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采用挤出滚圆法,以壳聚糖为骨架黏附材料,十八醇为漂浮材料,制备菠萝叶提取物(Bolo leaf phenols,BLP)黏附漂浮微丸,评价其体外黏附性、漂浮性及体内滞留情况,并考察药物的体外释放特性。通过体外组织留存量法和直接观察法分别评价微丸的体外黏附性和漂浮性;采用体内组织留存量法和小动物活体成像法考察微丸在大鼠体内的滞留情况;对微丸中指标成分对香豆酸和咖啡酸的体外释放情况进行评价。结果显示,制备的黏附漂浮微丸体外黏附性达(73.2±3.4)%,在人工胃液中可立即起漂,持续漂浮时间在12 h以上;黏附漂浮微丸在大鼠胃内6 h时滞留率达40%以上,而普通参比微丸胃滞留率低于15%,两者相比,滞留效果具有显著性差异(P<0.01);药物体外释放时间可达6 h以上,体外释药机制符合Higuchi方程。体内、外研究表明,制备的BLP黏附漂浮微丸具有良好的胃滞留效果和缓释特性。
Using the method of extrusion-spheronization, chitosan as the matrix adherent material and octadecyl alcohol as the floating material, the floating pellets were prepared by bolo leaf phenols (BLP), and their adhesion, floating and in vivo retention Situation, and examine the drug’s in vitro release characteristics. The in vitro adhesion and flotation of the pellets were evaluated by the method of in vitro tissue retention and direct observation respectively. The retention of pellets in vivo was evaluated by the method of in vivo tissue retention and small animal live imaging. Components in coumaric acid and caffeic acid in vitro release were evaluated. The results showed that the adhesion of floating pellets prepared in vitro (73.2 ± 3.4)% in the artificial gastric juice can be floated immediately, the sustained floating time of 12 h or more; sticky floating pellets in the rat stomach 6 h retention time (P <0.01). The drug release time in vitro was more than 6 h, and the release rate in vitro was higher than that in normal reference pellets The mechanism fits the Higuchi equation. In vitro and in vivo studies show that the prepared BLP adhesion floating pellets have good gastric retention and sustained release properties.