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Mechanisms of increased bioavailability through amorphous solid dispersions: a review
被引:259
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Huwyler, Jorg
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Univ Basel, Div Pharmaceut Technol, Dept Pharmaceut Sci, Klingelbergstr 50, CH-4056 Basel, Switzerland Univ Basel, Div Pharmaceut Technol, Dept Pharmaceut Sci, Klingelbergstr 50, CH-4056 Basel, Switzerland

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[1] Univ Basel, Div Pharmaceut Technol, Dept Pharmaceut Sci, Klingelbergstr 50, CH-4056 Basel, Switzerland
[2] Univ Hosp Basel, Dept Biomed, Div Clin Pharmacol & Toxicol, Basel, Switzerland
[3] Univ Basel, Basel, Switzerland
关键词:
Amorphous solid dispersion;
excipients;
poorly water-soluble drugs;
oral bioavailability;
dissolution;
drug absorption;
SOLUBILITY-PERMEABILITY INTERPLAY;
WATER-SOLUBLE DRUGS;
SUPERSATURATED AQUEOUS-SOLUTIONS;
LIQUID PHASE-SEPARATION;
ACTIVE PHARMACEUTICAL INGREDIENTS;
TRPV1 ANTAGONIST ABT-102;
IN-VITRO;
ORAL BIOAVAILABILITY;
BIOPHARMACEUTICAL CLASSIFICATION;
PHYSICOCHEMICAL CHARACTERIZATION;
D O I:
10.1080/10717544.2019.1704940
中图分类号:
R9 [药学];
学科分类号:
1007 ;
摘要:
Amorphous solid dispersions (ASDs) can increase the oral bioavailability of poorly soluble drugs. However, their use in drug development is comparably rare due to a lack of basic understanding of mechanisms governing drug liberation and absorption in vivo. Furthermore, the lack of a unified nomenclature hampers the interpretation and classification of research data. In this review, we therefore summarize and conceptualize mechanisms covering the dissolution of ASDs, formation of supersaturated ASD solutions, factors responsible for solution stabilization, drug uptake from ASD solutions, and drug distribution within these complex systems as well as effects of excipients. Furthermore, we discuss the importance of these findings on the development of ASDs. This improved overall understanding of these mechanisms will facilitate a rational ASD formulation development and will serve as a basis for further mechanistic research on drug delivery by ASDs.
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页码:110 / 127
页数:18
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