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牛蒡子苷元大鼠皮下注射给药后的血浆动力学及组织分布研究

韩舒 谷元 杨元辉 商庆节 姚景春 刘万卉 司端运

烟台大学学报(自然科学与工程版)2017,Vol.30Issue(2):131-137,7.
烟台大学学报(自然科学与工程版)2017,Vol.30Issue(2):131-137,7.DOI:10.13951/j.cnki.37-1213/n.2017.02.009

牛蒡子苷元大鼠皮下注射给药后的血浆动力学及组织分布研究

Plasma Kinetics and Tissue Distribution of Arctigenin in Ratsafter Subcutaneous Injection

韩舒 1谷元 2杨元辉 2商庆节 2姚景春 3刘万卉 3司端运1

作者信息

  • 1. 烟台大学药学院,山东 烟台 264005
  • 2. 天津药物研究院有限公司 释药技术与药代动力学国家重点实验室,天津 300193
  • 3. 中药制药共性技术国家重点实验室,山东 临沂 276000
  • 折叠

摘要

Abstract

The plasma kinetics and tissue distribution of arctigenin after subcutaneous injection in Wistar rats are investigated.Wistar rats are injected subcutaneously with arctigeninare of 0.1, 0.3 and 1.0 mg/kg, blood and tissue samples are collected at different time points after injection, and concentrations of arctigenin in the samples are determined by liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS).After subcutaneous injection arctigenin 0.1, 0.3 and 1.0 mg/kg, Tmax of the 3 groups is 0.3 h, AUC is 22.8±5.77, 83.5±15.3 and 412±117 h·ng/mL respectively, Cmax is 17.6±4.74, 61.8±8.05 and 285±77.0 ng/mL respectively, t1/2 is 0.781~1.08 h, Vd is 3.84~5.59 L/kg, and the calculated absolute bioavailability is 103%.Arctigenin is quickly and widely distributed in Wistar rats organs, and mainly distributes in intestine, heart, liver, pancreas and kidney without apparent accumulating effect.Arctigenin is absorbed and eliminated quickly in Wistar rats after subcutaneous injection, the distribution is wide, and Cmax and AUC0-t are in a linear proportion to arctigenin dose.It is concluded that subcutaneous injection can effectively improve the level of systemic and tissular exposure in rats, and shows good kinetics.

关键词

牛蒡子苷元/皮下注射/血浆动力学/组织分布/液相色谱串联质谱联用

Key words

arctigenin/subcutaneous injection/plasma kinetics/tissue distribution/liquid chromatograhph-mass spectrometry/mass spectrometry(LC-MS/MS)

分类

医药卫生

引用本文复制引用

韩舒,谷元,杨元辉,商庆节,姚景春,刘万卉,司端运..牛蒡子苷元大鼠皮下注射给药后的血浆动力学及组织分布研究[J].烟台大学学报(自然科学与工程版),2017,30(2):131-137,7.

基金项目

国家自然科学基金资助项目(81503154) (81503154)

山东省自主创新及成果转化专项计划项目(2015ZDJQ05004). (2015ZDJQ05004)

烟台大学学报(自然科学与工程版)

1004-8820

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