Itraconazole/TPGS/Aerosil®200 solid dispersions: Characterization, physical stability and in vivo performance

摘要: Solid dispersions were successfully prepared by co-spray-drying of TPGS-stabilized itraconazole nanosuspensions with Aerosil200, followed heat treatment the powders. The itraconazole/Aerosil200 weight ratios amounted to 50/50, 30/70, 40/60 and 20/80. content powders was close expected value, relative errors between 0.3% 7.8%. X-ray powder diffraction (XRPD), solid state NMR (SSNMR) differential scanning calorimetry (DSC) evaluation on revealed formation amorphous absence glassy itraconazole. Dissolution enhanced compared crystalline (a 2-dimensional structured form itraconazole). However, no clear trend could be observed drug loading dissolution performance dispersions. Upon storage, conversion for 50/50 based XRPD, SSNMR DSC measurements. Although remained upon did reveal that a small fraction (7.5+/-1.6% after 10 months storage) crystallized storage. For 30/70 20/80 dispersions, crystallization seen. After important changes in behavior observed. A decrease seen dispersion, which attributed On other hand, 40/60, showed an increase rate (more than 60% min). not completely at this stage, adsorption onto Aerosil200 surface during storage might responsible behavior. Finally, vivo experiments performed rat. Oral bioavailability dispersion was, although lower marketed Sporanox formulation, significantly drug.