富马酸依美斯汀缓释胶囊制备工艺与体外释放度研究

Preparation Process and in Vitro Release Rate of Emedastine Difumarate Sustained-Release Capsules

目的制备富马酸依美斯汀缓释胶囊,考察不同包衣增重对其体外释放度的影响。方法采用流化床底喷包衣工艺,以羟丙基纤维素(HPC)为致孔剂、柠檬酸三乙酯(TEC)为增塑剂、乙基纤维素(EC)为阻滞剂,制备富马酸依美斯汀缓释胶囊;采用高效液相色谱法测定其含量及体外释放度,并与参比制剂的释放度进行比较。结果与参比制剂相比,富马酸依美斯汀缓释胶囊缓释层包衣增重为12.0%,13.5%,15.0%时,体外释放曲线相似因子(f_(2))分别为69.9,89.6,74.1。结论所建立的制备工艺可行,缓释层包衣增重为13.5%时体外释放度与参比制剂基本一致。

Objective To prepare Emedastine Difumarate Sustained-Release Capsules,and to investigate the effect of different coating weight gain on its in vitro release rate.Methods The fluidized-bed bottom spray coating process was used to prepare the Emedastine Difumarate Sustained-Release Capsules with hydroxypropyl cellulose(HPC)as the pore-forming agent,triethyl citrate(TEC)as the plasticizer,and ethyl cellulose(EC)as the blocker.The high-performance liquid chromatography(HPLC)method was used to determine the content and in vitro release rate of emedastine difumarate,and its release rate was compared with that of reference preparation.Results When the coating weight gain of Emedastine Difumarate Sustained-Release Capsules was 12.0%,13.5%and 15.0%,the similarity factor(f_(2))of its in vitro release curve relative to the reference preparation was 69.9,89.6 and74.1,respectively.Conclusion The established preparation process is feasible,and Emedastine Difumarate Sustained-Release Capsules with the coating weight gain of 13.5%has the similar in vitro release rate to the reference preparation.