Mechanisms of increased bioavailability through amorphous solid dispersions: a review

被引:259
作者
Schittny, Andreas [1 ,2 ,3 ]
Huwyler, Jorg [1 ]
Puchkov, Maxim [1 ]
机构
[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.
引用
收藏
页码:110 / 127
页数:18
相关论文
共 136 条
[71]   A Win-Win Solution in Oral Delivery of Lipophilic Drugs: Supersaturation via Amorphous Solid Dispersions Increases Apparent Solubility without Sacrifice of Intestinal Membrane Permeability [J].
Miller, Jonathan M. ;
Beig, Avital ;
Carr, Robert A. ;
Spence, Julie K. ;
Dahan, Arik .
MOLECULAR PHARMACEUTICS, 2012, 9 (07) :2009-2016
[72]   The Solubility-Permeability Interplay When Using Cosolvents for Solubilization: Revising the Way We Use Solubility-Enabling Formulations [J].
Miller, Jonathan M. ;
Beig, Avital ;
Carr, Robert A. ;
Webster, Gregory K. ;
Dahan, Arik .
MOLECULAR PHARMACEUTICS, 2012, 9 (03) :581-590
[73]   The Solubility-Permeability Interplay: Mechanistic Modeling and Predictive Application of the Impact of Micellar Solubilization on Intestinal Permeation [J].
Miller, Jonathan M. ;
Beig, Avital ;
Krieg, Brian J. ;
Carr, Robert A. ;
Borchardt, Thomas B. ;
Amidon, Gregory E. ;
Amidon, Gordon L. ;
Dahan, Arik .
MOLECULAR PHARMACEUTICS, 2011, 8 (05) :1848-1856
[74]   Impact of polymer type on bioperformance and physical stability of hot melt extruded formulations of a poorly water soluble drug [J].
Mitra, Amitava ;
Li, Li ;
Marsac, Patrick ;
Marks, Brian ;
Liu, Zhen ;
Brown, Chad .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2016, 505 (1-2) :107-114
[75]   Pharmaceutical development and preliminary clinical testing of an oral solid dispersion formulation of docetaxel (ModraDoc001) [J].
Moes, J. J. ;
Koolen, S. L. W. ;
Huitema, A. D. R. ;
Schellens, J. H. M. ;
Beijnen, J. H. ;
Nuijen, B. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2011, 420 (02) :244-250
[76]   Development of an oral solid dispersion formulation for use in low-dose metronomic chemotherapy of paclitaxel [J].
Moes, Johannes ;
Koolen, Stijn ;
Huitema, Alwin ;
Schellens, Jan ;
Beijnen, Jos ;
Nuijen, Bastiaan .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2013, 83 (01) :87-94
[77]   Crystallization Inhibition Properties of Cellulose Esters and Ethers for a Group of Chemically Diverse Drugs: Experimental and Computational Insight [J].
Mosquera-Giraldo, Laura I. ;
Borca, Carlos H. ;
Parker, Andrew S. ;
Dong, Yifan ;
Edgar, Kevin J. ;
Beaudoin, Stephen P. ;
Slipchenko, Lyudmila V. ;
Taylor, Lynne S. .
BIOMACROMOLECULES, 2018, 19 (12) :4593-4606
[78]   Influence of Polymer and Drug Loading on the Release Profile and Membrane Transport of Telaprevir [J].
Mosquera-Giraldo, Laura I. ;
Li, Na ;
Wilson, Venecia R. ;
Nichols, Brittany L. B. ;
Edgar, Kevin J. ;
Taylor, Lynne S. .
MOLECULAR PHARMACEUTICS, 2018, 15 (04) :1700-1713
[79]   Glass-Liquid Phase Separation in Highly Supersaturated Aqueous Solutions of Telaprevir [J].
Mosquera-Giraldo, Laura I. ;
Taylor, Lynne S. .
MOLECULAR PHARMACEUTICS, 2015, 12 (02) :496-503
[80]   Impact of surfactants on the crystal growth of amorphous celecoxib [J].
Mosquera-Giraldo, Laura I. ;
Trasi, Niraj S. ;
Taylor, Lynne S. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2014, 461 (1-2) :251-257