Wang Min, Arkins Chase A, Snyder Scott E
Molecular Imaging Ligand Development Program, Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN, USA.
Molecular Imaging Ligand Development Program, Department of Radiology and Imaging Sciences, Indiana University School of Medicine, Indianapolis, IN, USA.
Appl Radiat Isot. 2025 Jul;221:111802. doi: 10.1016/j.apradiso.2025.111802. Epub 2025 Mar 22.
A reliable and fully automated method for synthesis, purification and formulation of [F]FCH on the GE FASTlab II utilizing a single-use cassette was reported. The radiosynthesis sequences of [F]FCH was written based on the two-step, gas phase synthesis methodology. Dibromomethane (DBM) was fluorinated with no-carrier-added [F]fluoride ion, assisted by K/KCO to afford [F]fluorobromomethane ([F]FBM) as a gas. [F]FCH was then prepared by bubbling [F]FBM through Sep-Pak Silica cartridges to react with dimethylethanolamine (DMAE) preloaded on Sep-Pak C18 cartridge. The resulting [F]FCH was purified using Sep-Pak C18 and Accell CM cartridges in series. The purified [F]FCH was eluted from the CM cartridge and formulated with 0.9 % sodium chloride for injection. With this method, the radiochemical yield of [F]FCH was 17.8 ± 2.5 % with a high radiochemical purity (>99 %). Three consecutive [F]FCH validation runs were performed, and all quality control parameters met the release criteria for human use. This method is quite straightforward utilizing single-use cassettes. [F]FCH was reproducibly produced at sufficiently high radioactive concentration for multiple preclinical or human imaging doses from a single radiosynthesis.
报道了一种在通用电气FASTlab II上利用一次性盒进行[F]FCH合成、纯化和制剂制备的可靠且完全自动化的方法。[F]FCH的放射性合成序列基于两步气相合成方法编写。在K/KCO辅助下，用无载体添加的[F]氟离子对二溴甲烷（DBM）进行氟化，得到气态的[F]氟溴甲烷（[F]FBM）。然后将[F]FBM鼓泡通过Sep-Pak硅胶柱，使其与预载在Sep-Pak C18柱上的二甲基乙醇胺（DMAE）反应，制备[F]FCH。所得的[F]FCH依次使用Sep-Pak C18柱和Accell CM柱进行纯化。纯化后的[F]FCH从CM柱上洗脱下来，并用0.9%的注射用氯化钠制剂。采用该方法，[F]FCH的放射化学产率为17.8±2.5%，放射化学纯度高（>99%）。进行了连续三次[F]FCH验证运行，所有质量控制参数均符合供人使用的放行标准。该方法使用一次性盒非常简便。从单次放射性合成中，以足够高的放射性浓度可重复生产出用于多次临床前或人体成像剂量的[F]FCH。
