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Pharmaceutical cocrystals: along the path to improved medicines
Naga K Duggirala1, Miranda L Perry1, Örn Almarsson2
1Department of Chemical & Environmental Sciences and Bernal Institute, University of Limerick, Limerick, Republic of Ireland. xtal@ul.ie.
Chemical Communications (Cambridge, England)
|November 14, 2015
Summary
Pharmaceutical cocrystals offer a way to improve drug properties without altering the drug molecule itself. This review covers recent advances in designing, discovering, and developing these cocrystals for drug products.
Area of Science:
- Crystal engineering
- Pharmaceutical sciences
- Materials science
Background:
- Cocrystals, crystalline solids composed of multiple components, are increasingly vital in drug development.
- Pharmaceutical cocrystals modify drug physicochemical properties without covalent modification.
- Recent advances have spurred interest since a 2004 review.
Purpose of the Study:
- To review recent advances in the design, discovery, and development of pharmaceutical cocrystals.
- To explore nomenclature, design strategies, synthesis methods, and drug product development.
- To highlight the potential of cocrystals in improving drug performance.
Main Methods:
- Review of literature and recent case studies.
- Analysis of cocrystal classification (molecular cocrystals and ionic cocrystals).
- Discussion of design principles using supramolecular synthons.
Main Results:
- Cocrystals, particularly ionic cocrystals (ICCs), offer diverse compositions and properties.
- Design strategies enable tailored physicochemical properties.
- Seven case studies demonstrate improved drug properties and clinical performance, including an approved ICC product.
Conclusions:
- Pharmaceutical cocrystals are a valuable tool for enhancing drug properties and clinical efficacy.
- Ionic cocrystals present significant opportunities due to their compositional diversity and designability.
- Continued research and development in cocrystal technology are crucial for future drug products.
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