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

被引:335
作者
Jermain, Scott V. [1 ]
Brough, Chris [2 ]
Williams, Robert O., III [1 ]
机构
[1] Univ Texas Austin, Coll Pharm, Div Mol Pharmaceut & Drug Delivery, 2409 Univ Ave,A1920, Austin, TX 78712 USA
[2] DisperSol Technol LLC, 111 Cooperat Way, Georgetown, TX 78626 USA
关键词
Amorphous solid dispersion; Nanocrystal; Solubility; Oral delivery; FDA approved product; BIOPHARMACEUTICS CLASSIFICATION-SYSTEM; HOT-MELT EXTRUSION; POSACONAZOLE TABLET; PHASE-DIAGRAM; PARTICLE-SIZE; PHARMACOKINETIC VARIABILITY; PHARMACEUTICAL APPLICATIONS; IMPROVED BIOAVAILABILITY; DISSOLUTION ENHANCEMENT; STATE CHARACTERISTICS;
D O I
10.1016/j.ijpharm.2017.10.051
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:379 / 392
页数:14
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