Journal
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Volume 129, Issue -, Pages 367-377Publisher
ELSEVIER
DOI: 10.1016/j.jpba.2016.07.026
Keywords
Glipizide; Amorphization; Solid forms; Solid-state transformations
Categories
Funding
- Applied Basic Research Project of Sichuan Province [2014JY0042]
- Testing Platform Construction of Technology Achievement Transform of Sichuan Province [13CGPT0049]
- National Development and Reform Commission and Education of China [2014BW011]
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In this study, the amorphization of glipizide was systematically investigated through high-energy ball milling at different temperatures. The results of solid-state amorphization through milling indicated that glipizide underwent direct crystal-to-glass transformation at 15 and 25 degrees C and crystal-to-glass-to-crystal conversion at 35 degrees C; hence, milling time and temperature had significant effects on the amorphization of glipizide, which should be effectively controlled to obtain totally amorphous glipizide. Solid forms of glipizide were detailedly characterized through analyses of X-ray powder diffraction, morphology, thermal curves, vibrational spectra, and solid-state nuclear magnetic resonance. The physical stability of solid forms was investigated under different levels of relative humidity (RH) at 25 degrees C. Forms land III are kinetically stable and do not form any new solid-state forms at various RH levels. By contrast, Form II is kinetically unstable, undergoing direct glass-to-crystal transformation when RH levels higher than 32.8%. Therefore, stability investigation indicated that Form II should be stored under relatively,dry conditions to prevent rapid crystallization. High temperatures can also induce the solid-state transformation of Form II; the conversion rate increased with increasing temperature. (C) 2016 Elsevier B.V. All rights reserved.
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