FDG合成模块流程.docVIP

FDG模块自动化合成2-18F-乙酸盐及其临床前研究 —转载 FDG模块自动化合成2-乙酸盐及其临床前研究 张锦明 田嘉禾 姚树林 刘晓飞 刘振峰 郭喆 【摘要】 目的 研究国产商用-FDG模块自动化合成2-乙酸盐的可行性及其肿瘤显像。方法在商用FDG模块上未经修改参数，采用柱色层水解和纯化合成2-乙酸盐，并进行了放化纯、稳定性检测，生物学分布实验及荷乳腺癌和肺腺癌小鼠显像。结果 采用商用FDG模块自动化合成2-乙酸盐，无需高效液相色谱 HPLC 法纯化，时间短，产率高，平均合成效率达59.3％，放化纯 99％，合成时间为23 min。2-乙酸盐的稳定性高，毒性较低，正常鼠生物学分布示血液清除慢，PET显像示乳腺癌和肺腺癌特异性摄取示踪剂。结论2-乙酸盐是一种有潜在应用前景的肿瘤显像剂。 【关键词】 乙酸盐类；氟放射性同位素；化学合成；放射性核素显像;小鼠 Fully automated synthesis of -fluoroacetate on FDG synthesizer and preclinical study ZHANG Jin-ming，TIAN Jia-he，YAO Shu-lin，et al．Department of Nuclear Medicine，The PLA General Hospital，Beijing 100853，China 【Abstract】0bjective Radiolabeled acetate was considered a potential tracer complimentary to -FDG．The aim of the current study Was to investigate and validate the feasibility of fully automated synthesisof -fluoroacetate by a commercial synthesizer of FDG．Methods -fluoroacetate Was synthesized onFDG synthesizer with column hydrolyze and purification on Sep-Pak column．The radiochemical purity andthe stability were measured by thin layer chromatography TLC and high performance liquid chromatography HPLC ．The biodistribution in NH mice Was studied．PET imaging Was performed on mice models bearing breast or lung cancers．Results -fluoroacetate Was successfully synthesized with FDG synthesizer．avoiding time-consuming HPLC purification and reducing the cost．The yield Was 59.3％ end of synthesis in a short time 23 min with radiochemical purity higher than 99％．The stability of -fluoroacetate Was high at room temperature, and toxicity low to NH mice．The slower clearance from blood Was observed in NH mice．-fluoroacetate PET imaging showed radioactive uptake in the lesions bore by micemodels．Conclusion -fluoroacetate could be synthesized with FDG module and of potential in tumor imaging． 【Key words】 Acetates；Fluorine radioisotopes；Chemical synthesis；Radionuclide imaging；Mice 1986年Sykes等[1]合成了2-乙酸盐，并研究了其生物学分布。后又证实2-乙酸盐体内生物学分布同-乙酸盐类似，氧化成氟柠檬酸后不能被进一步代谢，因此可用于研究心肌代谢和局部氧代谢。进一步研究发现，复发的前列腺癌特异性摄取2-乙酸盐，其靶／本底比值高于