心肌显像剂[^(99)Tc^m(CO)_3(MIBI)_3]^+和^(99)Tc^m-MIBI药理实验对比研究  

Comparative study of pharmacology of a new myocardial imaging agent [^(99)Tc^m(CO)_3(MIBI)_3]^+ and ^(99)Tc^m-MIBI

作　　者：王金城[1] 刘伯里[2] 米宏志[1] 蒋燕[2] 唐志刚[2] 归海旻[1] 

机构地区：[1]首都医科大学附属北京安贞医院核医学科,100029 [2]北京师范大学化学系

出　　处：《中华核医学杂志》2002年第4期231-232,I002,共3页Chinese Journal of Nuclear Medicine

基　　金：国家自然科学基金资助项目 (2 9731 0 2 0 )

摘　　要：目的　对心肌显像剂羰基99Tcm 甲氧基异丁基异腈 (MIBI) ([99Tcm(CO) 3(MIBI) 3]+ )和99Tcm MIBI进行动物药理对比研究。方法　制备 [99Tcm(CO) 3(MIBI) 3]+ 注射液 ,放化纯 85 %。实验犬 3只 ,每次静脉注射剂量 5 5 5MBq ,通过动态采集、全身显像和采集血样 ,获得药代动力学参数、体内生物分布、靶 非靶比值和药效学结果。结果　 [99Tcm(CO) 3(MIBI) 3]+ 符合一次静脉给药的药代动力学二室模型 ,快相清除半衰期T(α) 1 2 =(1.33± 0 .12 )min,慢相清除半衰期T(β) 1 2 =(10 2 .33± 2 5 .5 8)min,总清除速率 (CL) =(40 1.33± 73.5 1)mL h。心、肝、肺时间 放射性曲线显示 [99Tcm(CO) 3(MIBI) 3]+ 肝摄取曲线幅度低于心肌曲线 ,而99Tcm MIBI肝曲线明显高于心肌曲线。 10、30、6 0、90和 12 0min[99Tcm (CO) 3(MIBI) 3]+ 在心、肺、肝百分注射剂量 (%ID)与99Tcm MIBI比较 ,前者心肌摄取较高 ,肺本底较低 ,肝摄取低。 [99Tcm(CO) 3(MIBI) 3]+ 心 肺和心 肝比值均高于99Tcm MIBI,差异有显著性 ,P均 <0 0 1。静脉注射 [99Tcm(CO) 3(MIBI) 3]+ 后 10～ 12 0min均可获得清晰的心肌图像 ,肝胆排泄较快 ,肝内放射性较低 ,左室下壁不受肝影影响 ,无需脂餐促进肝胆排泄。结论　 [99Tcm(CO) 3(MIBI) 3]+Objective To study the biological properties of a new myocardial perfusion imaging agent [ 99 Tc m(CO) 3(MIBI) 3] + in animal and to compare it with 99 Tc m methoxyisobutylisonitrile (MIBI). Methods Solution of [ 99 Tc m(CO) 3(MIBI) 3] + for intravenous injection was prepared. The radiochemical purity was 85% and labelling percentage was over 90%. Three dogs were involved, the dose of [ 99 Tc m(CO) 3(MIBI) 3] + for each dog was 555 MBq at each time of experiment. The pharmacokinetics, biodistribution, ratio of T/NT and myocardial imaging were investigated. Results The pharmacokinetics of [ 99 Tc m(CO) 3(MIBI) 3] + conformed to two compartment model, T(α) 1/2 =(1.33±0.12) min, T(β) 1/2 =(102.33±25.58) min, CL=(401.33±73.51) mL/h. The time radioactivity curves showed that the liver uptake curves of [ 99 Tc m(CO) 3(MIBI) 3] + were below the myocardial curves, while that of 99 Tc m MIBI were above the myocardial curves. The myocardial uptake %ID at 10, 30, 60, 90 and 120 min, and heart to lung and heart to liver activity ratio of the new agent were higher compared with 99 Tc m MIBI. The planar and SPECT images of [ 99 Tc m(CO) 3(MIBI) 3] + during 10 to 120 min showed with good quality with lower lung and liver radioactivities. Conclusion The results of this study show that the [ 99 Tc m(CO) 3(MIBI) 3] + is better than 99 Tc m MIBI in myocardial imaging and warrant further investigation as a potential myocardial perfusion imaging agent.

关 键 词：心肌显像剂 [(CO)3(MIBI)3]^+ MIBI 药理学 药代动力学 实验研究 

分 类 号：R817[医药卫生—影像医学与核医学]