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Cocrystallisation by freeze-drying: preparation of novel multicomponent crystal forms

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
1528-7483
4599-4606
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.
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), 4599-4606. (doi:10.1021/cg401179s).

Record type: Article

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

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e-pub ahead of print date: 28 August 2013
Published date: 2 October 2013
Organisations: Chemistry

Identifiers

Local EPrints ID: 356235
URI: http://eprints.soton.ac.uk/id/eprint/356235
ISSN: 1528-7483
PURE UUID: d686af91-3d85-41d3-a661-c15ab6dcb1ab
ORCID for Graeme M. Day: ORCID iD orcid.org/0000-0001-8396-2771

Catalogue record

Date deposited: 30 Aug 2013 13:48
Last modified: 05 Nov 2019 01:38

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