盐酸可乐定脉冲释药微丸的制备工艺研究

Study on Preparation Process of Clonidine Hydrochloride Pulsatile Release Pellets

目的研究盐酸可乐定脉冲释药微丸的制备方法。方法采用挤出-滚圆工艺和流化床包衣法制备,用正交试验设计优化处方,考察产品的体外释放度。结果各考察因素均对药物的释放影响显著。优选工艺结果为,含药丸芯采用微晶纤维素,溶胀层材料采用低取代羟丙纤维素,控释层采用乙基纤维素水分散体,溶胀层和控释层包衣增重分别为10%和15%。制备的微丸时滞时间为4.2 h左右,时滞后1 h内累积释药百分率达到90%。结论盐酸可乐定微丸在体外具有有脉冲释药特性。

Objective To study the preparation of Clonidine Hydrochloride Pulsatile Release Pellets and its in vitro dissolution. Methods Clonidine Hydrochloride Pulsatile Release Pellets was prepared with extrusion-spheronization and fluidized bed coating technology. The formulation was optimized by orthogonal design. The in vitro release of the pellets was determined. Results The drug release was strikingly influenced by various investigation factors. The optimal technology was as follows with microcrystalline cellulose as the pill core containing drug, low-substituted hydroxypropylcellulose for the swelling layer and ethylcellulose aqueous dispersion（surelease） for outer controlled-release layer with 10% and 15% weight increment of coating in swelling layer and controlled-release layer respective- ly. The lag time of prepared pellets was about 4.2 h and the accumulative release rate reached 90% within 1 h. Conclusion Clonidine Hydroehloride Pulsatile Release Pellets has the pulsatile drugrelease characteristic in vitro.