基于CFN—MPS-100模块的18F-FMISO自动化合成与质量分析  

Automated synthesis and quality analysis of 18F-FMISO based on CFN-MPS-100 module

作　　者：陈礼平[1] 张雨[1] 吴娜静[1] 尤徐阳[1] 程亮 万卫星[1] 

机构地区：[1]江南大学附属医院、无锡第四人民医院核医学科,214062 [2]北京安迪科生物技术有限公司

出　　处：《中华核医学与分子影像杂志》2015年第4期303-305,共3页Chinese Journal of Nuclear Medicine and Molecular Imaging

基　　金：无锡市医院管理中心医学技术联合攻关项目（YGZX1214）

摘　　要：目的制备18F-氟硝基咪唑（FMISO）并进行质量分析。方法采用基于标记前体1-（2＇-硝基-1’-咪唑基）-2．氧-四氢吡喃基-3-氧-甲苯磺酰基-丙二醇（NITYP）的“一锅法”，利用CFN-MPS-100氟多功能放射性药物化学合成模块，在密闭的平底反应瓶中依次完成放射性氟化反应、水解反应，粗产品经过半制备HPLC分离纯化后旋蒸除去溶剂，注人生理盐水得到18F-FMISO注射液。采用HPLC和TLC等方法测定放化纯等质量控制指标。结果18F—FMISO的自动化合成时间约为60min，放化产率为（32±5．0）％（未衰减校正，n=25），放化纯大于99．0％，放置6h仍大于98．5％，放射性浓度大于1．11×10^12Bq／L。产品为无色澄清溶液，pH值7．0，氨基聚醚（K222）含量低于25μg／ml，核素纯度大于99％。结论基于CFN-MPS-100氟多功能模块的18F-FMISO自动化合成方法稳定，产率高，产品稳定性好、化学纯度高。Objective To synthesize 18F-FMISO and analyze the quality of the product. Methods 1- （2＇-nitro- l＇-imidazolyl ） -2-O-tetrabydropyranyl-O-trluenduffonylpropanediol （ NITTP ） was taken as the precursor and simple ＂one pot＂ method was used. CFN-MPS-100 fluorine multifunetion radiopharmaeeutieal chemical synthesis module was adopted to complete the radioactive fluorination reaction in a closed flat flask, and the crude product was purified by semi-preparative HPLC, the solvent was removed by rotary e- vaporation. Then 15 ml saline＂ was added into the product to get ISF-FMISO injection. Radio-HPLC and ra- dio-TLC were applied for quality control. Results 1SF-FMISO was obtained in 60 min with the radioehemi cal yield of （32±5.0）% （no decay corrected, n = 25）. The radiochemical purity was above 99.0% and still above 98.5% after 6 h. The radioactive concentration was above 1.11×1012 Bq/L. The product was colorless solution, with pH value of 7.0. The radioactive nuclear purity was more than 99%. The K222 was less than 25μg/ml. Conelusion is F-FMISO could be synthesized with automatic synthesis method based on the CFN-MPS-100 fluorine multifunction module. The labeling rate, stability and chemical purity are high.

关 键 词：FMISO 同位素标记 氟放射性同位素 化学合成 

分 类 号：R917[医药卫生—药物分析学] R914.5[医药卫生—药学]