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静脉注射后放射性标记的 40 kDa 聚乙二醇在小鼠体内的分布与排泄。

Biodistribution and excretion of radiolabeled 40 kDa polyethylene glycol following intravenous administration in mice.

机构信息

Department of Pharmacology and Toxicology, Enzon Pharmaceuticals, Inc., Piscataway, New Jersey 08854, USA.

出版信息

J Pharm Sci. 2013 Jul;102(7):2362-70. doi: 10.1002/jps.23506. Epub 2013 Apr 23.

Abstract

The pharmacokinetics, excretion, and tissue distribution of [(14)C]-labeled polyethylene glycol-alanine (PEG-Ala) were determined after slow bolus administration into the femoral vein of male CD-1 mice. The pharmacokinetics of PEG-Ala in blood and plasma revealed a biphasic elimination with a terminal half-life of 20 h. Eighty-five percent of the excreted material was voided in the urine and the remaining amount was detected in the feces. PEG-Ala-derived radioactivity was widely distributed with detectable levels of radioactivity observed in all tissues examined. The highest concentration was observed in the kidneys followed by lungs, heart, and liver. Six hours after administration, PEG-Ala levels were significantly reduced in all tissues. Despite a slow prolonged decrease, radioactivity was still detectable after 28 days.

摘要

[(14)C]-标记的聚乙二醇-丙氨酸(PEG-Ala)经缓慢静脉推注到雄性 CD-1 小鼠股静脉后,其药代动力学、排泄和组织分布情况得到了确定。PEG-Ala 在血液和血浆中的药代动力学呈双相消除,末端半衰期为 20 小时。85%的排泄物质在尿液中排出,其余部分在粪便中检测到。PEG-Ala 衍生的放射性物质广泛分布,在所检查的所有组织中均观察到可检测水平的放射性。放射性最高的浓度出现在肾脏,其次是肺、心脏和肝脏。给药 6 小时后,所有组织中的 PEG-Ala 水平均显著降低。尽管放射性缓慢且持续下降,但在 28 天后仍可检测到放射性。

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