Continuous cocrystallization for dissolution rate optimization of a poorly water-soluble drug

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Moradiya, Hiren and Islam, Muhammad T. and Woollam, Grahame R. and Slipper, Ian J. and Halsey, Sheelagh and Snowden, Martin J. and Douroumis, D. (2014) Continuous cocrystallization for dissolution rate optimization of a poorly water-soluble drug. Crystal Growth and Design, 14 (1). pp. 189-198. ISSN 1528-7483 (https://doi.org/10.1021/cg401375a)

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Abstract

A continuous manufacturing process, hot melt extrusion (HME), was employed for the development of high quality carbamazepine–saccharin (CBZ–SCH) cocrystals. The produced cocrystals were compared with a prototype prepared by a solvent method. It was found that processing parameters such as temperature, screw speed, and screw configuration were the critical processing parameters. In-line near-infrared analysis demonstrated that cocrystallization takes place gradually during the process along the extruder’s mixing zones. Further characterization of the extruded cocrystals proved that the manufactured highly crystalline cocrystals were similar to the prototype but had improved CBZ dissolution rates. Continuous manufacturing of cocrystals of water-insoluble drugs is a novel and robust approach.

ORCID iDs

Moradiya, Hiren, Islam, Muhammad T. ORCID logoORCID: https://orcid.org/0000-0002-3530-0519, Woollam, Grahame R., Slipper, Ian J., Halsey, Sheelagh, Snowden, Martin J. and Douroumis, D.;
CORE (COnnecting REpositories)