Bourrinet P, Dencausse A, Cochet P, Bromet-Petit M, Chambon C
Laboratoire Guerbet, Aulnay Sous Bois, France.
Invest Radiol. 1994 Dec;29(12):1057-60. doi: 10.1097/00004424-199412000-00008.
Iobitridol is a new nonionic low-osmolality contrast medium. During preclinical development of this agent, it was of interest to verify that it behaves like other urographic and angiographic contrast agents (i.e., as a tracer of extracellular fluid).
Male and female rats were imaged using a quantitative autoradiographic method after intravenous administration of iodine-125-labeled product at a dose of 300 mg iodine/kg.
The radioactivity was rapidly distributed with substantial uptake in the thyroid, kidneys, and skin after 10 minutes. The central nervous system showed no uptake. The radioactivity was rapidly eliminated (i.e., after 24 and 48 hours, only traces were found) except in the thyroid (because of free radiolabeled iodides present in small quantities in the administered solution). The considerable renal uptake after administration can be attributed to urinary excretion of the radioactivity (86% of the administered dose after 24 hours). Total elimination was achieved after 48 hours. No sex-related effects were observed.
The absence of a target organ, the abundant and rapid urinary elimination, and the absence of transfer across the blood-brain barrier suggest that iobitridol is a tracer of extracellular fluid.
碘比醇是一种新型非离子低渗性造影剂。在该制剂的临床前研发过程中,有必要验证其是否与其他尿路造影和血管造影造影剂的行为相似(即作为细胞外液的示踪剂)。
给雄性和雌性大鼠静脉注射剂量为300mg碘/千克的碘-125标记产物后,采用定量放射自显影法进行成像。
给药10分钟后,放射性迅速分布,甲状腺、肾脏和皮肤有大量摄取。中枢神经系统无摄取。除甲状腺外(由于给药溶液中存在少量游离放射性碘化物),放射性迅速消除(即24小时和48小时后仅发现微量)。给药后肾脏摄取量可观,这可归因于放射性物质经尿液排泄(24小时后为给药剂量的86%)。48小时后实现完全消除。未观察到性别相关影响。
缺乏靶器官、大量且快速经尿液消除以及不存在血脑屏障转运表明碘比醇是细胞外液的示踪剂。