离心造粒法制备盐酸坦索罗辛缓释微丸胶囊的工艺影响因素及体外释放度考察

Preparation Technology Factors of Tamsulosin Hydrochloride Sustained-release Pellets Capsules by Centrifugal Granulator and Drug Release Behavior of It in Vitro

目的:制备盐酸坦索罗辛缓释微丸。方法:采用离心造粒粉末层积法制备盐酸坦索罗辛微丸。通过考察主机转速、喷浆泵转速、供粉速度、喷枪雾化条件、抛光时间、包衣增重对微囊收率的影响,确定各因素较佳水平;制备微晶纤维素空白丸芯和盐酸坦索罗辛含药微丸,并在此基础上进行丙烯酸树脂水分散体包衣,对包衣微丸的释药特征进行探讨。结果:微丸成丸的最佳工艺参数为主机转速200r·min-1,喷浆泵转速20r·min-1,供粉速度50r·min-1,喷气压力0.5MPa,喷气流量10～15L·min-1,抛光时间5min,包衣增重11%。3批样品经放大试验,测得微晶纤维素空白丸芯、含药微丸、包衣微丸的收率分别是97.5%、95.4%、96.8%。缓释微丸胶囊体外释药行为较好地符合零级方程。结论:采用离心造粒法在优化的工艺条件下可制得符合要求的盐酸坦索罗辛缓释微丸。

OBJECTIVE： To prepare Tamsulosin hydrochloride sustained-release pellets capsules. METHODS： Tamsulosin hydrochloride sustained-release pellets were prepared by means of powder layering with centrifugal granulation equipment. The effects of the speed of host turntable and spray pump, powder supply speed, atomization conditions, polishing time and the weight of coating layer on the yield of pellet capsules were investigated to confirm the optimal preparation technology factors. Microcrystalline cellulose blank core and tamsulosin hydrochloride-containing pellet were prepared. And they were coated with acrylic resins aqueous dispersion. The drug release characteristics of coated pellets were studied. RESULTS： The optimal preparation technology parameters were as follows： the rotating speed of plate was 200 r. min^-1, the rotating rate of pulp pump was 20 r. min^-1 and the speed of powder supply machine was 50 r. min^-1, the spray air pressure was 0.5 MPa, the flow rate of spray air was 10-15 L.min^-1, the polishing time was 5 min and the the weight of coating layer was 11%. The yield of microcrystalline cellulose blank core, drug-containing pellets and coated pellets in 3 batches of samples were 97.5%, 95.4%, 96.8%, respectively. The release behavior of Tamsu-losin hydrochloride sustained-release pellets capsule was in line with zero-order equation. CONCLUSION： Under the optimal condition, Tamsulosin hydrochloride sustained-release pellets prepared by means of centrifugal granulator are up to the standard.