4.7 Review

Pharmaceutical cocrystals and poorly soluble drugs

Journal

INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 453, Issue 1, Pages 101-125

Publisher

ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2012.10.043

Keywords

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

Funding

  1. Pfizer Institute for Pharmaceutical Materials
  2. Pfizer Global Research and Development
  3. EU INTERREG IVA 2 Mers-Seas-Zeeen Cross-border Cooperation Programme

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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. (c) 2012 Elsevier B.V. All rights reserved.

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