自动化合成11C-Raclopride 及质量控制

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10μL 的0.5 mol／L氢氧化钠的去甲基Raclopride的200μL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11 C‐Raclopride。结果表明，反应体系中加入碱的量（1～50μmol）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...

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Bibliographic Details
Published in	同位素 Vol. 27; no. 4; pp. 230 - 235
Main Author	张锦明张晓军李云钢刘健徐白萱王瑞民田嘉禾
Format	Journal Article
Language	Chinese
Published	中国人民解放军总医院核医学科,北京,100853 2014
Subjects	自动化合成质量控制雷氯必利 raclopride quality control 质量控制雷氯必利自动化合成 automatic synthesis
Online Access	Get full text
ISSN	1000-7512
DOI	10.7538/tws.2014.27.04.0230

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Summary:	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10μL 的0.5 mol／L氢氧化钠的去甲基Raclopride的200μL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11 C‐Raclopride。结果表明，反应体系中加入碱的量（1～50μmol）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11 C‐Raclopride的质量满足临床的要求。
Bibliography:	11-2566/TL raclopride;automatic synthesis;quality control Automatic synthesis of 11 C‐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 injec‐tion solution was formatted by 1mL alcohol eluated from the SEP‐C‐18 ,the eluated sol‐uation 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 concen‐tration was 370 to 550 MBq/mL at specific activity of 1.
ISSN:	1000-7512
DOI:	10.7538/tws.2014.27.04.0230