High-throughput crystallization: Importance in process research and drug development

ORGN 800

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.