克拉霉素漂浮-生物粘附微囊的制备及性能研究  

Preparation and Characteristics of Floating-bioadhesive Microcapsules Containing Clarithromycin

作　　者：郑建华[1] 刘朝武[1] 包德才[1] 赵燕军[1] 马小军[1] 

机构地区：[1]中国科学院大连化学物理研究所中国科学院研究生院,大连116023

出　　处：《高等学校化学学报》2006年第6期1182-1185,共4页Chemical Journal of Chinese Universities

基　　金：中国科学院知识创新工程领域前沿项目(批准号:K2002A2);国家自然科学基金(批准号:20176056)资助

摘　　要：选用乳化-溶剂挥发法制备乙基纤维素载药微球（EMs），并通过内部凝胶化法进行包衣制得海藻酸钠．乙基纤维素载药微囊（AEMs），最后通过离子交联法进一步包衣制得壳聚糖-海藻酸钠-乙基纤维素载药微囊（CAEMs）．研究克拉霉素漂浮-生物粘附微囊的制备工艺，并考察微囊的体外漂浮性能、粘附性能及体内滞留性能．结果表明，CAEMs球形度较好，药物包封率为72．3％-78．2％，载药量为7．1％．12．7％．在pH：5的醋酸缓冲液中，6h时的累积释放率为56．6％-70．6％，漂浮率大于70％，4h时的体内滞留率为60.5％．CAEMs有望通过延长药物胃内滞留时间，在临床用于根除幽门螺旋杆菌，从而降低消化道溃疡的复发率．Floating-bioadhesive microcapsules containing clarithromycin were prepared by a combined method of emulsion solvent diffusion and internal/ion gelation for the treatment of Helicobacter pylori. Ethylcellulose microsphers（EMs） were prepared by the emulsion solvent diffusion method. EMs were coated with alginate and chitosan by the internal/ion gelation method to get alginate-ethylcellulose microcapsules（AEMs） and chitosan-alginate-ethylcellulose microcapsules（CAEMs）. The drug efficiency and drug content of clarithromycin in CAEMs were determined to be 72. 3%-78.2% and 7.1%-12. 7%, respectively. CAEMs showed an obviously sustaining effect for more than 6 h in vitro, and more than 70% of CAEMs floated in acetate buffer solution for 8 h in vitro. Furthermore, the in vitro remaining percentage of CAEMs in the stomach 4 h after the administration was 60. 5%. The results suggest that floating-bioadhesive microcapsules might be a promising drug delivery system for the treatment of Helicobacter pylori infection.

关 键 词：克拉霉素 漂浮-生物粘附微囊 体外漂浮性能 胃内滞留性能 幽门螺旋杆菌 

分 类 号：O631[理学—高分子化学] R318[理学—化学]