骨骼显像剂^(18)F-NaF的制备及生物分布研究  

Preparation and Biodistribution of [Fluorine-18] Sodium Fluoride

作　　者：范文博[1] Fan Wenbo(Department of Nuclear Medicine&PET centre,The First Affiliated Hospital of Xiamen University,Xiamen 361003,China)

机构地区：[1]厦门大学附属第一医院核医学科PET中心,福建厦门361003

出　　处：《山东化工》2022年第22期55-57,61,共4页Shandong Chemical Industry

摘　　要：研究^(18)F-NaF注射液的制备方法及其动物体内生物分布,利用^([18])O(p,n)18F核反应,经直接处理法制备18-NaF注射液,测定其在小鼠体内的生物分布。用30μA的质子束流连续轰击^([18])O-H_(2)O 50 min后,^(18)F-NaF的平均产额(EOS)为800 GBq;^(18)F-NaF注射液的放射性浓度均大于74.0 GBq/mL,产物经TLC测定,放射化学纯度大于90%。小鼠生物分布实验显示注射后骨骼对^(18)F-NaF的摄取率最高,平均为84.1%;注射10 min后,骨骼/血液、骨骼/肌肉比值大于10;注射后90 min,骨骼与肌肉的比值最高,与60 min和120 min的比值相比有显著性差异(均为P<0.05)。注射后10 min,约有19.8%的^(18)F-NaF经肾脏排泄到膀胱中,60 min后经肾脏排泄的^(18)F-NaF平均为2.2%;其他器官放射性均相对较低。直接处理法是简单有效的制备方法,制备^(18)FNaF注射液生物性能稳定、安全。^(18)F-NaF的骨骼/肌肉比值高,是理想的骨血流和代谢显像剂。在注射^(18)F-NaF后90 min进行PET骨显像可获得清晰的图像。To study the synthetic methods,quality control and biodistribution of[fluorine-18]sodium fluoride(^(18)F-NaF).^(18)F-NaF was produced by the^([18])O(p,n)18F reaction from target irradiated with 800 GBq proton at 30μA for 50 min and using the direct method.Over 90%of radiochemical purity was determined by TLC.The biodistribution of fluorine-18-fluoride in mice indicated that the mean uptake in bone was as high as 84.1%.After injection 10~120 min,the uptakes of motility bone was slightly high than non-motility bone,but both had no significant difference.After injection,the high bone-to-blood and bone-to-muscles ratios were found.The bone-to-blood ratios was above 10.0 after 10 min,and bone-to-muscles ratios was above 10.0 after 30 min.The bone-to-muscles ratios reached the peak at 90 min,and the ratio had significant difference as compared with 60 min and 120 min after injection(P<0.05).About 19.8%of ^(18)F-NaF were excreted via kidney from blood into urinary bladder at 10min,and the excreted ^(18)F-NaF were 2.2%after 60 min.The radioactivity in orther organ was lower and stable level,and were almost approaching blood level after 60 min.The results suggust that the direct method is a simple and rapid means for the preparation of ^(18)F-NaF injection.The skeletal PET imaging with ^(18)F-NaF had low background and interferes.^(18)F-NaF was an excellent bone imaging agent and suitable for clinical skeletal blood flow and bone metabolism measurement.PET imaging with ^(18)F-NaF is better at 90 min after injection.

关 键 词：^(18)F-NaF注射液 正电子药物 生物分布 

分 类 号：TQ460[化学工程—制药化工] R817.4[医药卫生—影像医学与核医学]