High-throughput crystallization: Importance in process research and drug development
Arlene E. McKeown, arlene_mckeown@merck.com, Jennifer R. Chilenski, Louis S. Crocker, crocker@merck.com, David J. Mathre, and Vicky K. Vydra. Center for Physichochemical Characterization, Merck Research Laboratories, Process Research, PO Box 2000, Rahway, NJ 07065
Owing to an
increasing demand for the identification of crystalline phases of a drug
substance early in the development process, employing minimal quantities of
valuable compound, high throughput crystallization is playing an increasing
role in drug development. Fast evaluation and identification of solid phases of
a drug are critical for drug substance phase selection and intellectual
property protection. Moreover, the discovery of crystalline synthetic intermediates
of a drug has importance in process development allowing for more efficient
syntheses of the drug substance. The work described herein details rapid and
economical methods for the identification and evaluation of crystalline phases
of drug substances and their key synthetic intermediates, and highlights the
importance of high throughput crystallization in the pharmaceutical industry.