Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 106, Issue 1, Pages 100-110Publisher
WILEY-BLACKWELL
DOI: 10.1016/j.xphs.2016.06.017
Keywords
amorphous; crystallization; polymers; stabilization; solubility
Funding
- Dane O. Kildsig Center for Pharmaceutical Processing Research
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The effectiveness of different polymers, alone or in combination, in inhibiting the crystallization of celecoxib (CEX) fromamorphous solid dispersions (ASDs) exposed to different temperatures and relative humidities was evaluated. It was found that polyvinylpyrrolidone (PVP) and PVP-vinyl acetate formed stronger or more extensive hydrogen bonding with CEX than cellulose-based polymers. This, combined with their better effectiveness in raising the glass transition temperature (T-g) of the dispersions, provided better physical stabilization of amorphous CEX against crystallization in the absence of moisture when compared with dispersions formed with cellulose derivatives. In ternary dispersions containing 2 polymers, the physical stability was minimally impaired by the presence of a cellulose-based polymer when the major polymer present was PVP. On exposure to moisture, stability of the CEX ASDs was strongly affected by both the dispersion hygroscopicity and the strength of the intermolecular interactions. Binary and ternary ASDs containing PVP appeared to undergo partial amorphous-amorphous phase separation when exposed 94% relative humidity, followed by crystallization, whereas other binary ASDs crystallized directly without amorphous-amorphous phase separation. (C) 2016 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
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