【摘要】 目的制备以氧氟沙星为主药的胃漂浮缓释微丸。方法以微晶纤维素为骨架材料,采用挤出滚圆法制备氧氟沙星微丸。以Kollicoat SR30D为内层包衣材料(缓释层),碳酸氢钠为中间层(产气层),Eudragit RL30D为外层包衣材料(阻滞层)进行包衣,制成氧氟沙星胃漂浮微丸。通过星点设计-效应面优化法考察了胃漂浮微丸的处方,分别考察各处方微丸的漂浮性和体外释放性质。结果试验制得的胃漂浮微丸既能快速起漂、持续漂浮达8 h以上,又能达到2、4、8和24 h累计释放率分别为(32.37±0.88)%、(50.18±0.37)%、(69.36±0.89)%和(97.64±0.87)%的缓释效果。结论所制得的包衣微丸在人工胃液(p H=1.2)中具有良好的漂浮性能和缓释性能。更多还原

【Abstract】 Objective To prepare the gastric floating pellets for sustained release of ofloxacin. Methods ofloxacin pellets was prepared using microcrystalline cellulose carrier by extrusion-spheronization method.The pellets of ofloxacin were firstly coated with Kollicoat SR30 D as inner layer( a release-rate controlling layer),sequentially,Na HCO3 as middle layer( effervescent layer) and Eudragit RL30 D as outer layer( gas-entrapped layer). The formulation was optimized by the central composite design-response surface method. The floating ability and In vitro drug release properties of the coated pellets were evaluated. Results The resultant gastric floating pellets could float within 5 min,maintain the buoyancy over 8 h,and exhibit a good sustained-release effect. The accumulative release of ofloxacin was about( 32. 37 ±0. 88) %,( 50. 18 ± 0. 37) %,( 69. 36 ± 0. 89) % and( 97. 64 ± 0. 87) % at 2,4,8,and 24 h,respectively. Conclusions Optimized pellets showed good floating and release properties in artificial gastric fluid( p H = 1. 2).更多还原