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Experimental cocrystal screening and solution based scale-up cocrystallization methods
Faculty of Engineering and Science, University of Greenwich, Medway Campus, Chatham Maritime, Kent .
Faculty of Engineering and Science, University of Greenwich, Medway Campus, Chatham Maritime, Kent .
Faculty of Engineering and Science, University of Greenwich, Medway Campus, Chatham Maritime, Kent .
Luleå University of Technology, Department of Health Sciences, Medical Science.ORCID iD: 0000-0002-0654-5410
2017 (English)In: Advanced Drug Delivery Reviews, ISSN 0169-409X, E-ISSN 1872-8294Article in journal (Refereed) Epub ahead of print
Abstract [en]

Cocrystals are crystalline single phase materials composed of two or more different molecular and/or ionic compounds generally in a stoichiometric ratio which are neither solvates nor simple salts. If one of the components is an active pharmaceutical ingredient (API), the term pharmaceutical cocrystal is often used. There is a growing interest among drug development scientists in exploring cocrystals, as means to address physicochemical, biopharmaceutical and mechanical properties and expand solid form diversity of the API. Conventionally, coformers are selected based on crystal engineering principles, and the equimolar mixtures of API and coformers are subjected to solution-based crystallization that are commonly employed in polymorph and salt screening. However, the availability of new knowledge on cocrystal phase behaviour in solid state and solutions has spurred the development and implementation of more rational experimental cocrystal screening as well as scale-up methods. This review aims to provide overview of commonly employed solid form screening techniques in drug development with an emphasis on cocrystal screening methodologies. The latest developments in understanding and the use of cocrystal phase diagrams in both screening and solution based scale-up methods are also presented. Final section is devoted to reviewing the state of the art research covering solution based scale-up cocrystallization process for different cocrystals besides more recent continuous crystallization methods.

Place, publisher, year, edition, pages
Elsevier, 2017.
National Category
Other Health Sciences
Research subject
Health Science
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URN: urn:nbn:se:ltu:diva-65221DOI: 10.1016/j.addr.2017.08.006PubMedID: 28811184OAI: oai:DiVA.org:ltu-65221DiVA: diva2:1134680
Available from: 2017-08-21 Created: 2017-08-21 Last updated: 2017-08-21

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CiteExportLink to record
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