Formulation Characterization and Pharmacokinetic Evaluation of Amorphous Solid Dispersions of Dasatinib. Academic Article uri icon


  • The aim of this study was to improve the physicochemical properties and oral bioavailability of dasatinib (DST) by the amorphous solid dispersion (ASD) approach using cellulose acetate butyrate (CAB) as a carrier. Various formulations of ASD (DST:CAB 1:1 to 1:5) were prepared by the solvent evaporation method. ASDs were characterized for physicochemical attributes, stability and pharmacokinetics. Scanning electron microscopy, Fourier transformed infrared, X-ray powder diffraction, and differential scanning calorimetry confirmed the transformation of the crystalline drug into amorphous phase. ASD formation resulted in a 3.74.9 fold increase in dissolution compared to DST or physical mixture. The ASDs formulation exhibited relative stability against transformation from the unstable amorphous phase to a stable crystalline phase that was indicated by spectral and X-ray powder diffraction data, and insignificant (p > 0.05) decrease in dissolution. Tmax, Cmax and AUC0- of ASD were 4.3-fold faster and 2.0 and 1.5 fold higher than the corresponding physical mixture. In conclusion, the ASD of DST significantly improved dissolution and oral bioavailability which may be translated into a reduction in dose and adverse events.

published proceedings

  • Pharmaceutics

author list (cited authors)

  • Dharani, S., Mohamed, E. M., Khuroo, T., Rahman, Z., & Khan, M. A.

citation count

  • 1

complete list of authors

  • Dharani, Sathish||Mohamed, Eman M||Khuroo, Tahir||Rahman, Ziyaur||Khan, Mansoor A

publication date

  • November 2022