Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals

The aim of the study was the manufacturing and scale-up of theophylline-nicotinamide (THL-NIC) pharmaceutical cocrystals processed by hot-melt extrusion (HME). The barrel temperature profile, feed rate and screw speed were found to be the critical processing parameters with a residence time of appro...

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Bibliographic Details
Published in:Pharmaceutics 2021-03, Vol.13 (3), p.419
Main Authors: Ross, Steven A, Hurt, Andrew P, Antonijevic, Milan, Bouropoulos, Nicolaos, Ward, Adam, Basford, Pat, McAllister, Mark, Douroumis, Dennis
Format: Article
Language:English
Subjects:
cocrystals
continuous manufacturing
hot-melt extrusion
Rietveld refinement
scale-up
X-ray
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Summary:The aim of the study was the manufacturing and scale-up of theophylline-nicotinamide (THL-NIC) pharmaceutical cocrystals processed by hot-melt extrusion (HME). The barrel temperature profile, feed rate and screw speed were found to be the critical processing parameters with a residence time of approximately 47 s for the scaled-up batches. Physicochemical characterization using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction of bulk and extruded materials revealed the formation of high purity cocrystals (98.6%). The quality of THL-NIC remained unchanged under accelerated stability conditions.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics13030419