目的 制备泼尼松脉冲片并考察其在体外的释放特性。方法 采用粉末直接压片法制备速释片芯, 以羟丙甲纤维素(HPMC)为溶胀层包衣材料, 以乙基纤维素(EC)为控释层包衣材料, 采用多层包衣技术制备泼尼松脉冲片。考察了致孔剂PEG 400、增塑剂PEG 6000比例与用量以及控释层包衣增重对释放的影响。以迟滞时间和累积释放度为指标, 考察泼尼松脉冲片的体外释放特性。结果 以片芯崩解剂用量为11%, 致孔剂用量为10%, 增塑剂用量为1%, 溶胀层和控释层包衣分别增重为5%、10.5%制备的泼尼松脉冲片效果最佳。按照最优处方工艺制备的泼尼松脉冲片体外释放迟滞时间为4 h, 时滞后0.5~1.0 h累积释放度达95%以上。结论 泼尼松脉冲片处方组成合理, 工艺简便可行, 体外释放特性符合脉冲释放设计要求。

Objective To prepare Prednisone Pulse-release Tablets and investigate the release characteristics in vitro. Methods Powder direct compression method was adopted to prepare quick-release tablets core. Multilayer coating were used to prepared Prednisone Pulse-release Tablets, in which hypromellose (HPMC) and ethyl cellulose (EC) were used as coating materials of the swelling layer and controlled release layer respectively. Effects of dosages and ratio of porogenic agent and plasticizer, and different weight on release were studied. Lag time and the accumulated amounts of release were used to evaluate the release characteristics in vitro. Results The optimized formulation and preparation of Prednisone Pulse-release Tablets were as following: the dosage was 11%, 10%, and 1% of the disintegrate, porogenic agent, and plasticizer. As well as, the coating weight obtained 5% and 10.5% of swelling layer and controlled release layer. The optimized lag time was 4 h and the accumulated amounts of release were more than 95% when the pulse-release time was between 0.5 h and 1.0 h. Conclusion The formulation of Prednisone Pulse-release Tablets is reasonable, the industrial arts is convenient and feasible, and the release characteristics in vitro is fit to the design of pulse-release.

天津市科技计划项目(13ZXCXSY13600)