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难溶性药物体外-体内相关性(IVIVC)的体外方法:基于脂质的制剂视角

In vitro Methods for In vitro-In vivo Correlation (IVIVC) for Poorly Water Soluble Drugs: Lipid Based Formulation Perspective.

作者信息

Kazi Mohsin, Al Amri Rayan, Alanazi Fars K, Hussain Muhammad Delwar

机构信息

Kayyali Chair for Pharmaceutical Industries, College of Pharmacy, King Saud University, Riyadh-11451, Saudi Arabia.

Department of Pharmaceutical and Biomedical Sciences, College of Pharmacy, California Health Science University, Clovis, California 93612, United States.

出版信息

Curr Drug Deliv. 2018;15(7):918-929. doi: 10.2174/1567201815666180116090910.

DOI:10.2174/1567201815666180116090910
PMID:29336263
Abstract

A great number of new drug candidates identified from the discovery pipeline are poorly water soluble, which is a drawback to bring such candidates into the pharmaceutical market. Formulating these compounds as self-emulsifying/microemulsifying/ nanoemulsifying drug delivery systems (SEDDS/SMEDDS/SNEDDS) within lipid based formulations is of growing interest. Some of the recent studies have resulted in commercial products that provided improved bioavailability and dissolution due to the better dispersion properties of SEDDS/SMEDDS/SNEDDS. An ongoing challenge that the pharmaceutical industry is facing is identifying in vitro tests that are needed in order to predict the behavior of dosage forms in the GI tract. The goal of the current review is to present the various levels of in vitro-in vivo correlations (IVIVCs) and to provide tools on the utilization of the IVIVCs in product development and optimization of SEDDS/SMEDDS/SNEDDS.

摘要

从发现流程中确定的大量新药候选物水溶性较差,这是将此类候选物推向医药市场的一个缺点。将这些化合物制成基于脂质的自乳化/微乳化/纳米乳化药物递送系统(SEDDS/SMEDDS/SNEDDS)越来越受到关注。最近的一些研究已产生了商业产品,由于SEDDS/SMEDDS/SNEDDS具有更好的分散特性,这些产品的生物利用度和溶出度得到了提高。制药行业目前面临的一个挑战是确定预测剂型在胃肠道中行为所需的体外试验。本综述的目的是介绍体外-体内相关性(IVIVC)的不同水平,并提供在产品开发以及SEDDS/SMEDDS/SNEDDS的优化中利用IVIVC的工具

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