摘要
采用全自动合成模块,合成临床使用的11 C-Raclopride。用11 C-Triflate-CH3通入含10μL的0.5mol/L氢氧化钠的去甲基Raclopride的200μL的丙酮溶液中,常温反应1min,经半制备HPLC分离,收集粗产品,再经固相萃取,用1mL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28min,前体用量为0.1~0.4mg,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11 C-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。
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 1.73 ×1014 Bq/g .The injection＆amp;nbsp;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 suit‐able for clinical PET imaging .
出处
《同位素》
CAS
2014年第4期230-235,共6页
Journal of Isotopes
基金
军队医疗机构制剂标准提高项目(14ZJZ21-1)
关键词
雷氯必利
自动化合成
质量控制
raclopride
automatic synthesis
quality control
