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1.江西省肿瘤医院 核医学科 南昌 330029
2.中国人民解放军总医院 核医学科 北京 100853
[ "李海峰, 男, 1981年出生, 2011年于南昌大学获硕士学位, 化学师, 主要从事放射性药物的合成与标记", "LI Haifeng, male, born in 1981, graduated from Nanchang University with a master's degree in 2011, chemist, mainly engaged in radiopharmaceuticals' synthesis and label" ]
张锦明, E-mail:zhangjm301@163.com ZHANG Jinming, E-mail: zhangjm301@163.com
收稿日期:2016-04-03,
修回日期:2016-04-29,
纸质出版日期:2016-08
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李海峰, 张晓军, 李云钢, 等. 国产模块酸水解全自动化合成18F-FDG[J]. 核技术, 2016,39(8):080301
Haifeng LI, Xiaojun ZHANG, Yungang LI, et al. Fully automated synthesis of 18F-FDG by acidic hydrolysis on domestic module[J]. Nuclear techniques, 2016, 39(8): 080301
李海峰, 张晓军, 李云钢, 等. 国产模块酸水解全自动化合成18F-FDG[J]. 核技术, 2016,39(8):080301 DOI: 10.11889/j.0253-3219.2016.hjs.39.080301.
Haifeng LI, Xiaojun ZHANG, Yungang LI, et al. Fully automated synthesis of 18F-FDG by acidic hydrolysis on domestic module[J]. Nuclear techniques, 2016, 39(8): 080301 DOI: 10.11889/j.0253-3219.2016.hjs.39.080301.
FDG
18
F-脱氧葡萄糖(
18
F-FDG)合成模块一般仅能采用一种工艺进行生产,改变工艺条件会对产品质量造成影响,本文旨在解决此问题,同时优化生产工艺。本研究对国产碱水解FDG合成模块进行改进,省去自动加碱装置及在柱水解部件。通过研究亲核反应时间、盐酸量、水解时间及残留溶剂等影响因素,寻求酸水解合成
18
F-FDG最优化的合成工艺。从淋洗18F-离子至终产品
18
F-FDG的总合成时间为27 min,合成效率为60.27%±2.29%(
n
=37,未校正效率),产品放化纯度大于98%,产量(29.15±3.09)GBq(
n
=37)。改进的合成工艺实现了自动化、稳定合成
18
F-FDG,产品满足临床需求,实现了两种不同工艺在同一模块上制备
18
F-FDG。
Background:
2
The FDG
18
F-fluorodeoxyglucose (
18
F-FDG) synthesis module was obtained by one process of production generally. The adjusting of synthetic technology would have a significant influence on the quality of product.
Purpose:
2
In order to solve the problem and optimize the production process
in this paper
the domestic FDG synthesis module has been improved.
Methods:
2
The domestic FDG synthesis module of basic hydrolysis was optimized by removing the components of automatic alkali-adding and on-column hydrolysis. The influencing factors of synthesis process were discussed
including the time of nucleophilic reaction
the amount of HCl
the hydrolysis time and the residual solvents.
Results:
2
It took 27 min from
18
F-to final product of
18
F-FDG
and a radiochemical yield of 60.27%±2.29% (
n
=37
End of Synthesis (EOS)) was obtained. The radiochemical purity of
18
F-FDG was higher than 98% and the radioactivity was (29.15±3.09) GBq (
n
=37).
Conclusion:
2
The synthetic process was reliable and automated
and the product was suitable for clinical use. Finally
two different processes were used for synthesizing
18
F-FDG on the same module.
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K Hamacher , H H Coenen , G Stocklin , . Efficient stereospecific synthesis of no-carrier-added 2-[ 18 F]-fluoro-2-deoxy-D-glucose using aminopolyether supported nucleophicic substitution . The Journal of Nuclear Medicine , 1986 . 27 ( 2 ): 235 - 238 .
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刘 晓飞 , 张 锦明 , 田 嘉禾 , . 固相柱水解和IC-H柱中和法制备 18 F-FDG及放射性损失分析 . 国际药学研究杂志 , 2008 . 35 ( 1 ): 1 - 4 . DOI: 10.3969/j.issn.1674-0440.2008.01.001 http://doi.org/10.3969/j.issn.1674-0440.2008.01.001 .
Xiaofei LIU , Jinming ZHANG , Jiahe TIAN , . Preparation of 18 F-FDG by hydrolysis on solid phase cartridge and neutralization with IC-H cartridge and analysis of the loss of radioactive nuclide . International Journal of Pharmaceutical Research , 2008 . 35 ( 1 ): 1 - 4 . DOI: 10.3969/j.issn.1674-0440.2008.01.001 http://doi.org/10.3969/j.issn.1674-0440.2008.01.001 .
李 云钢 , 张 晓军 , 刘 健 , . 气相色谱法测量正电子放射性药物中有机溶剂残留及原因分析 . 同位素 , 2013 . 26 ( 3 ): 152 - 157 . DOI: 10.7538/tws.2013.26.03.0152 http://doi.org/10.7538/tws.2013.26.03.0152 .
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