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

Molecules

Francesco Tres²  Steven R. Coombes³  Andrew R. Phillips³  Leslie P. Hughes³  Stephen A. C. Wren³  Jonathan W. Aylott²  Jonathan C. Burley²  Thomas Rades¹  Holger Grohganz¹ 

[1] School of Pharmacy, Boots Science Building, University of Nottingham, Nottingham NG7 2RD, UK; E-Mail;School of Pharmacy, Boots Science Building, University of Nottingham, Nottingham NG7 2RD, UK; E-Mail:;Pharmaceutical Development, AstraZeneca, Macclesfield SK10 2NA, UK; E-Mails:

关键词: bicalutamide;    poorly soluble drugs;    amorphous solid dispersions;    hot melt extrusion;    solid-state transformations;    magnetic resonance imaging;    suppressed water ¹H-NMR;   

DOI  :  10.3390/molecules200916404

来源: mdpi

【 摘 要 】

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 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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.