挤出滚圆法制备盐酸多西环素肠溶微丸

The Preparation of Doxycycline Hydrochloride Intestinal Soluble Pellets by Extrusion/Spheronization Technology

目的应用挤出滚圆法及包衣锅包衣制备盐酸多西环素肠溶微丸,并对其性质进行考察。方法用挤出滚圆法制备了盐酸多西环素微丸,采用单因素考察和L9(34)正交设计筛选最优处方和工艺条件,再用包衣锅将微丸包肠溶衣,考察了微丸的粉体学性质及不同包衣增重微丸的体外释放情况。结果制得的盐酸多西环素肠溶微丸圆整度好,大小均匀,收率高。15%包衣增重的微丸在0.1 mol·L-1盐酸释放度<10%,在pH6.8的缓冲液中释放度>80%,体外释放较理想。结论该法制备工艺简单易行,重复性好,采用适当的包衣工艺,制得的盐酸多西环素肠溶微丸具备较理想的肠溶特征。

Objective To prepare doxycycline hydrochloride pellets by extrusion/spheronization technology and determine the pellets＇ properties. Methods Doxycycline hydrochloride pellets were prepared by using extrusion/spheronization.Influenitial factors and L9（34）orthogonal design was used to obtain optimal formulation.The pellets were coated with enteric coats by using the coated pot equipment.The micromeritic properties and in vitro dissolution of the pellets were determined. Results Doxycycline hydrochloride pellets obtained by extrusion/spheronization were round,smooth,even and on high-yield.The release rate of the pellets coating weight at 15%,is lower 10% in the 0.1 mol·L-1 HCl,while in buffer solution（pH 6.8）their release rate is over 80%.The dissolution test in vitro from the coated pellets was perfect. Conclusion The process is easy and repeatable.The produced doxycycline hydrochloride pellets have an excellent intestinal solubility by a proper coating.