Approaches to high-throughput physical form screening and discovery

A.J. Florence, Harry G. Brittain (Editor)

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

The development of experimental methods for increasing the throughput and efficiency of all stages of drug discovery and development is an important area of research within the pharmaceutical industry. In the context of physical form discovery of pharmaceuticals, the fundamental aim when establishing a rigorous experimental crystallization search strategy is to achieve as wide a coverage of crystallization conditions and methods as possible within the constraints of available time, material, and resources. For the purposes of this chapter, physical form will be taken to mean any solid form of the compound being examined, whether crystalline (polymorphs, solvates, salts, and co-crystals) or non-crystalline (amorphous). Automated crystallization approaches allow the basic process steps involved in a typical manual solution recrystallization method (Fig. 1) to be efficiently replicated over large numbers of parallel experiments. In principle, this enables the routine implementation of search strategies designed to maximize the diversity of crystallization conditions tested, allowing the experimental search to be carried out over a finer grid (e.g., a larger solvent library).
Original languageEnglish
Title of host publicationPolymorphism in Pharmaceutical Solids, Second Edition
PublisherInforma Healthcare
Number of pages664
ISBN (Print)9781420073225
Publication statusPublished - Jul 2009

Keywords

  • polymorphism
  • pharmaceutical
  • solids
  • solvatomorphism
  • thermodynamic
  • phase rule
  • computational methodologies
  • cocrystals
  • crystallographic
  • spectroscopy
  • amorphous solids
  • high-throughput

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