Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with poloxamer 188.

摘要

Ibuprofen-Poloxamer 188 (P 188) binary solid dispersions (SD) with different drug loadings were prepared, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR), and evaluated for solubility, in vitro release, and oral bioavailability of ibuprofen in rats. Loss of their individual surface properties during melting and solidification as revealed by SEM micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of its interactions with P 188. However, no such interactions in the solid state were confirmed by FTIR spectra which showed the presence of drug crystalline in SDs. Immediate and complete release of ibuprofen from SDs might be because of the reduction in the drug crystalline due to eutectic formation, and their dosing to fasted rats resulted in a significant increase in the area under curve (AUC) of the plasma concentration versus time curve and the maximum plasma concentration (Cmax), and a significant decrease in the time to reach Cmax (Tmax) over ibuprofen and physical mixtures.