摘要
Abstract
OBJECTIVE:To prepare cyclobenzaprine hydrochloride extended-release pellets,and to investigate its release rate in vitro. METHODS:The core pellets were prepared by fluid bed coating technology,and sustained-release pellets were prepared using Surelease® aqueous dispersion as sustained-release coating film material. Box-Behnken response surface methodology was used to optimize inlet air temperature,atomization pressure and liquid feed rate using coating time,coating efficiency and pellets adhesion rate as dependent variables. The release rate of prepared pellets and commercially available pellets(AMRIX®)in different mediums(water,pH 1.2 hydrochloric acid solution,pH 4.5 acetate buffer solution,6.8 phosphate buffer solution)were compared by f2 similarity factor. RESULTS:The weight gain of coating material was 7%;inlet air temperature was 55 ℃;atomization pres-sure was 0.36 MPa;liquid feed rate was 12.5 ml/min. The relative error of coating time [(47.1 ± 2.1) min],coating efficiency [(88.4±1.6)%] and pellets adhesion rate [(2.7±0.3)%] to corresponding predicted value(44.5 min,90.0%,2.9%)were 5.8%, 1.8%,6.9%,respectively. The f2 for prepared pellets and commercially available pellets in 4 kinds of medium were 77.7,85.9, 83.5,84.6,respectively. CONCLUSIONS:Cyclobenzaprine hydrochloride sustained-release pellets have been prepared,and have good drug release in vitro.关键词
盐酸环苯扎林/缓释微丸/体外释放度/Box-Behnken响应面法/包衣工艺/优化Key words
Cyclobenzaprine hydrochloride/Sustained-release pellets/Release rate in vitro/Box-Behnken response surface methodology/Coating technology/Optimization分类
医药卫生
