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Stoichiometric control of co-crystal formation by solvent free continuous co-crystallization (SFCC).

Kulkarni, Chaitrali S.
Wood, Clive
Kelly, Adrian L.
Blagden, Nicholas
Publication Date
2015
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© 2016 ACS. Reproduced in accordance with the publisher's self-archiving policy. This document is the author's version of a Submitted Work that was accepted for publication in Crystal Growth & Design. Copyright © American Chemical Society after peer review. To access the final edited and published work see http://dx.doi.org/10.1021/acs.cgd.5b00806
Peer-Reviewed
Yes
Open Access status
openAccess
Accepted for publication
2015-10-29
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Abstract
Reproducible control of stoichiometry and difficulties in large scale production have been identified as two of the major challenges to commercial uptake of pharmaceutical co-crystals. The aim of this research was to extend the application of SFCC to control stoichiometry in caffeine: maleic acid co-crystals. Both 1:1 and 2:1 caffeine: maleic acid co-crystals were produced by control of the feedstock composition and process conditions. It was also observed that formation of 2:1 stoichiometry co-crystals involved formation of a 1:1 co-crystal which was subsequently transformed to 2:1 co-crystals. The investigation of stoichiometric transformation revealed that although 1:1 co-crystals could be converted into 2:1 form with addition of excess caffeine, the reverse was not possible in the presence of excess maleic acid. However, conversion from 2:1 into 1:1 was only achieved by melt seeding with the phase pure 1:1 co-crystals. This investigation demonstrates that stoichiometric control can be achieved by SFCC by control of parameters such as extrusion temperature.
Version
Accepted manuscript
Citation
Kulkarni C, Wood C, Kelly AL et al (2015) Stoichiometric control of co-crystal formation by solvent free continuous co-crystallization (SFCC). Crystal Growth & Design. 15(12): 5648–5651.
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Article
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