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Hansen solubility parameter as a tool to predict cocrystal formation
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Damascus University.
Luleå University of Technology, Department of Health Sciences, Medical Science.ORCID iD: 0000-0002-6050-0432
Luleå University of Technology, Department of Health Sciences, Medical Science.ORCID iD: 0000-0002-0654-5410
2011 (English)In: International Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 407, no 1-2, p. 63-71Article in journal (Refereed) Published
Abstract [en]

The objective of this study was to investigate whether the miscibility of a drug and coformer, as predicted by Hansen Solubility Parameters (HSPs), can indicate cocrystal formation and guide cocrystal screening. It was also our aim to evaluate various HSPs-based approaches in miscibility prediction. HSPs for indomethacin (the model drug) and over thirty coformers were calculated according to the group contribution method. Differences in the HSPs between indomethacin and each coformer were then calculated using three established approaches, and the miscibility was predicted. Subsequently, differential scanning calorimetry was used to investigate the experimental miscibility and cocrystal formation. The formation of cocrystals was also verified using liquid-assisted grinding. All except one of the drug-coformers that were predicted to be miscible were confirmed experimentally as miscible. All tested theoretical approaches were in agreement in predicting miscibility. All systems that formed cocrystals were miscible. Remarkably, two new cocrystals of indomethacin were discovered in this study. Though it may be necessary to test this approach in a wide range of different coformer and drug compound types for accurate generalizations, the trends with tested systems were clear and suggest that the drug and coformer should miscible for cocrystal formation. Thus, predicting the miscibility of cocrystal components using solubility parameters can guide the selection of potential coformers prior to exhaustive cocrystal screening work.

Place, publisher, year, edition, pages
2011. Vol. 407, no 1-2, p. 63-71
National Category
Other Health Sciences
Research subject
Health Science
Identifiers
URN: urn:nbn:se:ltu:diva-2591DOI: 10.1016/j.ijpharm.2011.01.030ISI: 000288777400008PubMedID: 21256944Scopus ID: 2-s2.0-79952312360Local ID: 0398b031-3548-4efb-b105-d72a6f089e26OAI: oai:DiVA.org:ltu-2591DiVA, id: diva2:975444
Note
Validerad; 2011; 20110128 (ysko)Available from: 2016-09-29 Created: 2016-09-29 Last updated: 2018-07-10Bibliographically approved

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Alhalaweh, AmjadVelaga, Sitaram

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