【摘要】 目的:研究c-erbB2反义寡脱氧核苷酸(ASODN)探针99mTc-ASODN-EGF的体内分布和药动学特性。方法:小鼠尾静脉注射99mTc-ASODN-EGF 370 kBq(10μC i).150μL-1,于0.5,1,2,4,8,24 h取血、肝、脾、肾等组织器官,测定每分钟放射性计数(cpm),并准确称重,计算每克组织百分注射剂量率(%ID.g-1)。兔经左侧耳缘静脉注射99mTc-ASODN-EGF 1110 kBq(30μC i).2 mL-1,于1,3,5,10,15,20,25,30,40,60,120,240,360 m in从右侧耳缘静脉采血约0.2 mL,测定cpm,准确称重,计算每克血液每分钟放射性计数,用3P97软件计算药动学参数。结果:99mTc-ASODN-EGF在小鼠肝、肾、脾和肺的放射性分布较高,1 h的%ID.g-1分别为22±8,7.4±2.0,46±28和13±7。在心、脑、骨和肌肉的放射性分布很低。兔药动学参数符合二室模型,t12α为(0.32±0.07)h,t12β为(9±3)h,Vc为(1.2±0.8)cpm.kg-1,Cl为(0.061±0.023)cpm.h-1。结论:99mTc-ASODN-EGF的组织器官分布和药动学特性能满足临床显像的要求,可用于肿瘤靶基因的显像。更多还原

【Abstract】 AIM: To study the tissue distribution in mice and pharmacokinetics characteristics in rabbits for c-erbB2 antisense oligodeoxynucleotides（ASODN） probe（）^99mTc-ASODN-EGF. METHODS: BALB/c mice were injected（）^99mTc-ASODN-EGF（370 kBq）（10μCi）·150 μL^-1 via the caudal vein.They were sacrificed at 0.5,1,2,4,8,24 h taking sample of blood,liver,spleen,kidney etc and measuring the γ radio activitycounts per minut（cpm） with accurate weight and definite percentage of injected dosage of per gram tissue(%ID·g^-1).Rabbits were injected(（）^99mTc-ASODN-EGF) 1110 kBq（30 μCi）·2 mL^-1 per rabbit via left-marginal ear vein taking blood sample 0.2 mL and measuring cpm and exact weight from right-marginal ear vein at 1,3,5,10,15,20,25,30,40,60,120,240,360 min,simultaneously recording the γ radio activity-counts per minute,per gram blood.Pharmacokinetics parameters were calculated from the plasma drug concentration-time data with the 3P97 software package.RESULTS:（）^99mTc-ASODN-EGF was densely distributed in liver,kidney,spleen and lung in which %ID·g^-1 were 22±8,7.4±2.0,46±28 and 13±7 at 1 h,respectively,in mice. （）^99mTc-ASODN-EGF was less densely distributed in heart,brain and muscle.Pharmacokinetics parameters had showed that the metabolism and clearance of（）^99mTc-ASODN-EGF were accorded with two-compartment model with t_<sub>12α as（（0.32±0.07） h,） t_<sub>12β（9±3） h,Vc（1.2±0.8） cpm·kg^-1,and Cl(0.061±（0.023） cpm·h^-1).CONCLUSION: The tissue distributions and pharmacokinetics characteristics of（）^99mTc-ASODN-EGF could fulfil the basic requirement of clinical imaging for opacification of tumor target gene.更多还原