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Open AccessArticle

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
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Authors to whom correspondence should be addressed.
Academic Editors: Thomas Rades, Holger Grohganz and Korbinian LÃűbmann
Molecules 2015, 20(9), 16404-16418; https://doi.org/10.3390/molecules200916404
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)
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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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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