Development of omega-3 phospholipid-based solid dispersion of fenofibrate for the enhancement of oral bioavailability

作者：Yang Liang; Shao Yating; Han Hyo Kyung^*

来源：European Journal of Pharmaceutical Sciences, 2015, 78: 103-110.

DOI：10.1016/j.ejps.2015.07.007

• Antisolvent
• Omega-3 phospholipids
• Fenofibrate
• Dissolution
• Bioavailability

This research aimed to develop the omega-3 phospholipids based solid dispersion to improve the oral bioavailability of fenofibrate. The omega-3 phospholipids based solid dispersion formulation (OPSD) was prepared by an antisolvent precipitation with immediate freeze-drying and the optimal composition of the formulation was determined as the ratios of sucrose to krill oil of 5:1 (w/w), krill oil to fenofibrate of 1.5:1 (w/w), and antisolvent to solvent of 6:4 (v/v). The developed OPSD formulation was characterized by using scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC), which indicated the crystalline state of fenofibrate in the OPSD. The drug release profiles were also examined at different pHs. The OPSD achieved almost complete dissolution within 15 min, while the untreated powder and physical mixture exhibited minimal dissolution (less than 10% even after 2 h). Furthermore, this formulation effectively increased the oral drug exposure in rats, as the C-max and AUC of fenofibric acid (an active metabolite) were enhanced by approximately 6-7 folds. These results suggest that the OPSD formulation should be promising for improving the oral bioavailability of fenofibrate.

• 出版日期2015-10-12