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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]+ 有望
OBJECTIVE To compare the pharmacological pharmacology of myocardial 99Tcm MIBI ([99Tcm (CO) 3 (MIBI) 3] +) and 99Tcm MIBI. Method Preparation of [99Tcm (CO) 3 (MIBI) 3] + injection, 85% pure radiochemistry. Three dogs were treated with intravenous injection of 5 55 MBq. Pharmacokinetic parameters, in vivo biodistribution, target non-target ratio and pharmacodynamic results were obtained by dynamic acquisition, whole body imaging and blood sampling. Results The [99Tcm (CO) 3 (MIBI) 3] + was consistent with a two-compartment pharmacokinetic model for intravenous administration. The half-life of the phase clearance T 1 was 1.33 ± 0.12 min, The half-life T (β) 1 2 = (102.33 ± 2.58.5) min, total clearance rate (CL) = (40 1.33 ± 73.5 1) mL h. The time curve of heart, liver and lung showed that the amplitude of hepatic uptake of [99Tcm (CO) 3 (MIBI) 3] + was lower than that of myocardium, while the curve of 99Tcm MIBI was significantly higher than that of myocardium. Compared with the 99Tcm MIBI, the myocardial infarction rate of 10,30,6 0,90 and 12 0min [99Tcm (CO) 3 (MIBI) 3] + in heart, lung and liver were higher Lower, low liver uptake. [99Tcm (CO) 3 (MIBI) 3] + heart-lung and heart-liver ratio were higher than 99Tcm MIBI, the difference was significant (P <0.01). Intravenous injection of [99Tcm (CO) 3 (MIBI) 3] + 10 ~ 120min after can obtain a clear myocardial images, rapid excretion of liver and gallbladder, low intrahepatic radioactivity, left ventricular wall is not affected by liver, without lipid Meal to promote liver and gallbladder excretion. Conclusion [99Tcm (CO) 3 (MIBI) 3] + is expected