[Getting the right crystal structure for commercial use]
This is one of those things we never think much about here in biofreak land. Process chemistry. The end game of drug development. But substantial improvements in process chemistry can save the entire industry bundles of money, and as such, they are worth digging for. Today Derek Lowe profiled this paper as showing the potential for such an improvement:
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A New Strategy of Transforming Pharmaceutical Crystal Forms
Jian Tian†, Scott J. Dalgarno§, and Jerry L. Atwood*
Department of Chemistry, University of Missouri—Columbia, Columbia, Missouri 65211, United States
J. Am. Chem. Soc., Article ASAP
DOI: 10.1021/ja107617m
Publication Date (Web): January 5, 2011
atwoodj@missouri.edu
† Author Present Address
Energy and Environment Directorate, Pacific Northwest National Laboratory, Richland, WA, 99352, U.S.A.
§ Author Present Address
School of Engineering and Physical Sciences-Chemistry, Heriot-Watt University, Edinburgh, EH14 4AS, U.K.
Abstract
The robust nature of network materials allows them to (for example) respond to external stimuli such as pressure, temperature, light, or gas/solvent adsorption and desorption. There is difficulty in retaining long-range order in purely molecular organic solids, due to weak intermolecular interactions such as van der Waals forces. Here, we show gas-induced transformations of the well-known pharmaceuticals clarithromycin and lansoprazole. For clarithromycin, the stimulus is capable of converting the kinetic solvate and guest-free crystal forms to the commercial thermodynamically stable polymorph with a huge saving in energy cost relative to industrially employed methods. The synthesis of the marketing form of lansoprazole involves a solvate that readily decomposes and that is stirred in water, filtered, and dried intensively. Our method readily circumvents such synthetic problems and transforms the sensitive solvate to the marketed drug substance with ease. Such expedient transformations hold great implications for the pharmaceutical industry in general when considering the ease of transformation and mild conditions employed.<<
Dr. Lowe's thoughts on it here:
pipeline.corante.com
I did a quick patent and app search and found nada for these authors -- which I find a little strange. Filing in the worth watching category.
Cheers, Tuck |
