Intestinal Absorption Investigation of Scutellarin Ethyl Ester by  Single Pass Intestinal Perfusion Model

XU Xue-lin; YI Hong; ZHAO Jie; XIE Xiao-ke; WANG Zhi-min; ZHANG Qi-wei; LIU Xiao-qian; GAO Hui-min

doi:10.13422/j.cnki.syfjx.2015110011

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Intestinal Absorption Investigation of Scutellarin Ethyl Ester by Single Pass Intestinal Perfusion Model

更新时间：2024-01-04

- Intestinal Absorption Investigation of Scutellarin Ethyl Ester by Single Pass Intestinal Perfusion Model
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 21, Issue 11, Pages: 11-15(2015)
- 作者机构：
- 作者简介：
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- DOI：10.13422/j.cnki.syfjx.2015110011
  CLC： R285.5
- Published：2015
- 稿件说明：
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XU Xue-lin, YI Hong, ZHAO Jie, et al. Intestinal Absorption Investigation of Scutellarin Ethyl Ester by Single Pass Intestinal Perfusion Model[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(11): 11-15.
DOI：

XU Xue-lin, YI Hong, ZHAO Jie, et al. Intestinal Absorption Investigation of Scutellarin Ethyl Ester by Single Pass Intestinal Perfusion Model[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(11): 11-15. DOI： 10.13422/j.cnki.syfjx.2015110011.

摘要

目的: 分析灯盏乙素乙酯(scutellarin ethyl ester

DZY-02)在大鼠小肠各肠段的吸收机制. 方法: 采用大鼠在体单向肠灌流模型

运用HPLC测定肠灌流液中DZY-02含量

考察3个剂量组DZY-02在大鼠十二指肠、空肠、回肠的吸收情况

分析P-糖蛋白(P-glycoprotein

P-gp)和乳腺癌耐药蛋白(breast cancer resistance protein

BCRP)抑制剂对DZY-02吸收的影响. 结果: DZY-02在低、中、高质量浓度下

各小肠段的吸收速率常数和有效渗透系数(Peff)均无显著性差异

Peff均>0.2×10-4 cm·s-1.在相同质量浓度下

DZY-02在不同肠段的吸收速率常数均无显著性差异;P-gp和BCRP抑制剂均对DZY-02吸收无影响. 结论: DZY-02在大鼠肠道内为高渗透性药物

在小肠内均有吸收

且无特定的吸收窗.在一定质量浓度范围内

DZY-02在大鼠肠道内吸收无高浓度饱和抑制现象

推断DZY-02在大鼠肠道内的吸收机制可能为被动扩散.DZY-02不是P-gp和BCRP蛋白的底物.

Abstract

Objective: To investigate absorption mechanism of scutellarin ethyl ester (DZY-02). Method: In situ single pass intestinal perfusion model was established

HPLC was adopted to study absorptions of three dose groups of DZY-02 in different segments

effects of different protein inhibitors on absorption parameters of DZY-02 in different intestinal segments were investigated. Result: Absorption rate constant and effective permeability coefficient (Peff) were no significantly differences in different segments of rat intestine or concentration of DZY-02

Peff was more than 0.2×10-4 cm·s-1.Protein inhibitors had no obvious effects on intestinal absorption of DZY-02. Conclusion: DZY-02 is a high-permeability candidate drug and can be absorbed in whole intestinal segments

transport mechanism of DZY-02 in vivo is similar to passive diffusion.DZY-02 may be not a substrate of P-glycoprotein and breast cancer resistance protein.

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