| 黄政海,任超,吴美其,张现忠,霍力.基于AllinOne合成模块自动化合成18F-MK-6240并初步用于阿尔茨海默病[J].中国医学影像技术,2024,40(12):1909~1913 |
| 基于AllinOne合成模块自动化合成18F-MK-6240并初步用于阿尔茨海默病 |
| Automatic synthesis of 18F-MK-6240 with AllinOne synthesis module and preliminary application in Alzheimer disease |
| 投稿时间：2024-08-13 修订日期：2024-12-04 |
| DOI：10.13929/j.issn.1003-3289.2024.12.022 |
| 中文关键词: 阿尔茨海默病 tau蛋白质类 正电子发射断层显像和计算机体层摄影术 18F-MK-6240 |
| 英文关键词:Alzheimer disease tau proteins positron-emission tomography and computed tomography 18F-MK-6240 |
| 基金项目:北京协和医院中央高水平医院临床科研专项(2022-PUMCH-B-071)。 |
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| 中文摘要: |
| 目的 采用AllinOne合成模块自动化合成18F-MK-6240,初步观察其用于阿尔茨海默病(AD)的价值。方法 基于AllinOne合成模块使18F-MK-6240前体与18F－发生亲核反应而形成18F标记中间体18F-MK-6240-Boc,再经酸水解、高效液相色谱法分离及固相萃取纯化获得18F-MK-6240;对其进行质量控制。前瞻性对1例AD及1例非AD认知障碍患者行18F-MK-6240 PET/CT扫描;观察其初步应用价值。结果 基于AllinOne合成模块成功自动合成18F-MK-6240,合成时间为80 min,不校正合成效率为20.74%±2.31%,放射化学纯度＞95%,无菌检测、细菌内毒素检测、异常毒性检测及溶剂残留检测均符合国家标准。18F-MK-6240 PET/CT显示AD患者双侧额叶、顶叶、颞叶及岛叶tau蛋白沉积,非AD认知障碍患者颅内未见tau蛋白沉积。结论 基于AllinOne合成模块可自动化合成18F-MK-6240且产品质量合格,用于AD具有临床价值。 |
| 英文摘要: |
| Objective To observe the preliminary application value of 18F-MK-6240 automatically synthesized with AllinOne synthesis module in Alzheimer disease (AD). Methods Based on AllinOne synthesis module, 18F-labeled intermediate 18F-MK-6240-Boc was formed with 18F-MK-6240 precursor through nucleophilic reaction with 18F－. After hydrolyzed by acid, separated by high performance liquid chromatography and purified by solid-phase extraction, 18F-MK-6240 was obtained, and quality control was performed. 18F-MK-6240 PET/CT scanning was performed in 1 AD patient and 1 non-AD patient with cognitive impairment who were prospectively enrolled, and the preliminary application value of the product was observed. Results 18F-MK-6240 was successfully automatically synthesized based on AllinOne synthesis module, the synthesis time was 80 min, no-corrected synthesis efficiency was 20.74%±2.31%, radiochemical purity was greater than 95%, and sterility test, bacterial endotoxins test, abnormal toxicity test and solvent residual test all met national standards. 18F-MK-6240 PET/CT showed tau protein deposition of bilateral frontal, parietal, temporal and insular lobes in AD patients, while no tau protein deposition was observed in non-AD patients with cognitive impairment. Conclusion 18F-MK-6240 could be automatically synthesized based on AllinOne synthesis module, with qualified product quality and clinical application value in AD. |
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