新型葡萄糖类似物99TcmN-DGDTC的药代动力学和显像研究

摘要

目的 探讨[99TcmN]2+ 间接标记二硫代氨基甲酸脱氧葡萄糖 (deoxyglucose dithiocarbamate,DGDTC) 药代动力学特点以及在荷瘤模型小鼠和兔的显像效果.方法 药代动力学研究:标记后的[99TcmN]-DGDTC化合物经耳缘静脉注射入健康成年新西兰大白兔体内,于特定时间点采血测定放射计数,以专业软件进行药代动力学计算.动物肿瘤模型显像:分别以荷瘤Balb/C小鼠和新西兰大白兔进行.分别移植H22鼠肝癌细胞系和VX2兔肝癌细胞系于10只小鼠和5只兔子皮下,待肿瘤成型后静脉注射99TcmN-DGDTC 复合物行显像观察,并均以99Tcm-高锝酸盐显像作为对照研究.扫描方法:采集血流相、血池相和连续静态图像直至注射后2-4 h(小时).结果 药代动力学结果证明99TcmN-DGDTC 复合物体内分布为二室模型,有效半衰期为34.05 min.显像结果证明99TcmN-DGDTC复合物能充分显示小鼠和兔肿瘤模型的病变所在,注射后2 h肿瘤区/周围组织放射计数比值大于2.结论 药代动力学和显像研究结果充分证实了99TcmN-DGDTC作为新的肿瘤代谢显像剂的可行性.%：Objective 　To evaluate the pharm acokinetic characteristics and feasibility of imaging in tumor-bearing mice and rabbits of [99Tcm N]2 + intermediate radiolabelled deoxyglucose dithiocarbamate (DGDTC) .Methods 　The DGDTC was synthesized and radiolabelled with [99Tcm N ]2 + to form the 99Tcm N-DGDTC complex under the guideline of kit .Pharm acokinetics data of healthy rabbits were acquired by collecting radio counts of auricular vein and processed with software DAS2 .1 .1 .Animal tumor model(10mice with H 22 transplanted cancer and 5 rabits with VX 2 transplanted cancer） imaging was designed to two groups,99 Tcm N-DGDTC group and 99Tcm pertechnetate group(as a control) .Scintigraphy was performed with blood flow,blood pool ，and static acquisition continuously ，till2 - 4 hours after injection .Results 　The pharm acokinetics results were proved to be a two-compartment model,and t1/2 was 34 .05 minutes .Scintigraphic results showed 99Tcm N-DGDTC complex could display tumor well in mice and rabbits tumor model .The count ratio of tumor to nontum orous tissue kept above 2 within 3 hours injected,suggesting the well tumor utilizing of 99TcmN-DGDTC .Conclusion 　The pharm acokinetics results and scintigraphic findings supported the potential use of 99TcmN – DGDTC as a functional imaging agent .