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超顺磁性氧化铁磁共振造影剂在大鼠体内的药代动力学

Pharmacokinetics of superparamagnetic iron-oxide MR contrast agents in the rat.

作者信息

Majumdar S, Zoghbi S S, Gore J C

机构信息

Department of Radiology, Yale University, New Haven, Connecticut.

出版信息

Invest Radiol. 1990 Jul;25(7):771-7. doi: 10.1097/00004424-199007000-00004.

DOI:10.1097/00004424-199007000-00004
PMID:2391194
Abstract

The in vivo pharmacokinetics and the biodistribution of superparamagnetic iron-oxide particles (AMI25, Advanced Magnetics, Cambridge, MA) were investigated in anesthetized rats. Four different dose concentrations, ranging from 49.8 to 408.9 mumol of Fe (or 2.78-22.84 mg Fe) per kilogram, radiolabeled with 6.0 microCi of 59Fe-AMI25 were injected intravenously into 18 rats. The radioactivity cleared from the circulation with a fast component with a half-life of approximately 10 minutes and a slower component with a half-life of 92 minutes. Both half-lives were independent of the injected dose (ID) in the range of 105.4-408.9 mumol (5.89-22.84 mg) Fe/kg. The relative uptake in the liver, spleen, and kidneys was 57%, 2.9%, and 2.0% of the ID, respectively. At a dose of 52.1 mumol (2.91 mg) of Fe/kg, the relative concentration of iron significantly increased in the liver and decreased in the blood. Within the kidney, autoradiography showed that the iron was selectively taken up by the cortex. In the kidney, a concentration of 0.23 mumol (0.013 mg) Fe/g resulted in a 30% reduction in image intensity in a single echo magnetic resonance image obtained using a spin-echo sequence and an echo time of 70 ms.

摘要

在麻醉大鼠体内研究了超顺磁性氧化铁颗粒(AMI25,Advanced Magnetics,剑桥,马萨诸塞州)的药代动力学和生物分布。将18只大鼠静脉注射每千克含49.8至408.9 μmol铁(或2.78 - 22.84 mg铁)、用6.0 μCi的59Fe - AMI25进行放射性标记的四种不同剂量浓度的药物。放射性从循环中清除时,快速成分的半衰期约为10分钟,较慢成分的半衰期为92分钟。在105.4 - 408.9 μmol(5.89 - 22.84 mg)铁/千克的注射剂量范围内,这两个半衰期均与注射剂量无关。肝脏、脾脏和肾脏中的相对摄取量分别为注射剂量的57%、2.9%和2.0%。在铁剂量为52.1 μmol(2.91 mg)/千克时,肝脏中铁的相对浓度显著增加,血液中铁的浓度降低。在肾脏内,放射自显影显示铁被皮质选择性摄取。在肾脏中,每克0.23 μmol(0.013 mg)铁的浓度导致使用自旋回波序列和70 ms回波时间获得的单次回波磁共振图像的图像强度降低30%。

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