OBJECTIVE: To prepare Rabeprazole sodium enteric-coated pellets. METHODS: Extrusion-spheronisation and air-flow coating method were used to prepare Rabeprazole sodium enteric-coated pellets. Using angle of repose, yield and release rate as index, the amount of microcrystalline cellulose, mannitol and lactose, the concentration of polyethylene glycol 6000 (PEG 6000) solution as factors, the formulation of pellet core was optimized by orthogonal test. The weight gain of isolated layer coating was screened using content and release rate as index; that of enteric layer was screened using acid resistance and release rate as index. The optimal formulation was validated, and prepared pellet was compared with commercial enteric-coated tablet and ?capsule in respects of acid resistance and release rate. RESULTS: The optimal formulation of pellet core was as follows as microcrystalline cellulose 30%, mannitol 20%, lactose 15%, PEG6000 solution 15%, rabeprazole sodium 10%, weight gain of isolated layer 10%, weight gain of enteric-coated layer 10%. The angle of repose, yield, content, acid resistance and 30 min release rate of 3 batches of samples were 16.93-17.17 °, 65.24%-67.36%, 96.7%-99.9%, 99.66%-99.85% and 90.13%-93.62%, respectively. The acid resistance of sample was similar to that of commercial enteric-coated tablet and capsule, and release rate of sample was in between them. CONCLUSIONS: Rabeprazole sodium enteric-coated pellets are prepared successfully, they are stable and controllabe in quality and simple in preparation technology.
关键词
雷贝拉唑钠肠溶微丸挤出滚圆-流化床包衣正交试验
Keywords
Rabeprazole sodiumEnteric-coated pelletsExtrusion-spheronisation and air-flow coating methodOrthogonal test