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Int J Pharm. 2013 Aug 30;453(1):101-25. doi: 10.1016/j.ijpharm.2012.10.043. Epub 2012 Dec 1.

Pharmaceutical cocrystals and poorly soluble drugs.

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Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, UK.


In recent years cocrystal formation has emerged as a viable strategy towards improving the solubility and bioavailability of poorly soluble drugs. In this review the success of numerous pharmaceutical cocrystals for the improvement of the solubility and dissolution rates of poorly soluble drugs is demonstrated using various examples taken from the literature. The role of crystal engineering principles in the selection of appropriate coformers and the nature of the supramolecular synthons present within the crystals are described. Evidence for improved animal pharmacokinetic data is given for several systems. A summary is provided of our current understanding of the relationship between cocrystal structure and solution phase interactions on solubility as well as those factors that influence overall cocrystal thermodynamic stability.


Cocrystals; Crystal engineering; Pharmaceutical cocrystallisation; Poorly soluble drugs; Solubility enhancement; Supramolecular chemistry

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