以纳米颗粒形式给药的BCS II类药物的肠道吸收:基于肠道灌注模型体内数据的综述

IF 3.4 Q2 CHEMISTRY, MEDICINAL ADMET and DMPK Pub Date : 2020-09-17 DOI:10.5599/admet.881
D. Dahlgren, E. Sjögren, H. Lennernäs
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引用次数: 8

摘要

提高低溶解度-高渗透性药物口服吸收的既定药物策略是制造纳米颗粒。减小固体颗粒的尺寸增加了它们通过黏液屏障和水边界层的溶解和运输速率。纳米颗粒的悬浮液有时也会表现得与那些在喂食状态下的大颗粒不同。这篇综述比较了纳米颗粒和大颗粒在不同膳食状态下在腔内的吸收机制,重点是来自体内模型的数据。根据临床前肠道灌注模型的信息,详细讨论了四种BSC II类药物-阿瑞吡坦,环孢素,那那唑和非诺贝特。
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Intestinal absorption of BCS class II drugs administered as nanoparticles: A review based on in vivo data from intestinal perfusion models
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.
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来源期刊
ADMET and DMPK
ADMET and DMPK Multiple-
CiteScore
4.40
自引率
0.00%
发文量
22
审稿时长
4 weeks
期刊介绍: ADMET and DMPK is an open access journal devoted to the rapid dissemination of new and original scientific results in all areas of absorption, distribution, metabolism, excretion, toxicology and pharmacokinetics of drugs. ADMET and DMPK publishes the following types of contributions: - Original research papers - Feature articles - Review articles - Short communications and Notes - Letters to Editors - Book reviews The scope of the Journal involves, but is not limited to, the following areas: - physico-chemical properties of drugs and methods of their determination - drug permeabilities - drug absorption - drug-drug, drug-protein, drug-membrane and drug-DNA interactions - chemical stability and degradations of drugs - instrumental methods in ADMET - drug metablic processes - routes of administration and excretion of drug - pharmacokinetic/pharmacodynamic study - quantitative structure activity/property relationship - ADME/PK modelling - Toxicology screening - Transporter identification and study
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