Solid-phase preparation and characterization of albendazole solid dispersion
Keywords:
Bioavailability, Solid dispersion, Solid-state interactionAbstract
Solid dispersion of albendazole (ABZ) was prepared by powder mixing method using Eudragit E-100 (EGT) as a carrier.The X-ray diffraction patterns and differential scanning calorimetric thermograms demonstrated that the crystallinity ofthe drug in the physical mixture decreased with the storage time. The higher the storage temperature and the higherthe relative humidity, and the higher the weight ratio of polymer in the mixture, the lower was the heat of fusion of thestored mixture. The specifi c interaction of ABZ with EGT in the solid state was investigated by infrared spectroscopy,and nuclear magnetic resonance. It was understood that EGT undergoes N-protonation, forming hydrogen bond at thetertiary nitrogen, in preference to O-protonation. Phase solubility study showed a linear increase in the solubility withthe polymer concentration. The enhancement of dissolution rate and the dissolution effi ciency depended on the heat offusion value as well as mixing ratio of the polymer. The stored mixture showed a signifi cantly enhanced bioavailabilityin rabbits compared to the freshly prepared one.Downloads
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