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同位素  2014 

自动化合成11C-Raclopride及质量控制

DOI: 10.7538/tws.2014.27.04.0230, PP. 230-235

Keywords: 雷氯必利,自动化合成,质量控制

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Abstract:

采用全自动合成模块,合成临床使用的11C-Raclopride。用11C-Triflate-CH3通入含10μL的0.5mol/L氢氧化钠的去甲基Raclopride的200μL的丙酮溶液中,常温反应1min,经半制备HPLC分离,收集粗产品,再经固相萃取,用1mL乙醇淋洗SEP-PAKC-18柱,收集淋洗液,用生理盐水稀释即得可供注射的11C-Raclopride。结果表明,反应体系中加入碱的量(1~50μmol)对标记率影响不大,但影响了C-N甲基化的副反应产物比例。合成时间为28min,前体用量为0.1~0.4mg,合成效率为(55.1±8.4)%(n=40),放化纯度大于99%,放射性浓度为370~550MBq/mL,乙醇浓度低于10%,比活度为1.73×1014Bq/g,产品无菌、无热源符合要求。采用11C-Triflate-CH3为标记前体,经国产商品化模块全自动合成的11C-Raclopride的质量满足临床的要求。

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