Laboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University, Gifu, Japan.
Int J Pharm. 2010 Jun 15;392(1-2):101-6. doi: 10.1016/j.ijpharm.2010.03.037. Epub 2010 Mar 20.
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.
研究了α-葡萄糖基橙皮苷（Hsp-G）提高难溶性药物溶解和生物利用度的可行性。采用喷雾干燥法制备了 Hsp-G 与氟比洛芬（FP）的喷雾干燥粉末（SDP），FP 是一种酸性药物（pK(a)=3.78），水溶性低。粉末 X 射线衍射分析表明，FP 从晶体形式转变成无定形形式，当分散在 Hsp-G 中时。FP/Hsp-G 的 SDP 显著提高了 FP 的溶解速率和溶解度。与未处理的 FP 晶体相比，当以 SDP 的形式制备在 Hsp-G 中时，FP 在盐酸溶液（pH 1.2）中的表观溶解度提高了 10 倍。将制备的 SDP 口服给予大鼠后，与未处理的 FP 晶体进行了体内生物利用度评估。结果表明，口服 FP/Hsp-G 的 SDP 后，C(max)和 AUC 值分别提高了 2.5 倍和 2.8 倍。总之，Hsp-G 是一种有潜力的安全材料，可以提高难溶性药物的溶解和吸收。
