A classification system to assess the crystallization tendency of organic molecules from undercooled melts

Journal of Pharmaceutical Sciences
Jared A BairdLynne S Taylor

Abstract

Assessing the viability of an amorphous formulation strategy is of great importance in an era of drug discovery where a large percentage of new molecules have solubility limited dissolution rates, and disruption of the crystal lattice is a potential strategy to improve this process. The objective of the current study was to evaluate the glass forming ability (GFA) of a large data set of organic molecules and also to evaluate potential links between GFA and glass stability (GS). The crystallization tendency from the undercooled melt was evaluated for a group of 51 organic molecules and separated into three separate classes [class (I), class (II), class (III)] based upon the presence/absence of observable crystallization during a heating/cooling/heating cycle, as measured using differential scanning calorimetry (DSC). Class (I) molecules were further delineated based upon the observation of a crystalline [class (I-A)] or amorphous [class (I-B)] solid after quench cooling in liquid N(2). Principal component analysis (PCA) of various physiochemical descriptors suggested that molecules with low GFA tended to be low molecular weight (MW), rigid structures while class (III) molecules tended to be higher MW, more complex structures. Fo...Continue Reading

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Citations

Nov 1, 2011·European Biophysics Journal : EBJ·Richard J K WeberStephen R Byrn
Apr 27, 2013·International Journal of Pharmaceutics·Qingyan HuHarpreet Sandhu
Dec 18, 2013·International Journal of Pharmaceutics·Laura I Mosquera-GiraldoLynne S Taylor
May 29, 2012·Pharmaceutical Research·Zelalem AyenewGuy Van den Mooter
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Jan 4, 2012·Journal of Pharmaceutical Sciences·Kristyn Greco, Robin Bogner
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