Journal
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 20, Issue 3, Pages 305-317Publisher
ELSEVIER
DOI: 10.1016/S0928-0987(03)00201-X
Keywords
celecoxib; polymorph; pseudopolymorphs; amorphous; solid-state characterization
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This study deals with the generation and characterization of various solid-state forms of celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor. The drug was subjected to polymorphic screen using different solvents to explore the possibility of existence of different solid forms. N,N-Dimethyl acetamide (DMA) and N,N-dimethyl formamide (DMF) yielded solvates in 1: 1 stoichiometric ratio. Quench cooling of the melt resulted in amorphous form of the drug. All these solid-state forms were characterized by thermoanalytical (DSC, TGA, HSM), crystallographic (XRD), microscopic (polarized, SEM), spectroscopic (FTIR), and elemental analysis techniques. Solubility and van't Hoff studies were carried out for their thermodynamic interpretation. Influence of morphology of different solid-state forms on flow behavior was also investigated. Molecular modeling studies were used to elucidate the interaction between solute and solvent molecules in the solvate. (C) 2003 Elsevier B.V. All rights reserved.
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