尼莫地平双层渗透泵片的制备及其体外释放度考察

Preparation and in Vitro Release of Nimodipine Two-layer Osmotic Pump Tablets

目的:制备尼莫地平双层渗透泵控释片,并考察其体外释放度。方法:以体外累积释放度作为评价指标,以含药层助悬剂聚氧化乙烯(PEO)200000的用量、促渗剂氯化钠的用量、致孔剂聚乙二醇(PEG)2000的含量及包衣增重为考察因素,采用正交设计优化尼莫地平双层渗透泵控释片的处方;参照《中国药典》释放度测定法第二法测定其体外释放度。结果:最优处方为含药层PEO20000080mg,氯化钠10mg,助推层PEO500000040mg,PEG2000用量8%,包衣增重8%。所制片剂释药速率恒定,12h的体外累积释放度达90%以上。结论:尼莫地平双层渗透泵片工艺稳定,体外释放行为在12h内具有明显的零级释放特征(r=0.9903),达到了控释要求。

OBJECTIVE： To prepare Nimodipine two-layer osomatic pump tablets and to study the in vitro release of it. METH- ODS： The preparation formula of Nimodipine two-layer osomatic pump tablets was optimized by orthogonal design with accumula-tive release rate as index using the amount of PEO 200000 and osmotic promoter NaC1, the content of PEG 2000 and the weight growth of coating membrane as factors. The in vitro release of preparation, was determined in accordance with the method stated in Chinese Pharmacopeia. RESULTS： The optimal formula was as follows： PEO 200000 in drug-containing layer of 80 mg, NaC1 of 10 mg, PEO 5000000 in push layer of 40 mg, PEG 2000 of 8%, weight gain for coating membrane of 8%. The release rate was constant, the accumulative release rate was above 90% in 12 h. CONCLUSION： The preparation of Nimodipine two-layer osomat-ic pump tablets is stable, and the in vitro drug release shows excellent zero-release profile within 12 h （r=0.990 3）, and in line with controlled requirements.