| 초록 |
Itraconazole (ITZ) as a model hydrophobic drug was formulated to solid dispersion (SD) using enteric polymer, HPMCAS-LF, by a solvent controlled precipitation method (SCPM) using HCl as an anti-solvent, or a spray drying method (SDM). ITZ SD exhibited better dissolution compared to naive ITZ, limited dissolution in acidic conditions, and a burst release at neutral pH. Furthermore, the ITZ SD by SCPM indicated a smaller sized particle dispersion, limited dissolution at acidic pH, and a higher release at neutral pH compared to those by SDM. It showed improved ITZ absorption in male SD rats compared to the one by SDM and naïve ITZ. The increased protonation of the polymer by acidic anti-solvent could form a tighter hydrophobic aggregation with ITZ in SD and cause burst release in the transition state resulting in the supersaturation in the upper intestine and the enhanced drug absorption. This study suggests that the ITZ SD has potential to improve the bioavailability for patient. |
