^(99m)Tc-CPF制备及实验研究

Labeling and Experimental Studies of Infection Imaging Agent ^(99m)Tc-CPF

目的探讨炎症显像剂99mTc-环丙沙星(99mTc-CPF)在小鼠体内分布的特点,评价其作为新型炎症显像剂的价值。方法制备99mTc-CPF,并测定其放化纯度和标记率。制作小白鼠炎症模型,并经尾静脉注入0.1ml99mTc-CPF,分别于0.5、1、4、6、12h处死小白鼠,取血样和部分器官组织,测量其放射性。结果99mTc-CPE标记率>90%,室温下6h内化合物的放化纯稳定。小白鼠炎症组织与正常组织的放射性比值高,注射后1、4、6、12h,炎症组织与对侧正常组织比值分别为3.48、4.30、4.17、4.16.99mTc-CPF主要由肝脏代谢、经肾脏排泄,血液清除较快。结论99mTc-CPE是一种灵敏度高的炎症灶显像剂,且制备方法简单、方便。

Objective To discuss the biodistfibufion of inflammation tracer：^99mTc- Ciprofloxacin（CPF） in mice, and assessed the efficacy of it in accurately detecting sites of bacterial infection. Methods CPF was labeled with ^99mTc- and the radiechemical purity and labeling rate were measured. Rat model of infection was established, then the preparation of 0.1 ml ^99mTc- CPF was injected intravenously （ tail vein） to the animals within I h of the radiolabelling. 0.5, 1, 4, 6,12h after injection, the blood and tissues samples of organs were taken after the animals were kiUed. Samples were weighed and counted in a γ - counter, the biodistribution of ^99mTc- CPF in mice were measured. Results The labeling rate of ^99mTc- CPF was over 90% ^99mTc- Ciprotech was stable within 6 hours at room temperature. The inflammation tissue/normal tissue were 3.48,4.30,4.17 和4.16 at 1,4,6,12 hour after injection respectively. The radioactivity clearance mainly occurred in the liver and kidney, and the clearance from blood was rapid. Conclusions ^99mTc-CPF is a sensitive radiopharmaceutical for scintigraphy of inflammation lesions, and it is easy to prepare.