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

Autor: Francesco Tres, Steven R. Coombes, Andrew R. Phillips, Leslie P. Hughes, Stephen A. C. Wren, Jonathan W. Aylott, Jonathan C. Burley
Jazyk: angličtina
Rok vydání: 2015
Předmět:
Zdroj: Molecules, Vol 20, Iss 9, Pp 16404-16418 (2015)
Druh dokumentu: article
ISSN: 1420-3049
DOI: 10.3390/molecules200916404
Popis: 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.
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