In Vitro Characterization of Concentration Enhancing Polymer Solid Dispersions Containing Itraconazole Produced by KinetiSol(R) Dispersing

摘要

Solid dispersions of itraconazole (ITZ) and various grades (LF, MF, HF) of the concentration enhancing polymer hypromellose acetate succinate (HPMCAS) were prepared by KinetiSol(R) Dispersing, a novel high energy solvent free manufacturing process for the production of solid dispersions, and characterized for solid state properties and in vitro dissolution performance. Inprocess results showed that the KinetiSol(R) Dispersing process was a rapid method for producing amorphous solid dispersions, with all batches demonstrating potencies between 95.0% to 105.0% of target and no significant degradation observed. All batches were also shown to be amorphous and in vitro dissolution testing showed that HPMCAS-LF provided the greatest degree and extent of supersaturation in neutral media, indicating that this composition could provide enhanced oral bioavailability of ITZ.