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Molecules 2015, 20(9), 16404-16418; doi:10.3390/molecules200916404

Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR

1
School of Pharmacy, Boots Science Building, University of Nottingham, Nottingham NG7 2RD, UK
2
Pharmaceutical Development, AstraZeneca, Macclesfield SK10 2NA, UK
*
Authors to whom correspondence should be addressed.
Academic Editors: Thomas Rades, Holger Grohganz and Korbinian LÃűbmann
Received: 9 July 2015 / Revised: 30 August 2015 / Accepted: 2 September 2015 / Published: 10 September 2015
(This article belongs to the Collection Poorly Soluble Drugs)
View Full-Text   |   Download PDF [2273 KB, uploaded 10 September 2015]   |  

Abstract

We have investigated the dissolution performance of amorphous solid dispersions of poorly water-soluble bicalutamide in a Kollidon VA64 polymeric matrix as a function of the drug loading (5% vs. 30% bicalutamide). A combined suite of state-of-the-art analytical techniques were employed to obtain a clear picture of the drug release, including an integrated magnetic resonance imaging UV-Vis flow cell system and 1H-NMR. Off-line 1H-NMR was used for the first time to simultaneously measure the dissolution profiles and rates of both the drug and the polymer from a solid dispersion. MRI and 1H-NMR data showed that the 5% drug loading compact erodes linearly, and that bicalutamide and Kollidon VA64 are released at approximately the same rate from the molecular dispersion. For the 30% extrudate, data indicated a slower water ingress into the compact which corresponds to a slower dissolution rate of both bicalutamide and Kollidon VA64. View Full-Text
Keywords: bicalutamide; poorly soluble drugs; amorphous solid dispersions; hot melt extrusion; solid-state transformations; magnetic resonance imaging; suppressed water 1H-NMR bicalutamide; poorly soluble drugs; amorphous solid dispersions; hot melt extrusion; solid-state transformations; magnetic resonance imaging; suppressed water 1H-NMR
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Tres, F.; Coombes, S.R.; Phillips, A.R.; Hughes, L.P.; Wren, S.A.C.; Aylott, J.W.; Burley, J.C. Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR. Molecules 2015, 20, 16404-16418.

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