Improvement of dissolution and absorption properties of poorly water-soluble drug by preparing spray-dried powders with alpha-glucosyl hesperidin.

The feasibility of alpha-glucosyl hesperidin (Hsp-G) to improve the dissolution and bioavailability of poorly water-soluble drug was investigated. A spray-dried powder (SDP) of Hsp-G and flurbiprofen (FP), an acidic drug (pK(a)=3.78) with low water solubility, was prepared by a spray-drying method. Powder X-ray diffraction analysis revealed the conversion of FP from the crystal to the amorphous form when dispersed in Hsp-G. The SDPs of FP/Hsp-G resulted in pronounced improvement in both the dissolution rate and solubility of FP. The apparent solubility of FP in hydrochloric acid solution (pH 1.2) was improved by 10-fold more than untreated FP crystals when prepared as SDPs in Hsp-G. The bioavailability of FP from the prepared SDPs was evaluated in vivo after oral administration to rats, in comparison with the untreated FP crystals. The results revealed 2.5- and 2.8-fold improvement in the C(max) and AUC values, respectively, after oral administration of the SDPs of FP/Hsp-G. In conclusion, Hsp-G is a potentially safe material to enhance the dissolution and absorption of poorly water-soluble drugs. Copyright 2010 Elsevier B.V. All rights reserved.