自动化合成11C-Raclopride及质量控制

doi:10.7538/tws.2014.27.04.0230

摘要/Abstract

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。

关键词: 雷氯必利, 自动化合成, 质量控制

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.

Key words: raclopride, automatic synthesis, quality control

张锦明;张晓军;李云钢;刘健;徐白萱;王瑞民;田嘉禾. 自动化合成¹¹C-Raclopride及质量控制[J]. 同位素, 2014, 27(4): 230-235.

ZHANG Jin-ming;ZHANG Xiao-jun;LI Yun-gang;LIU Jian;XU Bai-xuan;WANG Rui-min;TIAN Jia-he. Automatic Synthesis and Quality Control of ¹¹C-Raclopride for Clinical Use[J]. Journal of Isotopes, 2014, 27(4): 230-235.

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自动化合成¹¹C-Raclopride及质量控制

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

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