青藤碱结肠给药微球的设计及体外释放研究  

Design and in Vitro Release of Chitosan Microspheres Containing Sinomenine for Colonic Drug Delivery

作　　者：田亮[1] 徐珊珊[1] 薛洁[1] 朱丽敏 胡欢 Tian Liang;Xu Shanshan;Xue Jie;Zhu Limin;Hu Huan(Shanghai Neuromedical Center, The Ninth Clinical Medicine School of Qingdao University, Shanghai, China 200331;Shanghai Punan Hospital of Pudong New District, Shanghai, China 200125)

机构地区：[1]上海德济医院.青岛大学第九临床医学院,上海200331 [2]上海市浦东新区浦南医院,上海200125

出　　处：《中国药业》2018年第10期8-11,共4页China Pharmaceuticals

摘　　要：目的以壳聚糖为囊材,丙烯酸树脂为包衣制备结肠释药微球,并评价其体外释药性能。方法采用乳化交联法制备青藤碱壳聚糖微球,以粒径分布、载药量、包封率为考察指标,采用正交设计试验优化其制备工艺;将最佳工艺制备的微球用乳化干燥法包裹丙烯酸树脂肠衣,对所制得微球采用扫描电镜观察形态,并在模拟体内消化道实时pH变化环境下测试其体外释放能力。结果制备的包肠衣载药微球在电镜下观察,呈球形,包衣均匀,粒径分布适宜,微球平均粒径为(23.51±7.12)μm,平均包封率为(75.11±1.76)%;微球在pH动态药物释放中,前3 h人工胃液(pH=1.2)和胃肠混合液(pH=4.5)不释药,在人工肠液(pH=6.8)2 h释药小于7%,在人工大肠液(pH=7.4)24 h释药接近60%,而在含大鼠结肠内容物中24 h释药可达70%。结论按此优化处方及工艺制备、用丙烯酸树脂包衣的青藤碱壳聚糖微球具有良好的形态和包封率,并符合结肠释药的要求,为进一步研究奠定了基础。Objective To prepare the colon drug delivery microspheres with chitosan as carrier and acrylic resin as coating material,and to evaluate their release properties in vitro. Methods Chitosan microspheres containing sinomenine emulsion was prepared by emulsion cross-linking method. The particle size distribution,drug loading,entrapment efficiency were taken as indicators,the orthogonal experimental design was used to optimize preparation. The microspheres prepared by the best process were encapsulated acrylic resin casing by emulsion drying method,and the morphology of prepared microspheres were observe by scanning electron microscopy,and the release properties in vitro were tested under pH real-time change of in the simulation digestive tract. Results The coated microspheres were observed by electron microscopy,they were spherical with coated uniformly,and the particle size distribution was suitable. The average diameter of the microspheres was（ 23. 51 ± 7. 12） μm and the average entrapment efficiency was（ 75. 11 ± 1. 76） %. No release of sinomenine from the microspheres was observed in the artificial gastric juice（ pH = 1. 2） and in the artificial intestinal juice（ pH = 4. 5）in the former 3 h,the release of sinomenine in artificial intestinal juice（ pH = 6. 8） was less than 7% in 2 h,and the release of drug in artificial colon juice（ pH = 7. 4） was close to 60% in 24 h,and the release in juice containing rat colon contents could reach 70%in 24 h. Conclusion Sinomenine chitosan microspheres prepared by the optimized formulation and technology and coated with acrylic resin have good morphology and encapsulation efficiency,which can conform to the requirements of colon-specific drug delivery,and lay a foundation for further research.

关 键 词：青藤碱 结肠释药系统 壳聚糖 丙烯酸树脂 微球 体外释放 

分 类 号：R965.2[医药卫生—药理学] R979.5[医药卫生—药学]