论文部分内容阅读
为了解脂肪酸代谢显像剂125I-对碘苯代十五烷酸(IPPA)在动物体内的分布、清除等行为,进行了125I-IPPA动物实验。结果表明,大鼠心肌对125I-IPPA的摄取高而快,最大心肌摄取值为4.4ID%/g,半清除时间T1/2α-3.8min;甲状腺摄取低,至120min,甲状腺摄取值仅为0.005ID%/organ.免血药清除T1/2α=2.7min.125I-IPPA与小鼠体内血浆蛋白结合高而快,体外血浆蛋白给会稳定;异常毒性试验合格,小鼠的耐受量是人的560倍。大鼠体内各主要脏器的摄取和清除、免血药清除、小鼠体内血浆蛋白结合等均呈现第二计数峰。提示125I-IPPA能被大鼠心肌迅速摄取并参与心肌代谢,其代谢产物进入血液,最终由肾脏排泄,几乎没有游离碘的释放,从而降低本底,提高显像的质量。
In order to understand the distribution and clearance of fatty acid metabolite 125I-p-iodobenzenepentadecanoic acid (IPPA) in animals, 125I-IPPA animal experiments were performed. The results showed that the uptake of 125I-IPPA in rat myocardium was high and fast, the maximum myocardial uptake value was 4.4ID% / g and the half clearing time was from T1 / 2α-3.8min. The thyroid uptake was low until 120min, and the thyroid uptake value 0.005ID% / organ. Blood-free drug clearance T1 / 2α = 2.7min. 125I-IPPA and plasma protein in mice with high and fast, in vitro plasma protein will be stable; abnormal toxicity test pass, the mouse tolerance is 560 times the human. In vivo absorption and clearance of major organs in rats, blood-free drug clearance, plasma protein binding in mice showed a second count peak. Tip 125I-IPPA can be rapidly uptake by the rat myocardium and involved in myocardial metabolism, the metabolites into the blood, and ultimately excreted by the kidneys, almost free release of free iodine, thereby reducing the background and improve the quality of imaging.