Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine, Songpa-gu, Seoul 138-736, South Korea.
Nucl Med Biol. 2011 May;38(4):593-7. doi: 10.1016/j.nucmedbio.2010.11.012. Epub 2011 Mar 3.
We describe new [(18)F]Fluoropropylcarbomethoxyiodophenyl-nor-tropane ([(18)F]FP-CIT) automatic preparation method by (1) using 2-methyl-2-butanol as [(18)F]fluorination solvent, (2) base amount control to minimize side reaction and (3) salt elution method to elute trapped [(18)F]fluoride. We developed manual synthesis procedures for automatic synthesis application. In this manual synthesis, we trapped [(18)F]F(-) on ion exchange cartridge and eluted with 0.2 M potassium methanesulfonate solution. We have [(18)F]fluorination at 100°C with 2-methyl-2-butanol as protic solvent for [(18)F]fluorination. After high-performance liquid chromatography analysis, we have 69.3±3.2% of [(18)F]F(-) incorporation ratio on the manual synthesis and applied these conditions to automatic preparation with GE TracerLab FX module. After setting-up of automatic synthesis and quality control procedures for clinical procedures, we have routine production of [(18)F]FP-CIT with 86.9±9.5 GBq/2.5 ml of [(18)F]F(-) as initial radioactivity and have 192 productions for 1.5 year. We have 42.5±10.9% of decay corrected radiochemical yields and they were satisfied all quality control procedures and stability to 6 h. New [(18)F]FP-CIT automatic preparation method showed high and reliable radiochemical yield and we could have enough >35 patient doses of [(18)F]FP-CIT from one production.
我们描述了一种新的 [(18)F] 氟丙基羰甲基碘代苯-nor 托烷 ([(18)F]FP-CIT) 自动制备方法，（1）使用 2-甲基-2-丁醇作为 [(18)F] 氟化溶剂，（2）通过碱量控制将副反应降到最低，（3）使用盐洗脱法洗脱捕获的 [(18)F] 氟化物。我们为自动合成应用开发了手动合成程序。在这种手动合成中，我们将 [(18)F]F(-) 捕获在离子交换柱上，并用 0.2 M 甲烷磺酸钾溶液洗脱。我们在 100°C 下用 2-甲基-2-丁醇作为亲核溶剂进行 [(18)F] 氟化。经过高效液相色谱分析，我们在手动合成中获得了 69.3±3.2%的 [(18)F]F(-) 结合率，并将这些条件应用于 GE TracerLab FX 模块的自动制备中。在建立了自动合成和临床程序的质量控制程序后，我们已经可以常规生产 [(18)F]FP-CIT，初始放射性为 86.9±9.5GBq/2.5ml [(18)F]F(-)，在 1.5 年内进行了 192 次生产。我们获得了 42.5±10.9%的衰变校正放射性化学产率，这些产率满足了所有质量控制程序和 6 小时的稳定性要求。新的 [(18)F]FP-CIT 自动制备方法显示出高且可靠的放射性化学产率，我们可以从一次生产中获得足够的用于 35 名以上患者的 [(18)F]FP-CIT 剂量。
