柚皮素胃漂浮微丸研究

Study on Intra-gastric Floating Beads of Naringenin

目的:结合固体分散技术制备柚皮素的海藻酸钙胃漂浮微丸,考察其漂浮率、包封率及体外释放。方法:以Eudragit RLPO为载体材料制备柚皮素固体分散体,粉碎后分散于添加制泡剂的海藻酸钠溶液中,并缓慢滴入添加醋酸的壳聚糖-氯化钙溶液中反应固化,干燥后得到胃漂浮缓释微丸。考察固体分散体对微丸体外释药的影响。结果:成功制备了柚皮素胃漂浮微丸,其在人工胃液中9 h漂浮率大于70%,包封率70%～80%。9 h释放柚皮素65%～70%。结论:运用固体分散技术提高了柚皮素的海藻酸钙胃漂浮微丸在人工胃液中的释放,为多单元胃漂浮给药系统发展提供了思路。

Objective：To prepare calcium alginate-chitosan intra-gastric floating beads of naringenin combining with the solid dispersion method and investigate the in vitro floating characteristics,entrapment efficiency and drug release property of the beads.Methods：The solid dispersion of naringenin was prepared by the Eudragit RLPO.Sodium alginate solution mixed with the powder of the solid dispersion of naringenin and frother was slowly dripped into chitosan-calcium chloride solution added with acetic acid.Calcium alginate-chitosan intra-gastric floating beads of naringenin were obtained after drying.The effects of solid dispersion on in vitro release of naringenin were investigated.Results：Intra-gastric floating beads of naringenin were acquired successfully.More than 70% of the beads kept floating in artificial gastric juice in 9 h,the release ratio of naringenin during 9 h was 65%~70% and the entrapment efficiency was about 70%~80%.Conclusion：The sustained release of naringenin in the calcium alginate-chitosan intra-gastric floating beads could be achieved by using the solid dispersion method and it provides some ideas of intra-gastric floating preparations.