对乙酰氨基酚复合微囊缓释栓的制备及体外释放度研究  

Preparation of compositive sustained-release suppository of acetaminophen microcapsule and release investigation in vitro

作　　者：王磊[1] 丁四海[1] 刘秀茹[1] 牛余杰 韩翠艳[1] 

机构地区：[1]齐齐哈尔医学院药学院,黑龙江齐齐哈尔161006

出　　处：《中国医院药学杂志》2016年第9期714-718,共5页Chinese Journal of Hospital Pharmacy

基　　金：国家黑龙江省大学生创新创业训练计划项目(编号:201411230002)

摘　　要：目的:采用复凝聚法制备对乙酰氨基酚(AAP)微囊并考察其体外释药行为。制备AAP复合微囊栓剂,具有良好释放效果。方法:考察复凝聚法制备AAP微囊过程的处方和工艺因素,并进行正交试验设计,筛选出最佳条件制备AAP微囊并考察其体外释药行为。同时采用复合缓释技术(速释部分+微囊缓释)制备复合微囊缓释栓剂,考察其释药行为。结果:建立了复凝聚法制备AAP微囊方法,优化后的制备条件为:明胶阿拉伯胶囊材用量各为7g(溶液浓度7%),药物用量为8g,搅拌速度为300r·min-1,制备温度55℃。此条件制备的微囊形态圆整,粒径均匀,重复性好,包封率为(79.71±0.10)%,载药量为23.11±0.69%。微囊有缓释效果,拟合缓释方程符合一级方程。制备的复合微囊栓与普通栓剂相比,具有更好的释放效果,其中缓释过程药物释放符合Higuchi方程。结论:基于普通栓剂与复合微囊技术制备的新型AAP栓具有更佳的释药特性。OBJECTIVE To prepare acetaminophen（AAP）microcapsule by using method of complex coacervation and to study drug release from microcapsule by in vitro release experiments,and prepare composite sustained-release suppository to produce better release effects in vitro.METHODS Factors of formulation and process of complex coacervation were investigated,and orthogonal experiment was performed.Optimal conditions were screened out to prepare AAP microcapsules and investigate the in vitro release behaviors.Composite sustained-release technique（immediate-release part＋ microcapsule sustainedrelease part）was used to prepare composite microcapsule suppository and investigate release behaviors.RESULTS Reliable complex coacervation was established to prepare AAP microcapsules.Under the best conditions,microcapsule was made with79.71±0.10% encapsulation efficiency and 23.11±0.69% drug loading.AAP microcapsule was sustained-release with first order equation.Composite suppository was sustained-released with Higuchi equation in latter release phase,and drug release characters were better than common suppository.CONCLUSION Drug release characters of the composite suppository prepared by AAP microcapsule are better than those of common suppository.

关 键 词：对乙酰氨基酚 微囊 复凝聚法 复合缓释 正交试验 缓释栓 

分 类 号：R943[医药卫生—药剂学]