件下的体外稳定性较好,放置15d后放射化学纯度降低不超过1%。结论以上结果提示,碘[^(131)I]苄胍中试生产工艺参数可控,重现性较好,为规模化碘[^(131)I]苄胍生产提供了数据支持。Objective To study the optimal parameters for ^131I-MIBG pilot production. Methods MIBG was labeled with ^131I catalyzed by CuSO4. The labeling yield, determined by paper chromatography, was used to evaluate in vitro stability of the labels. Results The preferred ^131I-MIBG pilot production process parameters were as follows; 95-100mg ascorbic acid, 6-8mg CuSO4·5H2O, 40-50mg MIBG and 55.5-74GBq Na^131I solution;The reaction liquid was adjusted to pH 1-3 by 0.3mol/L of H2SO4 solution and then reacted at 110-120℃ for 35 minutes. The labeling yield and the yield rate were 95%-99% and 70%-75%, respectively. The results of the stability tests demonstrated that in vitro stability of the labels stored in the dry ice was well accepted and the radiochemical purity was decreased by less than 1% after conserving for 15 days. Conclusion Our results indicated that the ^131I-MIBG pilot production process was well controlled with a good reproducibility, which provided data support for large-scale of ^131I-MIBG production.

关 键 词：碘[^131I]苄胍 稳定性 中试生产工艺 标记率 

分 类 号：TQ421.7[化学工程]