The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid DispersionsReportar como inadecuado

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Pharmaceutical Research

, Volume 34, Issue 5, pp 990–1001

First Online: 29 August 2016Received: 01 June 2016Accepted: 25 July 2016DOI: 10.1007-s11095-016-2018-x

Cite this article as: Punčochová, K., Ewing, A.V., Gajdošová, M. et al. Pharm Res 2017 34: 990. doi:10.1007-s11095-016-2018-x


PurposeImaging 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.

MethodsMagnetic 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.

ResultsThe 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.

ConclusionsAprepitant dissolution rate has been significantly enhanced. This study highlights the benefits of combining imaging methods in order to understand the release process.

KEY WORDSamorphous solid dispersion confocal Raman spectroscopy crystallisation FT-IR spectroscopic imaging magnetic resonance imaging AbbreviationsATR-FTIRAttenuated total reflection-Fourier transform infrared spectroscopy

BCSBiopharmaceutics classification system

DSCDifferential scanning calorimetry

DVSDynamic vapour sorption

FTIRFourier transform infrared spectroscopy

HPLCHigh performance liquid chromatography

MRIMagnetic resonance imaging

MSMEMulti slice multi echo

MTDSCModulated temperature differential scanning calorimetry


USPUnited States pharmacopeia


XRDX-ray diffraction

Electronic supplementary materialThe online version of this article doi:10.1007-s11095-016-2018-x contains supplementary material, which is available to authorized users.

Autor: Kateřina Punčochová - Andrew V. Ewing - Michaela Gajdošová - Tomáš Pekárek - Josef Beránek - Sergei G. Kazarian -


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