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江 骁, 王潇雄, 陆 皓, 等.CFN-MPS-200模块自动化制备 18F-FLT及其质量控制与生物评价.四川大学学报(医学版),2017,48(2):295-298
CFN-MPS-200模块自动化制备 18F-FLT及其质量控制与生物评价
Quality Control and Biological Assessment of Automated Synthesized 3′-deoxy-3′- 18F-fluorothymidine using CFN-MPS-200 Module
  
中文关键词:  【关键词】 18F-FLT PET分子探针 放射性药物 自动合成 PET扫描
英文关键词:【Key words】 18F-FLT PET tracer Radiopharmaceutical Automated synthesis PET scanning
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中文摘要:
      【摘要】 目的 利用CFN-MPS-200型自动合成模块制备3′-脱氧-3′-[氟-18]氟胸腺嘧啶(3′-deoxy-3′-18F-fluorothymidine, 18F-FLT),并对其进行质量分析,最后在Wistar大鼠体内对18F-FLT进行生物评价。 方法 以3-N-t-叔丁氧羰基-1-[5′-O-(4,4′-二甲氧基三苯甲基)-2′-脱氧-3′-O-(4-硝基苯磺酰基)-β-D-苏型-呋喃戊糖基]胸苷(3-N-Boc-5′-O-dimethoxytrityl-3′-O-nosyl-thymidine, Boc-FLT)为原料,用CFN-MPS-200型自动合成模块合成无溶剂残留的18F-FLT,通过radio-高效液相色谱(high performance liquid chromatography, HPLC)和radio-薄层色谱(thin layer chromatography, TLC)进行质量控制,在健康Wistar大鼠体内进行正电子发射断层显像(PET显像)。 结果 基于CFN-MPS-200多功能合成模块自动化合成18F-FLT的时间约为60 min,合成产率约为(24±5)%(衰减校正,n =20),放化纯大于99%,放射性浓度约为1.11×109 Bq/mL。产品为无色透明溶液,pH值在7.0~8.0之间,放化纯度大于99%。18F-FLT在正常Wistar大鼠体内主要浓聚在肾、膀胱、骨髓、肝,在其他部位分布较低。 结论 利用CFN-MPS-200多功能合成模块制备的18F-FLT方法稳定,产率高,安全无溶剂,产品质量控制指标合格。
英文摘要:
      【Abstract】 Objective To synthesize 3′-deoxy-3′-18F-fluorotyhymidine(18F-FLT) using CFN-MPS-200 automatic synthesis module, and evaluate its distribution in Wistar rats. Methods We used 3-N-Boc-5′-O-dimethoxytrityl-3′-O-nosyl-thymidine (Boc-FLT)-percursor as raw material to synthesize 18F-FLT without residual solvents. Its radiochemical purity was confirmed with radio-HPLC and thin layer chromatography (TLC). Normal Wistar rats were injected with 18F-FLT and underwent PET scanning. Results The entire preparation procedure took about 60 min, which resulted in a radio chemical yield of (24±5)% (after attenuation correction, n =20) and radiochemical purity of over 99%, with 1.11×109 Bq/mL specific activity. The 18F-FLT solution was colorless and had a pH value between 7.0-8.0. 18F-FLT was mainly concentrated in the kidney, bladder, liver, bone marrow and Liver of normal Wistar rats. Conclusion Automated synthesis of 18F-FLT using CFN-MPS-200 is a stable method, with high yield, safety without solvent, and acceptable quality.
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