右旋兰索拉唑脉冲肠溶胶囊的制备

Preparation of Dexlansoprazole Pulse Enteric Capsules

采用流化床包衣技术对微晶纤维素丸芯分别进行上药层、隔离层和肠溶层包衣,制备了两种在肠内释放速率不同的微丸(微丸A和微丸B),再按照一定比例装入胶囊,制成右旋兰索拉唑脉冲肠溶胶囊。以主药释放度为考察指标,采用单因素法优化隔离层增重,微丸A的肠溶层增重以及微丸B的肠溶层包衣液组成、增塑剂种类和包衣增重。结果表明,在隔离层增重15%,微丸A的肠溶材料采用Eudragit L30D-55、增重为40%,微丸B的肠溶材料采用Eudragit S100、加入10%枸橼酸三乙酯做增塑剂、增重为50%的条件下,能制得在酸中2 h基本不释药、在p H 7.0磷酸盐缓冲液中1 h和4 h分别基本释放完全的微丸A和微丸B。将微丸A和微丸B按照主药含量25%∶75%的比例混合,装入2号胶囊壳,所得胶囊与市售胶囊体外释药行为基本一致。

The microcrystalline cellulose pellets were coated with drug layer, isolating layer and enteric layer in sequence by fl uidized bed coating method. Two kinds of enteric pellets with different drug release behaviors in simulated enteric liquid were obtained, named as pellets A and pellets B. Then the two kinds of enteric pellets were mixed in a certain proportion followed by fi lling into the capsules to obtain the title capsules. The weight gain of isolating layer and enteric coating layer of pellets A, the composition, plasticizer type and weight gain of the enteric coating layer of pellets B were optimized by single factor test with the drug release as an index. The results showed that the isolating layer with weight gain of 15% could prevent the reaction between dexlansoprazole and the enteric materials. The pellets A with Eudragit L30D-55 and weight gain of 40% could completely release the drug within 1 h in p H 7.0 phosphate buffer. The pellets B with Eudragit S100 as a enteric material, 10% triethyl citrate as a plasticizer and weight gain of 50%could completely release within 4 h in p H 7.0 medium. Moreover, both two kinds of pellets did not release in 0.1 mol/L hydrochloric acid within 2 h. Finally, pellets A and pellets B were mixed in a proportion of 25%∶75% according to the drug content, then the mixture were fi lled into 2# capsule shells. The drug release behavior from the fi nal product was similar to that of the commercial capsules.