Yes / 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.
| Identifer | oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/7460 |
| Date | 29 October 2015 |
| Creators | Kulkarni, Chaitrali S., Wood, Clive, Kelly, Adrian L., Gough, Tim, Blagden, Nicholas, Paradkar, Anant R |
| Source Sets | Bradford Scholars |
| Language | English, English |
| Detected Language | English |
| Type | Article, Accepted manuscript |
| 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.5b00806, Unspecified |
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