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目的 研究正电子断层显像剂 2 18F 2 脱氧 D 葡萄糖 (18F FDG)的合成改进及其小鼠体内药动学。方法 采用回旋加速器通过核反应18O(p ,n) 18F生产18F-,18F-在相转移催化剂Kryptofix 2 2 2存在下与前体 1,3,4,6 四乙酰基 2 三氟磺酰甲基 β D(+)甘露糖发生亲核取代反应 ,经水解、中和、纯化得18F FDG注射液。建立其质量控制方法 ,并测定其药动学参数和体内生物分布。结果 经时间衰减校正后 ,18F FDG放射化学产率约为 72 % ,总合成时间为 5 0min ,各项质量控制指标符合美国药典要求。18F FDG的药动学符合三室模型 ,分布相半衰期分别为t1/ 2π(0 .4min)和t1/ 2α(4 .8min) ,消除相半衰期为t1/ 2 β(85 .4min)。18F FDG在小鼠心肌和脑中有较高的摄取率及较高的心 非靶器官和脑 非靶器官比 ,且放射性持续时间较长 ,并通过肾脏迅速排出 ;注入18F FDG 45min后 ,放射性在血和各脏器中的分布逐渐达到平衡。正常人体内分布实验结果与肺癌患者相类似 ,但肺癌患者体内有很高的肿瘤 正常组织的放射性比值。结论 制备的18F FDG适于PET研究和临床诊断
Objective To study the synthesis and improvement of 2 18F 2 deoxy D glucose (18F FDG) in positron emission tomography (PET) and its pharmacokinetics in mice. METHODS 18F- was produced by a cyclotron 18O (p, n) 18F using a cyclotron. 18F- was reacted with precursor 1,3,4,6 tetraacetyl 2 trifluoromethanesulfonylmethyl β D (+) mannose nucleophilic substitution reaction, after hydrolysis, neutralization, purified 18F FDG injection. Establish its quality control method, and determine its pharmacokinetic parameters and in vivo biodistribution. Results After the time attenuation correction, the 18F FDG radiochemical yield was about 72% and the total synthesis time was 50 min. The quality control indexes of the 18F FDG met the requirements of the US Pharmacopoeia. The pharmacokinetics of 18F FDG conformed to the three-compartment model. The half-life of the phase was t1 / 2π (0.4min) and t1 / 2α (4.8min), and the elimination half-life was t1 / 2β (85.4min). 18F FDG had higher uptake rate and higher non-target organ and brain non-target organ ratio in mouse myocardium and brain, and the radioactive duration was longer and rapidly excreted through the kidney. After 18F FDG injection for 45min, the radioactivity Distribution in the blood and various organs gradually balance. Normal human body distribution of experimental results and lung cancer patients are similar, but there is a high lung cancer patients with high tumor normal tissue radioactivity ratio. Conclusion 18F FDG prepared for PET study and clinical diagnosis