Stoichiometric control of co-crystal formation by solvent free continuous co-crystallization (SFCC).
View/ Open
Main article (507.3Kb)
Download
Publication date
2015Author
Kulkarni, Chaitrali S.Wood, Clive
Kelly, Adrian L.
Gough, Tim

Blagden, Nicholas
Paradkar, Anant R

Keyword
StoichiometryCaffeine
Maleic acid
Solvent free continuous co-crystallization (SFCC)
Co-crystals
Rights
© 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.5b00806Peer-Reviewed
YesOpen Access status
openAccessAccepted for publication
2015-10-29
Metadata
Show full item recordAbstract
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 manuscriptCitation
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.Link to Version of Record
https://doi.org/10.1021/acs.cgd.5b00806Type
Articleae974a485f413a2113503eed53cd6c53
https://doi.org/10.1021/acs.cgd.5b00806