琥珀酸去甲文拉法辛缓释微丸胶囊的制备及微丸体外释药研究  

Study on Preparation of Desvenlafaxine Succinate Sustained-release Pellets Capsules and Drug Release in vitro of Pellets

作　　者：陈才 何芳[1] 龙锐[1] 

机构地区：[1]重庆医科大学附属第一医院药学部,重庆400016

出　　处：《中国药房》2016年第31期4436-4439,共4页China Pharmacy

摘　　要：目的：制备琥珀酸去甲文拉法辛（DVS）缓释微丸胶囊,并对微丸体外释药特性进行研究。方法：采用醇溶上药法制备DVS微丸,并进行微丸质量评价及粉体学性质研究。用乙基纤维素和羟丙甲基纤维素作为包衣材料,流化床包衣制备DVS缓释微丸,干燥后装入肠溶空心胶囊中,制得缓释微丸胶囊。考察缓释微丸的体外释药特性、不同干燥时间（1-24 h）和人工胃液对其释药的影响。结果：DVS微丸和DVS缓释微丸的膜表面均光洁、有散在分布的小孔。DVS微丸中DVS的含量为19.56%（RSD=0.53%,n=10）,上药率为94%,堆密度为0.792 1 g/ml,圆整度为7.84°,休止角为21.3°。DVS缓释微丸经不同时间干燥后的释药差异无统计学意义（P〉0.05）,经人工胃液处理3 h后累积释放度降低;DVS缓释微丸释药规律符合一级动力学过程。结论：本方法成功制成具有缓释作用的DVS缓释胶囊,且制备过程中可不进行干燥。OBJECTIVE： To prepare Desvenlafaxine succinate （DVS） sustained-release pellets capsules, and to investigate the release property in vitro of pellets. METHODS： The pellets containing DVS were prepared by alcohol solution. The quality and micromeritics of DVS pellets were studied. Using ethylcellulose （EC） and hydroxypropyl methyl cellulose （HPMC） as coating materials, DVS sustained-release pellets were prepared by fluid-bed, and then put into enteric hollow capsule. The release property in vi- tro of DVS sustained-release pellets, and the effects of different drying time （1-24 h） and artificial gastric juice on drug release were investigated. RESULTS： DVS pellets and DVS sustained-release pellets were smooth and had scattered ostiole in surface. The content of DVS in DVS pellets was 19.56% （RSD=0.53%, n= 10）, and drug-loading rate was 94%; bulk density was 0.792 1 g/ml; roundness degree was 7.84 °; angle of repose was 21.3°. There was no statistical significance in the difference of drug release for DVS sustained-release pellets after dried for different time （P〉0.05）, and accumulative release rate decreased 3 h after treated with artificial gastric juice; the release regularity of DVS sustained-release pellets fitted to first-order kinetic equation. CONCLU- SIONS： DVS sustained-release capsules are prepared successfully by this method, and can be not dried during preparation.

关 键 词：琥珀酸去甲文拉法辛 缓释微丸 流化床包衣 体外释药 制备 

分 类 号：R943[医药卫生—药剂学]