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1.
Angew Chem Int Ed Engl ; 52(40): 10541-4, 2013 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-23955996

RESUMO

AFM of cocrystals: Atomic force microscopy can be used to observe phase changes at crystal surfaces where the transformation is accompanied by a change in the spacing between layers of molecules. The conversion of a metastable polymorph of the caffeine-glutaric acid cocrystal into the thermodynamically stable form was analyzed continuously in situ using intermittent-contact-mode atomic force microscopy.


Assuntos
Cristalização , Microscopia de Força Atômica/métodos , Cafeína/química , Glutaratos/química , Transição de Fase , Propriedades de Superfície , Termodinâmica
2.
J Pharm Sci ; 103(9): 2859-2864, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24481664

RESUMO

The dissociation at high humidity of cocrystals formed between caffeine and theophylline with a series of dicarboxylic acids is investigated and found to be driven by the partial dissolution of the acid, rather than by the formation of caffeine/theophylline hydrate. It is shown that partial dissociation occurs under all humidity conditions, and that cocrystals of compounds which do not form hydrates also dissociate by this mechanism. The observations made in this study indicate that cocrystal instability at high humidity will be a widespread issue, especially for cocrystals where the two coformers have widely differing aqueous solubilities, as is likely for systems where cocrystallisation is being used as means of improving the aqueous solubility, or dissolution rate, of a compound.


Assuntos
Preparações Farmacêuticas/química , Cafeína/química , Química Farmacêutica/métodos , Cristalização/métodos , Estabilidade de Medicamentos , Umidade , Solubilidade , Teofilina/química , Água/química
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