Formulation of solid dispersion to improve dissolution and oral bioavailability of poorly soluble dexibuprofen

Abstract

Dexibuprofen (DEXI) belongs to BCS class II drug with poor aqueous solubility resulting in poor bioavailability. To enhance solubility and bioavailability of DEXI, DEXI-loaded solid dispersion (SD) was formulated. DEXI-SDs were prepared by melting method and solvent evaporation method. Amphipathic polymer poloxamer 407 (pol 407) was selected based on solubility and dissolution tests. The ratio of DEXI:pol 407 was optimized as 1:2. The physicochemical properties, dissolution, and oral bioavailability of SD3 and SD6 were evaluated to compare preparation methods. The dissolution rate of DEXI from SD formulations was higher at pH 6.8 and pH 7.2 than at pH 1.2. Following oral administration in rats, the C_max and AUC_last of SD3 and SD6 formulations were significantly higher compared with raw DEXI. In addition, the SD6 formulation showed increased C_max and AUC_last by 1.34- and 1.33-fold, compared with those of SD3 formulation, respectively. These results demonstrated that SD formulation has excellent potential as a formulation for poorly soluble drug DEXI.

Graphical Abstract

Keywords:

• Dexibuprofen
• solid dispersion
• dissolution
• bioavailability

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This work was supported by research fund of Chungnam National University, South Korea in 2020.