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

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 c...

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Autores principales: Tres, Francesco, Coombes, Steven R., Phillips, Andrew R., Hughes, Leslie P., Wren, Stephen A. C., Aylott, Jonathan W., Burley, Jonathan C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6331940/
https://www.ncbi.nlm.nih.gov/pubmed/26378506
http://dx.doi.org/10.3390/molecules200916404
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author Tres, Francesco
Coombes, Steven R.
Phillips, Andrew R.
Hughes, Leslie P.
Wren, Stephen A. C.
Aylott, Jonathan W.
Burley, Jonathan C.
author_facet Tres, Francesco
Coombes, Steven R.
Phillips, Andrew R.
Hughes, Leslie P.
Wren, Stephen A. C.
Aylott, Jonathan W.
Burley, Jonathan C.
author_sort Tres, Francesco
collection PubMed
description 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 [Formula: see text] H-NMR. Off-line [Formula: see text] H-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 [Formula: see text] H-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.
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spelling pubmed-63319402019-01-24 Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR Tres, Francesco Coombes, Steven R. Phillips, Andrew R. Hughes, Leslie P. Wren, Stephen A. C. Aylott, Jonathan W. Burley, Jonathan C. Molecules Article 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 [Formula: see text] H-NMR. Off-line [Formula: see text] H-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 [Formula: see text] H-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. MDPI 2015-09-10 /pmc/articles/PMC6331940/ /pubmed/26378506 http://dx.doi.org/10.3390/molecules200916404 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tres, Francesco
Coombes, Steven R.
Phillips, Andrew R.
Hughes, Leslie P.
Wren, Stephen A. C.
Aylott, Jonathan W.
Burley, Jonathan C.
Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR
title Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR
title_full Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR
title_fullStr Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR
title_full_unstemmed Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR
title_short Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton NMR
title_sort investigating the dissolution performance of amorphous solid dispersions using magnetic resonance imaging and proton nmr
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6331940/
https://www.ncbi.nlm.nih.gov/pubmed/26378506
http://dx.doi.org/10.3390/molecules200916404
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