High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids

SL Morissette, Ö Almarsson, ML Peterson… - Advanced drug delivery …, 2004 - Elsevier
SL Morissette, Ö Almarsson, ML Peterson, JF Remenar, MJ Read, AV Lemmo, S Ellis…
Advanced drug delivery reviews, 2004Elsevier
The concepts of high-throughput (HT) screening and combinatorial synthesis have been
integrated into the pharmaceutical discovery process, but are not yet commonplace in the
pharmaceutical development arena. Emerging strategies to speed pharmaceutical
development and capture solid form diversity of pharmaceutical substances have resulted in
the emergence of HT crystallization technologies. The primary type of diversity often refers to
polymorphs, which are different crystal forms of the same chemical composition. However …
The concepts of high-throughput (HT) screening and combinatorial synthesis have been integrated into the pharmaceutical discovery process, but are not yet commonplace in the pharmaceutical development arena. Emerging strategies to speed pharmaceutical development and capture solid form diversity of pharmaceutical substances have resulted in the emergence of HT crystallization technologies. The primary type of diversity often refers to polymorphs, which are different crystal forms of the same chemical composition. However, diverse salt forms, co-crystals, hydrates and solvates are also amenable to study in HT crystallization systems. The impact of form diversity encompasses issues of stability and bioavailability, as well as development considerations such as process definition, formulation design, patent protection and regulatory control. This review highlights the opportunities and challenges of HT crystallization technologies as they apply to pharmaceutical research and development.
Elsevier
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