包衣处方和工艺对对乙酰氨基酚缓释微丸释放度的影响

Influence of Coating Formulation and Preparation of Acetaminophen Sustained-release Pellets on the Drug Release

目的研究包衣处方和工艺对离心法制备的膜控型缓释微丸的体外释药行为的影响。方法以对乙酰氨基酚为模型药,采用BZJ-360型离心造粒包衣机以液相层积法制备含药丸芯,以微丸的体外释放度为考察指标,分别用单因素考察和正交试验的方法来探讨包衣处方、工艺因素对缓释微丸的释药特征的影响,并筛选出最佳水平,通过对药物释放度曲线的药动学模型拟合确定微丸的缓释机制。结果以丙烯酸树脂(Eudragit RS PO∶RL PO=10∶1)为包衣材料,包衣增重为10%,聚合物浓度为6%时包衣微丸在pH 6.2的磷酸盐缓冲液中呈现良好的缓释效果,释药机制主要是以膜控为主的扩散作用,骨架溶蚀也起到了一定的协同作用。结论该技术制备的对乙酰氨基酚缓释微丸包衣均匀,操作简便,质量可靠,可工业化生产。

OBJECTIVE To study the influence of coating formulation and preparation of membrane controlled release pellets on its release profile in vitro.METHODS Acetaminophen pellets were prepared by means of liquid layering with the centrifugal granulation equipment.The single factor experiments and orthogonal design were applied to optimize the formulation of coating solution and the technical parameter.The release mechanism of coated pellets was studied by fitting with different release models.RESULTS The optimal drug sustained-release was showed at the ratio of Eudragit RS PO to RL PO of 10∶1,loading weight of copolymers of 10% and polymer concentration of 6%.The drug release from coated pellets was primarily promoted by osmotic pressure and skeleton dissolution also played a certain synergy.CONCLUSION The acetaminophen membrane controlled release pellets prepared by centrifugal granulation equipment are uniformly coated,easy to be operated,which has reliable quality,and can be a industrial production.