双嘧达莫胃漂浮缓释微丸的研究

Study on the calcium alginate-chitosan intra-gastric floating beads of dipyridamole

目的结合固体分散技术制备双嘧达莫的褐藻酸钙-壳聚糖胃漂浮型缓释微丸（Dip-Ca-alg-cs-beads）,对其漂浮性能,包封率,体外释药性能进行考察。方法以乙基纤维素,聚丙烯酸树脂II和Eudragit RLPO为联合载体制备双嘧达莫固体分散体,粉碎后分散于添加制泡剂的褐藻酸钠溶液中,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。结果通过调节配方,微丸在人工胃液中12 h漂浮率大于90%。双嘧达莫6 h释放65%~70%,包封率85%~90%。结论运用固体分散技术可实现双嘧达莫在褐藻酸钙-壳聚糖胃漂浮微丸（Ca-alg-cs-beads）中的缓释,并为这类药物的多单元胃漂浮给药系统的发展提供了思路。

Objective To prepare calcium alginate-chitosan intra-gastric floating beads of dipyridamole 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 dipyridamole was prepared by the combined carrier of the Ethylcellulose（EC）,Polyacrylic Resin Ⅱ（PRⅡ） and Eudragit RLPO.Sodium alginate solution mixed with the powder of the solid dispersion of dipyridamole and frother was slowly dripped into chitosan-calcium chloride solution added with acetic acid.Calcium alginate-chitosan intra-gastric floating beads of dipyridamole were obtained after drying.The effects of solid dispersion on in vitro release of dipyridamole were investigated.Results By the regulation of the formulation,more than 90% of the beads kept floating in artificial gastric juice in 12 h,the release ratio of dipyridamole during 6 h was 65%~70% and the entrapment efficiency was above 85%.Conclusion The sustained release of dipyridamole in the calcium alginate-chitosan intra-gastric floating beads could be achieved by using the solid dispersion method,it provide some ideas of intra-gastric floating preparations for this kind of drugs.