硝苯地平包芯片的研制

Study on the preparation of nifedipine package tablet

目的:通过比较硝苯地平包芯片3种制粒方式及不同处方并考察其体外溶出与释药行为,筛选出最佳制粒方式及最优处方,以期得到与原研药Adalat相似的溶出曲线。方法:通过对比直压、干法制粒和湿法制粒3种方式制备的颗粒的流动性及溶出结果差异,选出最佳制粒方式。调整芯片崩解剂及外层片壳中羟丙基纤维素来控制硝苯地平的释放,对芯片的处方、制备工艺进行研究,以自制品的释放曲线及其与参比制剂释放行为相似因子为考察指标,筛选包芯片最优处方组成。结果:低黏度羟丙基纤维素(HPC-L)∶中黏度羟丙基纤维素(HPC-M)比例3∶1,芯片崩解剂所占质量百分比为5%,采用干法制粒工艺制得的自制片与原研溶出曲线相似。结论:自制芯片与包芯片体外溶出相似因子f2均大于50,选择干法制粒方式制粒,工艺简单,颗粒出来后可以直接利用,不需要干燥,节省人力物力,提高工作效率。

Objective： In order to obtain the similar dissolution curve of the original Adalat and screen out the best granulation method and optimal prescription,the dissolution and release behavior of Nifedipine package tablet in vitro were investigated by comparing three different granulation methods and different prescriptions.Methods： In this study,powder direct tablets,dry granulation tablets,wet granulation tablets preparation method were investigated. The best method was selected by comparing the fluidity and dissolution results. The release of Nifedipine was controlled by adjusting the disintegration of the chip and the outer shell of hydroxypropyl cellulose.And the preparation process of the tablet core was studied. The best package prescription was selected by taking the release curve of self-made products and its similarity factor release behavior as the investigation index. Results：The ratio of HPC-L and HPC-M is 3∶ 1. The disintegrant percentage of tablet core is 5%. The dissolution curves of self-made tablets prepared by the dry granulation process are similar to original tablets. Conclusion： Compared to original drugs,the similarity factors（ f2） of chips and package chips are all above 50. The final process method is dry granulation method which is simple and efficient.