葛根黄酮胃肠道黏附漂浮颗粒的制备

目的 制备葛根黄酮胃肠道黏附漂浮颗粒,考察其体外黏附性、漂浮性及其Caco-2透膜吸收.方法 用挤出滚圆造粒机制备葛根黄酮胃肠道黏附漂浮颗粒,通过组织留存量法和直接观察法分别评价其体外黏附性和漂浮性,以Caco-2细胞模型考察其透膜吸收.结果 葛根黄酮胃肠道黏附漂浮颗粒收率为59.60％,黏附性达到71.43％,立即漂浮,持续漂浮时间为15min,且与原料药相比,其透膜吸收提高9.3倍.结论 本研究制备的葛根黄酮胃肠道黏附漂浮颗粒具有良好的黏附性和漂浮性,能够增加药物在Caco-2细胞的透膜吸收,为体内吸收研究提供了依据.

Preparation of Gastrointestinal Bioadhesive and Floating Pellets for Pueraria Flavonoids

Objective Gastrointestinal bio-adhesive and floating pellets loaded with Pueraria Flavonoids were prepared to investigate the in vitro muco-adhesivity,floatability and membrane permeability across Caco-2 cells.Methods Extrusion-spheronization was used to prepare the pellets.The muco-adhesivity and floatability were evaluated by quantifying the remained percentage of pellets in stomach tissue and visual observation.The membrane permeability of the pellets was characterized on the model of Caco-2 cells.Results The yield of gastrointestinal bio-adhesive and floating pellets was 59.60％.The remaining percentage of pellets in the stomach tissue was 71.43％.The pellets floated immediately after loading to hydrochloric acid and maintained for 15 min.The membrane permeability of the drug has been improved 9.3 times relative to the raw drug.Conclusion The gastrointestinal bioadhesive and floating pellets prepared in this study have been proved to have good bioadhesivity and floatability,the improved permeability across Caco-2 cell membrane provides a basis to correlate with further in vivo absorption studies.