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大鼠静脉注射或口服[125I] - 寡核苷酸后的药代动力学、吸收、分布及处置情况。

Pharmacokinetics, absorption, distribution and disposition of [125I]-oligotide following intravenous or oral administration in the rat.

作者信息

Fisher J, Holland T K, Pescador R, Porta R, Ferro L

机构信息

Inveresk Research International, Tranent, Scotland.

出版信息

Thromb Res. 1997 Mar 15;85(6):445-53. doi: 10.1016/s0049-3848(97)00034-0.

Abstract

Oligotide (O) was labelled with 125I. The radiolabelled compound ([125I]-Oligotide ([125I]-O)) retained the biological activity of parent O. Following single intravenous administration the half lives of radioactivity associated with O and/or O related components in plasma were 9-10 min and 9-10 h for alpha and beta phases respectively. Following single oral administration the half life of radioactivity associated with O and/or O related components in plasma was 11.45-12.76 h for beta fase. Following multiple oral administration once daily for 7 days, the half life of radioactivity associated with O and/or O related components following the 7th dose was 10-12 h for beta phase. The areas under plasma total radioactivity versus time curves were dose-dependent. Following single intravenous administration the major proportion of the administered dose was excreted via urine, while following single oral administration excretion via urine and faeces accounted for similar proportions of the administered dose. Following both single and oral administration the levels of radioactive components derived from [125I]-O in organs examined were generally highest in highly perfused organs.

摘要

寡核苷酸(O)用125I进行标记。放射性标记化合物([125I]-寡核苷酸([125I]-O))保留了母体O的生物活性。单次静脉注射后,血浆中与O和/或O相关成分相关的放射性半衰期,α相和β相分别为9 - 10分钟和9 - 10小时。单次口服给药后,血浆中与O和/或O相关成分相关的放射性半衰期,β相为11.45 - 12.76小时。每日一次多次口服给药7天,第7剂后血浆中与O和/或O相关成分相关的放射性半衰期,β相为10 - 12小时。血浆总放射性与时间曲线下的面积呈剂量依赖性。单次静脉注射后,给药剂量的主要部分经尿液排泄,而单次口服给药后,经尿液和粪便排泄的剂量占给药剂量的比例相似。单次和口服给药后,在检查的器官中,源自[125I]-O的放射性成分水平通常在高灌注器官中最高。

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