Cocrystallisation by freeze-drying: preparation of novel multicomponent crystal forms
Cocrystallisation by freeze-drying: preparation of novel multicomponent crystal forms
We demonstrate the utility of freeze-drying as a general method for cocrystal synthesis as well as for the preparation of new solid forms of drug-coformer cocrystal systems. Using this approach, several previously reported cocrystal phases containing pharmaceutical compounds were reproduced. In addition, a novel solid solution of caffeine and theophylline and a potential new crystal form of the theophylline:oxalic acid cocrystal were prepared. It is shown that cocrystal formation proceeds via an amorphous phase which is generated as solvent sublimes during the freeze-drying process. The application of freeze drying to cocrystallisation is advantageous as it avoids problems caused by differences in the solubilities of coformers, and is a technique which is widely used to prepare products on an industrial scale, such as in the manufacture of pharmaceutical dosage forms
4599-4606
Eddleston, Mark D.
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Patel, Bhavnita
a09373e5-b09f-44c1-8106-4bd93a05a408
Day, Graeme M.
e3be79ba-ad12-4461-b735-74d5c4355636
Jones, William
3173abf0-1cfa-45f0-996e-2586b385c21e
2 October 2013
Eddleston, Mark D.
01211ad8-8115-43de-914c-6501d1d4c584
Patel, Bhavnita
a09373e5-b09f-44c1-8106-4bd93a05a408
Day, Graeme M.
e3be79ba-ad12-4461-b735-74d5c4355636
Jones, William
3173abf0-1cfa-45f0-996e-2586b385c21e
Eddleston, Mark D., Patel, Bhavnita, Day, Graeme M. and Jones, William
(2013)
Cocrystallisation by freeze-drying: preparation of novel multicomponent crystal forms.
Crystal Growth & Design, 13 (10), .
(doi:10.1021/cg401179s).
Abstract
We demonstrate the utility of freeze-drying as a general method for cocrystal synthesis as well as for the preparation of new solid forms of drug-coformer cocrystal systems. Using this approach, several previously reported cocrystal phases containing pharmaceutical compounds were reproduced. In addition, a novel solid solution of caffeine and theophylline and a potential new crystal form of the theophylline:oxalic acid cocrystal were prepared. It is shown that cocrystal formation proceeds via an amorphous phase which is generated as solvent sublimes during the freeze-drying process. The application of freeze drying to cocrystallisation is advantageous as it avoids problems caused by differences in the solubilities of coformers, and is a technique which is widely used to prepare products on an industrial scale, such as in the manufacture of pharmaceutical dosage forms
Text
cg401179s_accepted.pdf
- Accepted Manuscript
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e-pub ahead of print date: 28 August 2013
Published date: 2 October 2013
Organisations:
Chemistry
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Local EPrints ID: 356235
URI: http://eprints.soton.ac.uk/id/eprint/356235
ISSN: 1528-7483
PURE UUID: d686af91-3d85-41d3-a661-c15ab6dcb1ab
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Date deposited: 30 Aug 2013 13:48
Last modified: 15 Mar 2024 03:44
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Author:
Mark D. Eddleston
Author:
Bhavnita Patel
Author:
William Jones
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