吲达帕胺结肠定位释药微球的制备及其体外释放度考察  

Preparation and release in vitro of indapamide colon-specific microspheres

作　　者：赵智卉[1,2] 赵志娟[2] 韩荣荣[2] 郭海丽[2] 

机构地区：[1]山西长治医学院附属和平医院,山西长治0460001 [2]山西医科大学药学院药剂学教研室,山西太原030001

出　　处：《中国医院药学杂志》2015年第23期2118-2122,共5页Chinese Journal of Hospital Pharmacy

基　　金：山西省自然科学基金(编号:2008011077-3);太原市科技创新项目(编号:110148091)

摘　　要：目的：以羟丙甲基纤维素琥珀酸酯（HAS）为载体材料制备吲达帕胺结肠定位释药微球并考察其体外释放度。方法：根据球晶造粒技术,采用乳化溶剂扩散法制备微球,以收率、载药量、包封率为优化指标,对影响微球制备的因素进行正交试验,通过神经网络遗传算法优选处方及工艺,并对以优化方案制备的微球进行了质量评价。结果：制备的吲达帕胺结肠定位释药微球形态圆整,大小均匀、表面光滑,粒径在50～250μm范围的微球占到92.07%,载药量为15.30%,包封率为95.48%;体外释药试验中,微球在模拟全胃肠不同pH条件下,即先在pH1.2和pH6.8介质中5 h累计释药17.54%,继在pH7.8介质中7 h后累积释药99.75%。结论：本试验筛选的处方及制备工艺可用于制备吲达帕胺结肠微球,且制备的微球能达到结肠定位释药的目的。OBJECTIVE To prepare indapamide colon-specific microspheres with carrier material of hydroxypropyl methylcellulose acetate succinate（HAS）and investigate its release in vitro.METHODS According to spherical crystallization technique,colon-specific microspheres of indapamide were prepared by emulsion solvent diffusion method.Quality indicators included recovery,particle size,drug load and entrapment rate.Factors affecting preparation process were optimized by orthogonal experimental design,and optimal prescription was achieved by NSGA-Ⅱand BPNN design.The best process validation test of indapamide microspheres were investigated.RESULTS Indapamide colon-specific microspheres were spherical,equal and regular,and microspheres of 50 ～ 250μm occupied 92.07%.Drug loading capacity and efficiency were found to be 15.30%and 95.48%.Under simulated conditions of gastrointestinal tract in different pH values,release in vitro results showed an accumulated dissolution rate of 17.54%in pH6.8 and pH1.2 solution medium for 5h,then an accumulated dissolution rate of99.75%in pH7.8 solution medium for 7 h.CONCLUSION The present method is suitable for indapamide colon-specific microspheres,and agents can achieve the purpose of colon specific release.

关 键 词：吲达帕胺 羟丙基纤维素琥珀酸酯 微球 球晶造粒技术 释放度 

分 类 号：R944.9[医药卫生—药剂学]