氟-18-左旋氧氟沙星的标记与动物实验研究

Labeling and animal study of fluorine-18-Levofloxacin

炎症显像是核素影像诊断的重要研究领域,但其中正电子核素标记的药物报道不多。为探索合成一种可特异性在炎症部位浓集、且可鉴别是否为细菌性感染的正电子核素标记的显像剂,我们研究制备了F标记18的Levofloxacin(LVFX)用于炎症显像。标记方法采用经典的Hamacher法(氟离子亲核取代)标记LVFX,放射化学纯大于98%,放射性得率约40%,热原检测为阴性。结果表明标记方法简单迅速,标记物稳定。研究了F-LVFX在正常炎症动物模型内的生物分布以及炎症动物模型的显像。生物分布和显像结果均表明1818F-LVFX在炎症组织内有较高的摄取,炎症组织与正常组织间有显著性差异(P<0.05),该标记物主要通过肾脏和肝脏排泄。研究表明F-LVFX是一种潜在的炎症显像剂。

Infection imaging is an important field in radionuclide imaging. But there are few reports about positron radionuclide labeled agents. To investigate a kind of specific infection imaging agent which can differentiate bacteria caused infection, we have radiosynthesized fluorine-18 labeled Levofloxacin （LVFX） for infection imaging. A typical Hamacher method was used to label LVFX. Radiochemistry purity was more than 98%, yield rate was about 40% and the pyretogen test result was negative. The labeling result showed that the labeling method was easy, procedure was simple and labeled agent was stable. The biodistribution and imaging of ISF-LVFX in animal model was also studied. Both biodistribution and imaging result showed higher uptake of 18^F-LVFX in infected tissues. The accumulation of labeled agent in infected and normal tissue showed significant difference （P〈0.05）. This labeled agent was mainly excreted through kidney and liver. It is suggested that fluorine-18 labeled LVFX is a potential infection imaging agent.