同位素 ›› 2020, Vol. 33 ›› Issue (3): 167-172.DOI: 10.7538/tws.2018.youxian.099

• 放射性同位素应用技术 • 上一篇    下一篇

18F]-苯丙氟硼酸的制备工艺改进及初步临床应用

周明;李玉来;杨能安;李建;陈小娟;胡硕   

  1. 中南大学湘雅医院 PET中心,湖南 长沙410008;湖南省肿瘤医院 药学部,湖南 长沙410013
  • 出版日期:2020-06-20 发布日期:2020-09-12

Modified Synthesis and Clinical Trial of [18F]-Phe-BF3

ZHOU Ming;LI Yulai;YANG Neng’an;LI Jian;CHEN Xiaojuan;HU Shuo   

  1. PET Center, Xiangya Hospital, Central South University, Changsha 410008, China;Department of Pharmacy, Hunan Cancer Hospital, Changsha 410013, China
  • Online:2020-06-20 Published:2020-09-12

摘要:

为优化新型显像剂[18F]-苯丙氟硼酸的放射标记工艺及初步临床应用,本研究以苯丙氟硼酸为底物,采用同位素交换方法直接标记,实验组以pH=2的NaCl溶液为18F-的淋洗液,以Sep-Park Light Al2O3柱为纯化柱;对照组以K2.2.2/K2CO3溶液为淋洗液,以Sep-Park Light C18柱为纯化柱。产物质控完成后用胶质瘤细胞系U87 MG进行特异性细胞摄取实验,并对健康志愿者进行PET/CT显像。结果表明:实验组产率和放化纯度分别是(10.26±0.42)%和大于99%,对照组产率和放化纯度分别为(4.16±0.26)%和大于99%,对照组产品溶液K2.2.2残留量大于50 mg/L。细胞摄取实验中实验组计数率为(9.6±1.5)/min-1,阻断组计数率为(7.5±1.1)/min-1,游离18F对照组计数率为(4.4±0.9)/min-1。健康志愿者PET显像结果提示,该显像剂在体内血液中清除很快,主要通过肾脏排泄,脑等其他脏器均无明显摄取。结果显示,改良[18F]-苯丙氟硼酸的标记方法不仅产率明显高于传统标记方法,质控检测项目以及检测结果也具有一定的优越性。此外,较好的细胞摄取率和体内分布也提示该显像剂有可能成为诊断脑胶质瘤等肿瘤疾病的良好显像剂。

关键词: 苯丙氟硼酸, 18F放射性标记, PET/CT, 胶质瘤

Abstract:

To improve the technology of fluorine-18 labelling of (1-ammonio-2-phenylethyl)trifluoroborate (Phe-BF3). Phe-BF3 was labelled by isotope exchange. Experimental groups used sodium chloride aqueous solution (pH=2) to elute fluorine-18 and the product solution was collected when the reaction system passed through an alumina cartridge; Control groups used K2.2.2/K2CO3 solution to elute fluorine-18 and the product was concentrated by a C18 cartridge first. Then, the product was eluted by 2 mL ethyl alcohol. After quality control, we used U87 glioma cells to study the specific binding experiment and then we performed PET imaging on healthy volunteers. The radiochemical yield of experimental groups was 10.6%, 9.78% and 10.4% and that of control grxoups were 3.86%, 4.28% and 4.33%. The radiochemical purity was more than 99% and the concentration of K2.2.2 was more than 50 mg/L in control group. In the cell experiment, experimental group cell counting rate was (9.6±1.5)/min-1, block group was (7.5±1.1)/min-1 and control group was (4.4±0.9)/min-1. What’s more, PET imaging results indicated the imaging agent mainly cleared by the kidneys and had no adverse effects in volunteers. The radiochemical yield and safety of experimental groups was obviously better. The results of cell uptake and PET imaging implied that 18F-Phe-BF3 has the potential to be a good imaging agent for tumor diseases such as glioma.

Key words: Phe-BF3, fluorine radio labelling, PET/CT, glioma