吗啡-壳聚糖缓释微球的制备及其体外药物释放性能研究  

Preparation and in vitro drug release performance of morphine-loaded chitosan microspheres

作　　者：李雅兰[1] 廖锦华[1] 胡冬华[1] 陈文斌[2] 周长忍[2] 鲁璐[2] 容建华[2] 

机构地区：[1]暨南大学附属第一医院麻醉科,广东广州510630 [2]暨南大学材料科学与工程系,广东广州510630

出　　处：《南方医科大学学报》2010年第3期490-493,共4页Journal of Southern Medical University

基　　金：广东省科技计划资助项目(2006B20401022)

摘　　要：目的应用乳化-离子交联法制备负载盐酸吗啡的壳聚糖微球并考察初始吗啡量和不同交联剂用量对微球载药量、包封率、体外缓释性能的影响。方法相对分子质量50000,脱乙酰度大于或等于90%的壳聚糖100mg,分别加入盐酸吗啡20、30、40、50mg溶于2%的乙酸制成20mg/ml的吗啡壳聚糖乙酸溶液作为水相,缓慢加入到15ml含0.75ml司盘80的大豆油中电动搅拌700r/min,温度35℃,乳化时间1.5小时。乳化完成后以微量注射泵缓慢滴入10mg/ml的三聚磷酸钠溶液进行交联,壳聚糖与三聚磷酸钠质量比分别为5∶1、7∶1、9∶1,交联时间2h。丙酮、无水乙醇去油干燥测定载药量、包封率和体外释放曲线。结果微球载药量随初始吗啡量的增加而增加,包封率随初始吗啡量的增加而减小,交联剂用量越大缓释作用越明显。结论制备的吗啡-壳聚糖缓释微球具有一定的缓释作用。Objective To prepare morphine-loaded chitosan microspheres by emulsion ionic cross-linking and investigate the effect of initial morphine quantity and different cross-linking degrees on drug loading, encapsulation efficiency and in vitro drug release. Methods Chitosan （with a relative molecular mass of 50 000 and deacetylation degree no less than 90%） at 100 mg and morphine at 20, 30, 40, or 50 mg were dissolved by 2% acetate and dripped slowly into 15 ml soy-bean oil containing 0.75 ml Span80. After full emulsification at 35 ℃ for 1.5 h, the mixture was dripped slowly into sodium tripolyphosphate （10 mg/ml） at the mass ratio of 5∶1, 7∶1, or 9∶1 to allow cross-linking for 2 h. The drug loading, encapsulation efficiency and in vitro drug release of the preparations were measured. Results The drug loading in the microsphere increased while the encapsulation efficiency reduced with the increment of the initial morphine quantity. High cross-linking degree resulted in prolonged release time of the drug loaded in the preparations. Conclusion The microspheres loaded with morphine allows sustained release of morphine.

关 键 词：乳化 吗啡 壳聚糖 微球 

分 类 号：R943[医药卫生—药剂学]