The combined use of imaging approaches to assess drug release from multicomponent solid dispersions
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Published version
Author(s)
Type
Journal Article
Abstract
PURPOSE: Imaging methods were used as tools to provide an understanding of phenomena that occur during dissolution experiments, and ultimately to select the best ratio of two polymers in a matrix in terms of enhancement of the dissolution rate and prevention of crystallization during dissolution. METHODS: Magnetic resonance imaging, ATR-FTIR spectroscopic imaging and Raman mapping have been used to study the release mechanism of a poorly water soluble drug, aprepitant, from multicomponent amorphous solid dispersions. Solid dispersions were prepared based on the combination of two selected polymers - Soluplus, as a solubilizer, and PVP, as a dissolution enhancer. Formulations were prepared in a ratio of Soluplus:PVP 1:10, 1:5, 1:3, and 1:1, in order to obtain favorable properties of the polymer carrier. RESULTS: The crystallization of aprepitant during dissolution has occurred to a varying degree in the polymer ratios 1:10, 1:5, and 1:3, but the increasing presence of Soluplus in the formulation delayed the onset of crystallization. The Soluplus:PVP 1:1 solid dispersion proved to be the best matrix studied, combining the abilities of both polymers in a synergistic manner. CONCLUSIONS: Aprepitant dissolution rate has been significantly enhanced. This study highlights the benefits of combining imaging methods in order to understand the release process.
Date Issued
2016-08-29
Date Acceptance
2016-07-25
Citation
Pharmaceutical Research, 2016, 34 (5), pp.990-1001
ISSN
1573-904X
Publisher
American Association of Pharmaceutical Scientists
Start Page
990
End Page
1001
Journal / Book Title
Pharmaceutical Research
Volume
34
Issue
5
Copyright Statement
© The Author(s) 2016. This article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.
Identifier
http://www.ncbi.nlm.nih.gov/pubmed/27573574
PII: 10.1007/s11095-016-2018-x
Subjects
Science & Technology
Physical Sciences
Life Sciences & Biomedicine
Chemistry, Multidisciplinary
Pharmacology & Pharmacy
Chemistry
amorphous solid dispersion
confocal Raman spectroscopy
crystallisation
FT-IR spectroscopic imaging
magnetic resonance imaging
WATER-SOLUBLE POLYMERS
PRECIPITATION
SURFACTANTS
BEHAVIOR
GROWTH
IMPACT
1115 Pharmacology And Pharmaceutical Sciences
Publication Status
Published