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

Kulkarni, Chaitrali and Wood, Clive and Kelly, Adrian L. and Gough, Tim and Blagden, Nicholas and Paradkar, Anant (2015) Stoichiometric control of co-crystal formation by solvent free continuous co-crystallization (SFCC). Crystal Growth & Design, 15 (12). pp. 5648-5651. ISSN 1528-7483

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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 cocrystal
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.

Keywords:Co-crystal, stoichiometry, caffeine, maleic acid, SFCC, NotOAChecked
Subjects:B Subjects allied to Medicine > B200 Pharmacology, Toxicology and Pharmacy
F Physical Sciences > F100 Chemistry
Divisions:College of Science > School of Pharmacy
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ID Code:19487
Deposited On:05 Nov 2015 11:40

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