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无定形固体分散体和纳米晶体技术在难溶性药物传递中的应用-更新。

Amorphous solid dispersions and nanocrystal technologies for poorly water-soluble drug delivery - An update.

机构信息

Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, 2409 University Ave., A1920, Austin, TX 78712, USA.

DisperSol Technologies, LLC, 111 Cooperative Way, Georgetown, TX 78626, USA.

出版信息

Int J Pharm. 2018 Jan 15;535(1-2):379-392. doi: 10.1016/j.ijpharm.2017.10.051. Epub 2017 Nov 8.

Abstract

Poor water-solubility remains a typical property of drug candidates in pharmaceutical development pipelines today. Various processes have been developed to increase the solubility, dissolution rate, and bioavailability of these active ingredients belonging to biopharmaceutical classification system (BCS) II and IV classifications. Since the early 2000s, nanocrystal delivery and amorphous solid dispersions are more established techniques to overcome the limitations of poorly-water soluble drugs in FDA available products. This article provides an updated review of nanocrystal and amorphous solid dispersion techniques primarily for orally delivered medicaments. The thermodynamic and kinetic theories relative to these technologies are presented along with marketed product evaluations and a survey of commercially relevant scientific literature.

摘要

如今,较差的水溶性仍然是药物研发管线上候选药物的典型特征。已经开发出各种工艺来提高属于生物药剂学分类系统 (BCS) II 和 IV 类的这些活性成分的溶解度、溶解速率和生物利用度。自 21 世纪初以来,纳米晶体传递和无定形固体分散体是克服 FDA 现有产品中水溶性差的药物局限性的更为成熟的技术。本文主要针对口服药物,对纳米晶体和无定形固体分散体技术进行了更新的综述。本文介绍了与这些技术相关的热力学和动力学理论,以及市售产品评估和商业相关科学文献调查。

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