^(124)I的制备、抗体标记及标记化合物的Micro-PET/CT显像  

Preparation of^(124)I,Antibody Labeling and Micro-PET/CT Imaging of Labeled Compounds

作　　者：侯兴国 王风[1] 丁缙 朱华[1] 杨志[1] HOU Xingguo;WANG Feng;DING Jin;ZHU Hua;YANG Zhi(Key Laboratory of Carcinogenesis and Translational Research(Ministry of Education/Beijing),NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals(National Medical Products Administration),Department of Nuclear Medicine,Peking University Cancer Hospital&Institute,Beijing 100142,China)

机构地区：[1]北京大学肿瘤医院暨北京市肿瘤防治研究所核医学科,国家药监局放射性药物与评价重点实验室,恶性肿瘤发病机制及转化研究教育部重点实验室,北京100142

出　　处：《同位素》2024年第4期387-393,共7页Journal of Isotopes

基　　金：国家自然科学基金(82171973,81371980);北京市医院管理中心“登峰”计划(DFL20191102)。

摘　　要：为使用医用回旋加速器生产^(124)I及研究^(124)I标记提供方法,本研究通过124Te(p,n)^(124)I核反应制备^(124)I,首先压制得到124TeO_(2)/Al_(2)O_(3)靶片,利用回旋加速器轰击3~8 h后,放置12 h去除副反应产生的杂质核素,最后通过碘升华-放化分离法得到Na^(124)I溶液。分析Na^(124)I的纯度并且标记抗间皮素(mesothelin,MSLN)抗体后,对KM小鼠进行尾静脉注射观察^(124)I-anti-MSLN的分布。结果显示,压制得到的124TeO_(2)/Al_(2)O_(3)靶片经过12.5 MeV能量,20μA质子束轰击后得到340.4~1121.1 MBq核素产品,经纯化后得274.2~758.5 MBq高纯度Na^(124)I溶液,其放射性浓度>54840 Bq/μL。使用该Na^(124)I溶液对抗MSLN抗体标记得到放化纯度>99%的^(124)I-anti-MSLN探针,经尾静脉注射入KM小鼠体内,通过Micro-PET/CT显像可以观察到小鼠甲状腺部位有明显的探针摄取,且该摄取可以被提前3 d喂食0.5%KI溶液阻断,代谢行为符合^(124)I标记的抗体探针在KM鼠体内的代谢规律。本研究总结了25次^(124)I的制备过程中涉及的设备、方法及纯化后Na^(124)I的使用等情况,结果表明,经过纯化得到的^(124)I具有较高的核纯度和化学纯度,满足放射性标记的需求,且平均回收率高于70%,自动纯化过程安全可靠。To provide a method for the production of^(124)I by using a medical cyclotron and the method of^(124)I labeling,^(124)I was prepared using a nuclear reaction of 124Te(p,n)^(124)I.Firstly,a 124TeO_(2)/Al_(2)O_(3)target was obtained by pressing,and then bombarded with a cyclotron for 3-8 hours.After 12 hours,impurity nuclides produced by the side reaction were removed.Finally,a Na^(124)I solution was obtained by iodine sublimation radiochemical separation method.Analyze the purity of Na^(124)I and label it with anti-mesothelin(MSLN)antibody,then inject it into the tail vein of KM mice to observe the distribution of^(124)I-anti-MSLN.The obtained 124TeO_(2)/Al_(2)O_(3)target was bombarded with 12.5 MeV energy and 20μA proton beam to obtain 340.4-1121.1 MBq nuclide products,and after purification,274.2-758.5 MBq of high-purity Na^(124)I solution was obtained.The final radioactive concentration of the obtained Na^(124)I solution was greater than 54840 Bq/μL.Using the Na^(124)I solution to label an anti-MSLN antibody,^(124)I-anti-MSLN probe with a radiochemical purity greater than 99%was obtained.The probe was injected into KM mice via the tail vein,and significant uptake of the probe was observed in the thyroid region of the mice through Micro-PET/CT imaging.This uptake can be blocked by feeding 0.5%KI solution 3 days in advance,and the metabolic behavior conforms to the metabolic pattern of the^(124)I labeled antibody probe in KM mice.This study summarized the purification of^(124)I samples of 25 batches in our unit,and tthe equipment and methods involved in the purification process and the use of Na^(124)I after purification were summarized.In order to provide reference for the production and efficient purification of^(124)I.The results showed that the purified^(124)I had high nuclear purity and chemical purity,which met the requirements of radiolabeling.The average recovery rate was higher than 70%,and the automatic purification process was safe and reliable.

关 键 词：固体靶核素 碘-124 碲-124靶片 ^(124)I自动纯化系统 Micro-PET/CT 

分 类 号：TL921.1[核科学技术—核燃料循环与材料] R817.4[医药卫生—影像医学与核医学]