自动化合成11C-Raclopride及质量控制

Automatic Synthesis and Quality Control of 11C-Raclopride for Clinical Use

  • 摘要: 采用全自动合成模块,合成临床使用的11C-Raclopride。用11C-Triflate-CH3通入含10 μL的0.5 mol/L氢氧化钠的去甲基Raclopride的200 μL的丙酮溶液中,常温反应1 min,经半制备HPLC分离,收集粗产品,再经固相萃取,用1 mL乙醇淋洗SEP-PAK C-18柱,收集淋洗液,用生理盐水稀释即得可供注射的11C-Raclopride。结果表明,反应体系中加入碱的量(1~50 μmol)对标记率影响不大,但影响了C-N甲基化的副反应产物比例。合成时间为28 min, 前体用量为0.1~0.4 mg,合成效率为(55.1±8.4)%(n=40),放化纯度大于99%,放射性浓度为370~550 MBq/mL,乙醇浓度低于10%,比活度为1.73×1014 Bq/g,产品无菌、无热源符合要求。采用11C-Triflate-CH3为标记前体,经国产商品化模块全自动合成的11C-Raclopride的质量满足临床的要求。

     

    Abstract: Automatic synthesis of 11C-Raclopride was used for routinely clinical imaging with home-made C-11 synthesized module. METHODS: 11C-Triflate-CH3 was bubbled through a vial at room temperature, containing a acetone solution of precursor and NaOH. The reaction solution was transferred to Semi-HPLC for purification. The crude production was purified by C-18 Solid-Extraction-Purification (SEP). The injection solution was formatted by 1mL alcohol eluated from the SEP-C-18, the eluated soluation was diluted with saline to less 10% of alcohol. RESULTE: The amount of base leaded to increase the yields of by production of C-N methlyation. The synthesis yield was (55.1±8.4)% (n=40) with precursor of 0.1 to 0.4 mg, and had no relationship with NaOH in 1 μmol to 50 μmol. It took 28 min from 11CO2 to obtain 11C-Raclopride injection solution. The radiochemical purity was over 99%. The radiochemical concentration was 370 to 550 MBq/mL at specific activity of 1.73×1014 Bq/g. The injection solution was proved to be sterile and pyrogen free. CONCLUSION: 11C-Raclopride was automatic synthesized from 11CH3-Triflate with home-made C-11 synthesizer module. The quality and quantity of 11C-Raclopride injection solution was confirmed to be suitable for clinical PET imaging.

     

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