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Use of supercritical CO 2 ‐aided and conventional melt extrusion for enhancing the dissolution rate of an active pharmaceutical ingredient
Author(s) -
Nagy Zsombor Kristóf,
Sauceau Martial,
Nyúl Katalin,
Rodier Elisabeth,
Vajna Balázs,
Marosi György,
Fages Jacques
Publication year - 2012
Publication title -
polymers for advanced technologies
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.61
H-Index - 90
eISSN - 1099-1581
pISSN - 1042-7147
DOI - 10.1002/pat.1991
Subject(s) - extrusion , supercritical fluid , dissolution , active ingredient , materials science , chemical engineering , solubility , chromatography , chemistry , organic chemistry , composite material , bioinformatics , engineering , biology
Dispersing at the molecular level a drug in a polymer matrix is a major challenge to be addressed by the pharmaceutical industry to enhance its bioavailability or to control its release. Melt extrusion and supercritical CO 2 ‐aided melt extrusion of solid pharmaceutical formulations were performed to enhance the dissolution rate of carvedilol, taken as a model of poorly soluble drug. The presence of the drug improved the processability of the polyacrylate matrix (Eudragit E) through its plasticizing effect. The supercritical method was found gentle compared with melt extrusion owing to the shorter residence time and lower processing temperature and melt viscosity. No traces of decomposition of the drug could be detected after the supercritical extrusion process based on capillary electrophoresis results. This extrusion process resulted in effective homogenization of the components and amorphization of the drug according to Raman mapping, Fourier transform infrared spectrometry, X‐ray diffraction, and polarized light microscopy. The kinetics of dissolution can be dramatically improved. Copyright © 2011 John Wiley & Sons, Ltd.