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作为纳米颗粒给药的BCS II类药物的肠道吸收:基于肠道灌注模型数据的综述

Intestinal absorption of BCS class II drugs administered as nanoparticles: A review based on data from intestinal perfusion models.

作者信息

Dahlgren David, Sjögren Erik, Lennernäs Hans

机构信息

Department of Pharmaceutical Biosciences, Translational Drug Discovery and Development, Uppsala University, Sweden.

出版信息

ADMET DMPK. 2020 Sep 17;8(4):375-390. doi: 10.5599/admet.881. eCollection 2020.

Abstract

An established pharmaceutical strategy to increase oral drug absorption of low solubility-high permeability drugs is to create nanoparticles of them. Reducing the size of the solid-state particles increases their dissolution and transport rate across the mucus barrier and the aqueous boundary layer. Suspensions of nanoparticles also sometimes behave differently than those of larger particles in the fed state. This review compares the absorption mechanisms of nano- and larger particles in the lumen at different prandial states, with an emphasis on data derived from in vivo models. Four BSC class II drugs-aprepitant, cyclosporine, danazol and fenofibrate-are discussed in detail based on information from preclinical intestinal perfusion models.

摘要

一种已确立的提高低溶解度-高渗透性药物口服吸收的制药策略是制备它们的纳米颗粒。减小固态颗粒的尺寸可提高其溶解速率以及跨黏液屏障和水相边界层的转运速率。纳米颗粒混悬液在进食状态下的行为有时也与较大颗粒的混悬液不同。本综述比较了不同用餐状态下纳米颗粒和较大颗粒在肠腔中的吸收机制,重点是来自体内模型的数据。基于临床前肠道灌注模型的信息,详细讨论了四种生物药剂分类系统(BSC)II类药物——阿瑞匹坦、环孢素、达那唑和非诺贝特。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a1e9/8915587/1b8663a2c9d2/admet-8-881-g001.jpg

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