CFN-MPS-200模块自动化制备 18F-FLT及其质量控制与生物评价

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

Quality Control and Biological Assessment of Automated Synthesized 3′-deoxy-3′- 18F-fluorothymidine using CFN-MPS-200 Module

摘要

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。

Abstract: 【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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