Hydroxypropyl-β-cyclodextrin-based solid dispersed granules: A prospective alternative to conventional solid dispersion

Abstract

The purpose of the present study was to develop hydroxypropyl-β-cyclodextrin (HP-β-CD)-based solid dispersed granules as a superior system to solid dispersion. The solid dispersed granules and solid dispersion were compared in terms of powder property improvement, solubility increment and oral bioavailability enhancement of poorly water-soluble dexibuprofen. Solid dispersion (drug/HP-β-CD/Tween80 = 1:7:0.1, weight ratio) and solid dispersed granules (drug/HP-β-CD/Tween80/Microcrystalline cellulose = 1:7:0.1:4) were fabricated using a spray-dryer and fluid bed granulator, respectively. The HP-β-CD-based solid dispersed granules significantly improved solubility, dissolution profile and oral bioavailability of dexibuprofen compared to pure drug powder. Moreover, the solid dispersed granules maximised the oral bioavailability of dexibuprofen to the same extent as the solid dispersion. However, considerable improvements of powder and tablet properties were observed in solid dispersed granules as compared with solid dispersion. Therefore, HP-β-CD-based solid dispersed granules would be a prospective alternative to solid dispersion.

Keywords: Dexibuprofen; Fluid bed granulator; Hydroxypropyl-β-cyclodextrin; Oral bioavailability; Powder property; Solid dispersed granules.