新型心肌灌注显像剂~(99)Tc~m-CO-MIBI与~(99)Tc~m-MIBI的药理学比较
Pharmacological Study of ~(99)Tc~m-CO-MIBI,a New Myocardial Perfusion Imaging Agent Comparison to ~(99)Tc~m-MIBI
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摘要: 以犬为实验动物,99Tcm-CO-MIBI和99Tcm-MIBI为显像剂,采用自身对照的方法,通过采集血样、采集动态图像和全身显像获得药物在犬体内的代谢动力学参数、生物分布、靶与非靶放射性摄取比和全身、心脏平面及断层影像等药效学结果。结果显示,99Tcm-CO-MIBI符合一次静脉给药的血药动力学二室开放模型,快相及慢相半衰期分别为Tα(1/2)=1.46±0.13 min,Tβ(1/2)=97.30±20.50 min,全血总清除率CL=436.36±54.77 mL/h。心、肺、肝时间-放射性曲线显示,在注射约40 min后,99Tcm-CO-MIBI肝脏曲线明显低于心肌曲线。多时间点心脏与肺脏及肝脏的放射性摄取比亦表明99Tcm-CO-MIBI在心肌摄取高,滞留久,肺本底低,肝脏药物排出比99Tcm-MIBI明显快。注射99Tcm-CO-MIBI后10~120 min内均可获得清晰的心肌图像,40 min后下壁心肌显示不再受肝内放射性干扰。表明99Tcm-CO-MIBI犬体内生物分布优异,有望成为一种新型心肌灌注显像剂。Abstract: Pharmacological experiment of ~(99)Tc~m-MIBI and ~(99)Tc~m-CO-MIBI are performed by self-contrast in dogs.The data of pharmacokinetics parameters,biodistribution,T/NT are collected and calculated during and after photograph.Moreover,the whole body image,heart plane scintigraphy and tomography are investigated.Blood-pool clearance of ~(99)Tc~m-CO-MIBI conforms to two-compartment with 436.36±54.77 mL/h of blood clearance(CL) and T_(α(1/2))=1.46±0.13 min for the fast early clearance,T_(β(1/2))=97.30±20.50 min for the slow late clearance,which faster than that of ~(99)Tc~m-MIBI.The time-radioactivity curves show that the hepatic uptake curves are below the heart curves at about 40 min after ~(99)Tc~m-CO-MIBI injecting.The heart-lung and heart-liver ratios,which are measured at several time points,also demonstrate that ~(99)Tc~m-CO-MIBI have higher uptake and longer retain in myocardium,lower lung radioactivity and faster excrete from liver compare to ~(99)Tc~m-MIBI.During 10-120 min after ~(99)Tc~m-CO-MIBI injected,the excellent plane and SPECT can be obtained,perfect myocardial image without liver activity disturbance are gained after 40 min injecting.It suggests that ~(99)Tc~m-CO-MIBI have better pharmacokinetics properties and offer a great possibility as a new myocardial perfusion image agent.