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目的:建立简便的全自动化生产正电子放射性示踪药物2-(4’-N-11C-甲胺基苯)-6-羟基苯并噻唑(11C-PIB)的方法,满足临床诊断需要。方法:采用气相法制备11C-CH3I,11C-CH3I通过灼热的三氟磺酸银粉末转换成11C-Triflate-CH3,然后与前体2-(4’-氨基苯基)-6-羟基苯并噻唑在室温发生反应,反应混合液经半制备HPLC分离后再通过Sep-Pak C18分离柱进行固相萃取,并用0.9%无菌氯化钠溶液稀释,最后通过0.22μm的微孔无菌滤膜过滤得到注射液。结果:合成时间从加速器轰击结束开始共35 min,放化产率经过衰减校正后为48.6%(n=25),化学纯度大于97%,放化纯度大于99%。产品的无菌及无热原要求均符合规定。结论:通过计算机远程控制实现了11C-PIB注射液的全自动生产,简化了生产步骤,保证了生产的可行性和重现性,可完全满足临床需要。
Objective: To establish a simple and automated method for the production of 2- (4’-N-11C-methylaminobenzene) -6-hydroxybenzothiazole (11C-PIB) Methods: 11C-CH3I was prepared by gas-phase method. 11C-CH3I was converted into 11C-Triflate-CH3 by burning silver trifluorosulfonate powder and then reacted with precursor 2- (4’-aminophenyl) Thiazole reacted at room temperature, the reaction mixture was separated by semi-preparative HPLC and then by Sep-Pak C18 column solid phase extraction, and diluted with 0.9% sterile sodium chloride solution, and finally through a 0.22μm microporous sterile filter Filtered to give injection. Results: The synthesis time was 35 min from the end of the bombardment, and the radiochemical yield was 48.6% (n = 25) after attenuation correction. The chemical purity was over 97% and the radiochemical purity was over 99%. Sterile and pyrogen-free products are required. Conclusion: The fully automatic production of 11C-PIB injection by computer remote control has simplified the production steps and ensured the feasibility and reproducibility of production, which can fully meet the clinical needs.