肿瘤显像药物^(11)C-胆碱的合成工艺优化研究  

Process Development for the Synthesis of ^(11)C-choline as Tumor Imaging Agents

作　　者：龙婷婷 周明[1] 杨能安 李建[1] 陈小娟 胡硕[1] LONG Tingting;ZHOU Ming;YANG Neng’an;LI Jian;CHEN Xiaojuan;HU Shuo(PET Center,Xiangya Hospital,Central South University,Changsha,Hunan,410008,China;Department of Pharmacy,Hunan Cancer Hospital/,the Affiliated Cancer Hospital of Xiangya School of Medicine,Central South University,Changsha,Hunan,410013,China)

机构地区：[1]中南大学湘雅医院PET中心,湖南长沙410008 [2]湖南省肿瘤医院/中南大学湘雅医学院附属肿瘤医院药学部,湖南长沙410013

出　　处：《肿瘤药学》2018年第3期324-328,共5页Anti-Tumor Pharmacy

基　　金：中南大学院内基金

摘　　要：目的 ^(11)C-胆碱目前被广泛应用于前列腺癌、脑肿瘤、肺癌等多种肿瘤的诊断、治疗及疗效评价研究。由于该显像药物半衰期只有20 min,优化其产率具有非常重要的意义。本实验拟研究不同前体载体对^(11)C-胆碱最终产率的影响。方法 GE回旋加速器每次轰击生产相近活度(7.4 GBq)的反应原料^(11)CH3I,对比传统商用Plus C18柱和自制Light C18柱作为标记前体载体时产物^(11)C-胆碱的产量。通过HPLC进行质控以后,再对志愿者进行显像分析(注射活度为(370±37)MBq)。结果使用Light C18柱时^(11)C-choline产率为(58.2±1.24)%,明显优于传统Plus C18柱的产率(22.9±0.68)%,差异有统计学意义(P<0.01)。HPLC结果显示产品溶液放化纯度均大于99%,且对病人进行显像时均无明显不良反应,在体内的放射性分布基本一致,对肿瘤病灶检出度良好。结论经过工艺优化,使用Light C18柱时^(11)C-胆碱的标记产率得到较大提升,具有一定的临床意义。Objective 11C-choline has been widely used for the diagnosis and staging of many cancers,such as prostate cancer,lung cancer,brain cancer and so on.Due to its short half-time(20 min),it would be significant to improve the radiochemical yield of 11C-choline.The aim of this study was to investigate the influence of different precursor carrier on the radiochemical yield of 11C-choline.Methods Approximately 7.4GBq of reactive material 11C-methyl iodide were collected in the CH3I trap every time.11C-choline was synthesized by using Plus or Light C18 cartridges as precursor carrier.The purity of 11C-choline in the final product was established by high-performance liquid chromatography(HPLC).Then,the subjects were injected with 370MBq±37MBq of 11C-choline to perform the PET/CT scan.Results 11Ccholine was synthesized with two kinds of C18 cartridge three times,respectively.The radiochemical yield of 11C-choline with Light C18 cartridges[(58.2±1.24)%]was obviously higher than that with Plus C18 cartridges[(22.9±0.68)%],which had a significant statistical difference.The radiochemical purity of the 11C-choline was greater than 99%.Moreover,no adverse effects were observed in patients.The radioactivity distribution of the two kinds of 11C-choline was almost the same in patients.The 11C-choline with Light C18 cartridges also got high tumor detection rate.Conclusion The radiochemical yield of 11C-choline with Light C18 cartridges increased obviously compared with the traditional synthesis method of 11C-choline.It will be a promising alternative solution for its clinical application.

关 键 词：11C-胆碱 放射合成 肿瘤显像 

分 类 号：R542.22[医药卫生—心血管疾病]