正电子药物^(11)C-β-CFT的合成及质量控制  

Synthesis and quality control of positron drug ^(11)C-β-CFT

作　　者：李毓斌[1] 张奇洲[1] 秦永德[1] LI Yubin;ZHANG Qizhou;QIN Yongde(Department of Nuclear Medicine, the First Affiliated Hospital of Xinjiang Medical University, Urumqi 830054, Chin)

机构地区：[1]新疆医科大学第一附属医院核医学科,乌鲁木齐830054

出　　处：《新疆医科大学学报》2018年第5期581-584,共4页Journal of Xinjiang Medical University

基　　金：新疆医科大学第一附属医院自然科学基金(2015ZRQN06)

摘　　要：目的通过对GE公司多功能碳合成器Tracerlab FXC进行改造,实现^(11 )C-β-CFT稳定地自动化合成,并对^(11 )C-β-CFT的合成进行了质量控制。方法改造合成器上不参与反应的装置,以^(11 )CO_2为起始原料在催化剂作用下与I_2生成^(11 )CH_3I,再转化成Triflate-^(11 )CH_3,最后与nor-β-CFT进行甲基化反应,采用固相萃取法分离纯化制得^(11 )C-β-CFT。通过性状检查、pH值检查、放射化学纯度测定、细菌内毒素检查、无菌检查和放射性浓度检查对^(11 )C-β-CFT注射液进行质量控制。结果经改造后连续5次合成^(11 )C-β-CFT,所得^(11 )C-β-CFT注射液为无色透明的无菌无热原的溶液,其放射化学纯度>95%,均符合规定。用制备的^(11 )C-β-CFT对正常志愿者与帕金森患者进行PET显像,PET显像显示正常对照者双侧纹状体显像清晰,帕金森病患者双侧纹状体不对称性和摄取性降低。结论系统改造后操作简单,可安全、快速地合成^(11 )C-β-CFT,所得产品放化纯度高,产率稳定,可满足临床应用要求。Objective Through the transformation of Tracerlab FXC manufactured by GE′s multifunctional carbon synthesizer,to achieve a stable and automated synthesis of ^（11 ）C-β-CFT,and perform the necessary quality control of ^（11）C-β-CFT.Methods The device that does not participate in the reaction was reconstructed on the synthesizer.^（11）C-CO_（2 ）was used as the starting material to generate ^（11）CH_3I with I_2under the action of the catalyst,and then converted into Triflate-^（11）CH_3.Finally,the methylation reaction with nor-β-CFT was performed using solid-phase extraction.Then it was separated and purified to obtain ^（11 ）C-β-CFT.The quality control of the ^（11 ）C-β-CFT injection was performed by character check,pH check,radiochemical purity measurement,bacterial endotoxin test,sterility test,and radioactive concentration test.Results ^（11）C-β-CFT was synthesized successively after five times modification.The resulting ^（11 ）C-β-CFT injection was a colorless,transparent and sterile pyrogen-free solution with a radiochemical purity of95%.PET imaging was conducted on normal volunteers and Parkinson＇s disease using prepared ^（11 ）C-β-CFT.PET imaging revealed bilateral striatum imaging in normal controls and bilateral striatum asymmetry and reduced uptake in patients with Parkinson＇s disease.Conclusion The modified system is simple in operation and can safely and rapidly synthesize the ^（11 ）C-β-CFT.The resulting product has high radiochemical purity and stable yield,which can meet the requirements of clinical application.

关 键 词：^11C-β-CFT 质量控制 化学合成 

分 类 号：R914[医药卫生—药物化学]