中华核医学与分子影像杂志
中華覈醫學與分子影像雜誌
중화핵의학여분자영상잡지
Chinese Journal of Nuclear Medicine and Molecular Imaging
2015年
4期
303-305
,共3页
陈礼平%张雨%吴娜静%尤徐阳%程亮%万卫星
陳禮平%張雨%吳娜靜%尤徐暘%程亮%萬衛星
진례평%장우%오나정%우서양%정량%만위성
FMISO%同位素标记%氟放射性同位素%化学合成
FMISO%同位素標記%氟放射性同位素%化學閤成
FMISO%동위소표기%불방사성동위소%화학합성
FMISO%Isotope labeling%Fluorine radiotopes%Chemical synthesis
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(NITFP)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,注入生理盐水得到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 18 F-FMISO的自动化合成时间约为60 min,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1.11×1012 Bq/L.产品为无色澄清溶液,pH值7.0,氨基聚醚(K222)含量低于25 μg/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.
目的 製備18F-氟硝基咪唑(FMISO)併進行質量分析.方法 採用基于標記前體1-(2'-硝基-1'-咪唑基)-2-氧-四氫吡喃基-3-氧-甲苯磺酰基-丙二醇(NITFP)的“一鍋法”,利用CFN-MPS-100氟多功能放射性藥物化學閤成模塊,在密閉的平底反應瓶中依次完成放射性氟化反應、水解反應,粗產品經過半製備HPLC分離純化後鏇蒸除去溶劑,註入生理鹽水得到18F-FMISO註射液.採用HPLC和TLC等方法測定放化純等質量控製指標.結果 18 F-FMISO的自動化閤成時間約為60 min,放化產率為(32±5.0)％(未衰減校正,n=25),放化純大于99.0％,放置6h仍大于98.5％,放射性濃度大于1.11×1012 Bq/L.產品為無色澄清溶液,pH值7.0,氨基聚醚(K222)含量低于25 μg/ml,覈素純度大于99％.結論 基于CFN-MPS-100氟多功能模塊的18F-FMISO自動化閤成方法穩定,產率高,產品穩定性好、化學純度高.
목적 제비18F-불초기미서(FMISO)병진행질량분석.방법 채용기우표기전체1-(2'-초기-1'-미서기)-2-양-사경필남기-3-양-갑분광선기-병이순(NITFP)적“일과법”,이용CFN-MPS-100불다공능방사성약물화학합성모괴,재밀폐적평저반응병중의차완성방사성불화반응、수해반응,조산품경과반제비HPLC분리순화후선증제거용제,주입생리염수득도18F-FMISO주사액.채용HPLC화TLC등방법측정방화순등질량공제지표.결과 18 F-FMISO적자동화합성시간약위60 min,방화산솔위(32±5.0)％(미쇠감교정,n=25),방화순대우99.0％,방치6h잉대우98.5％,방사성농도대우1.11×1012 Bq/L.산품위무색징청용액,pH치7.0,안기취미(K222)함량저우25 μg/ml,핵소순도대우99％.결론 기우CFN-MPS-100불다공능모괴적18F-FMISO자동화합성방법은정,산솔고,산품은정성호、화학순도고.
Objective To synthesize 18F-FMISO and analyze the quality of the product.Methods 1-(2'-nitro-l'-imidazolyl)-2-O-tetrahydropyranyl-O-trluendulfonylpropanediol (NITIT) was taken as the precursor and simple "one pot" method was used.CFN-MPS-100 fluorine multifunction radiopharmaceutical 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 evaporation.Then 15 ml saline was added into the product to get 18F-FMISO injection.Radio-HPLC and radio-TLC were applied for quality control.Results 18F-FMISO was obtained in 60 min with the radiochemical 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 25 μg/ml.Conclusion 18 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.
