Physicochemical Characterization of Febuxostat Microcomplexes with Parent and Modified Cyclodextrins

Sayee V. Aher, Yogesh V. Pore

Abstract


Febuxostat, a BCS class II antigout drug was complexed with β-cyclodextrin (βCD), hydroxypropyl-β-
cyclodextrin (HPβCD) and / or methyl-β-cyclodextrin (MβCD), to improve its physicochemical properties. Earlier
phase solubility and thermodynamic investigations in acetate buffer (pH 4.5) illustrated AL (linear) type of solubility
curve and enthalpy driven complexation process, respectively. The association constant and complexation efficiency
of modified cyclodextrins (CDs) were significantly higher than that of parent cyclodextrin (CD). The microcomplexes
prepared by spray drying process were examined for their spectral, diffractometric, thermal, particle size,
saturation solubility, Log P and dissolution properties. The physicochemical properties of pure drug were improved
upon complexation with CDs. However, modified CDs produced amorphous micro-complexes contributing for their
better performance as compared to parent CD.


Keywords


Febuxostat; cyclodextrins; micro-complexes; characterization; thermodynamic; phase solubility.

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The Dhaka University Journal of Pharmaceutical Sciences
ISSN 1816-1820 (Print) 1816-1839 (Online)