18F-NaF注射液的制备及新西兰兔骨折显像

由外伤或肿瘤骨转移造成的隐匿性骨折和愈合情况的准确诊断对制定合适的治疗方案具有非常重要的意义。为考查¹⁸F-NaF PET显像用于骨折诊断的诊断效能,本研究制备了¹⁸F-NaF注射液,并对其进行了质量控制和稳定性研究,然后建立新西兰兔骨折动物模型,模型建立约2周后进行了¹⁸F-NaF PET显像和⁹⁹Tc^m-亚甲基二磷酸盐（⁹⁹Tc^m-MDP）SPECT显像的自身对照实验,并对显像效果进行了比较。结果表明：¹⁸F-NaF的产量大于37 GBq,各项检验结果均符合质控要求,40 ℃下放置8 h和30 ℃下放置10 h所有检验结果均无明显变化;¹⁸F-NaF PET和⁹⁹Tc^m-MDP SPECT两种显像方式均可见全身骨骼,骨折部位呈明显放射性浓聚,但¹⁸F-NaF给药后30 min即可进行PET显像,骨折部位显示更为清晰,骨折部位与对侧正常骨骼的放射性摄取比（T/NT）明显高于⁹⁹Tc^m-MDP,而⁹⁹Tc^m-MDP需在给药后2 h才能进行SPECT显像。本研究表明¹⁸F-NaF PET对骨折的显像性能优于⁹⁹Tc^m-MDP,可明显提高检查流通量和诊断效能。     

99Tcm标记糖肽及其在荷瘤小鼠体内的分布与代谢动力学

Glucose and galactose are conjugated to the N- mercaptoacetyl-Val-Gly-Gly (MAVGG). The glycopeptides and MAVGG are labeled with 99Tcm. The partition coefficients between octanol and water (Pow) are measured. Glycopeptides or MAVGG labeled with 99Tcm areinjected into the mice bearing S180 tumor. 10μL blood samples are withdrawn at different time points and the radioactivities are counted to calculate the effective halflife (T1/2) using a bi-exponential fit. Biodistribution is measured at 3 h postinjection and the percentage of injected dose per gram ( ID%/g ) and tumor to normal tissue ratio (T/NT) were calculated. The assigned structures were confirmed on the basis of IR, NMR and MS. The 99Tcm labeling yield 巨radiochemical purity is greater than 90%. The lgPow of 99Tcm-Glu-MAVGG, 99Tcm-Gal-MAVGG and 99Tcm-MAVGG are –1.974, –2.128 and –1.378, respectively. The T1/2αof the three labeled peptides are 24.3, 37.1, 46.3 min and T1/2β are 221.5, 158.4 and 198.4 min, respectively. The tumor uptakes at 3 h postinjection are 1.46, 1.55 and 0.67 for 99Tcm-Glu-MAVGG, 99Tcm-Gal-MAVGG and 99Tcm-MAVGG, respectively. Their T/NT for tumor over muscle are 3.74、7.38 and 3.53, respectively. The results demonstrated that after carbohydrate conjugate of peptides, the lipophilicity is decreased , the blood clearance is increased and the tumor uptake is enhanced. Of the two glucopeptides, 99Tcm-Gal-MAVGG shows faster blood clearance, higher tumor uptake and T/NT, which suggests the potential utility of 99Tcm-Gal-MAVGG as a suitable tumor imaging agent.