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Coprocessing of pharmaceutical cocrystals for high quality and enhanced physicochemical stability

Coprocessing of pharmaceutical cocrystals for high quality and enhanced physicochemical stability

Ross, Steven A., Ward, Adam, Basford, Pat, McAllister, Mark and Douroumis, Dennis ORCID: 0000-0002-3782-0091 (2018) Coprocessing of pharmaceutical cocrystals for high quality and enhanced physicochemical stability. Crystal Growth & Design, 19 (2). pp. 876-888. ISSN 1528-7483 (Print), 1528-7505 (Online) (doi:https://doi.org/10.1021/acs.cgd.8b01440)

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Abstract

Solid state synthesis of high-quality indomethacin–saccharin cocrystals was achieved using hot melt extrusion. The physical and chemical stability of the formed cocrystals was enhanced through coprocessing with inert excipients at the final kneading zone. For the purposes of the study, the synthesized cocrystals were coprocessed with a crystalline hydrophilic polymer (PEG 6000), an amorphous hydrophilic polymer (hydroxypropylmethyl cellulose, HPMC), and an aluminometasilicate inorganic (Neusilin) excipient. Physiochemical characterization of the suspended cocrystals in the Neusilin and HPMC carriers revealed superior stability and the absence of any interactions between the excipients and the parent cocrystals. In contrast extruded cocrystals that were not suspended in any excipient or coprocessed with PEG 6000 underwent disassociation under accelerated conditions. Surface dissolution analysis demonstrated that Neusilin and PEG 6000 have no effect on the cocrystal dissolution rates (>90%), while HPMC led to in situ gelling effect and hence in slower rates (∼4%). In conclusion, cocrystals with high crystallinity and improved physicochemical stability can be synthesized by coprocessing with excipients that are inert and nonmiscible and have good thermal stability and low viscosity.

Item Type: Article
Uncontrolled Keywords: General materials science, general chemistry, condensed matter physics
Subjects: Q Science > QC Physics
Q Science > QD Chemistry
Faculty / Department / Research Group: Faculty of Engineering & Science
Faculty of Engineering & Science > School of Science (SCI)
SWORD Depositor: Publications Router
Last Modified: 01 May 2020 15:06
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
Selected for GREAT 2019: None
Selected for REF2021: REF 6
URI: http://gala.gre.ac.uk/id/eprint/25056

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