【摘要】 低剂量片剂最重要的考察指标为含量均匀度(CU),因此占片重绝大部分的药用辅料的性质至关重要.通过处方优化设计,着重研究了不同品牌的药用乳糖经三种压片方法处理之后的粉体性质,及其对最终压制的成片含量均匀度的影响.探讨了药物辅料、直压混合物、干/湿颗粒的粒径分布、休止角、流动性等粉体性质以及药物在混合物中的稳定性及晶型变化,并对成片进行了硬度、脆碎度、含量均匀度和体外释放的考察.结果表明:过筛/研磨乳糖湿颗粒的粉体性质使得成片含量均匀度结果普遍优于干法制粒,同时喷雾干燥乳糖湿颗粒具有最适宜的粒径分布和流动性,使得喷雾干燥乳糖湿法制粒片具有最好的含量均匀度.不同品牌性质相似的喷雾干燥乳糖所制备的成片体外溶出行为因颗粒性质的差异而有所差别.本研究所得出的一系列结论为其他低剂量处方片剂的设计提供了参考.更多还原

【Abstract】 The most important evaluation factor of low-dose tablet is content uniformity(CU),therefore the characteristics of excipients which take most part of the total materials are very crucial.Based on a optimized formulation,different pharmaceutical lactose were chosen and 3tableting methods were used.The powder/granules were studied by particle distribution,repose angle,flowability,drug stability in mixtures and crystal-form change of lactose.Tablets were evaluated by hardness/friability test,CU and in-vitro release profile.Dry-granulated sieved/milled lactose possessed powder properties for achieving better CU results while wet-granulated spray-dried lactose owned optimal particle distribution and flow ability.The release profiles were different from each other even the granules were similar in particle characteristics.These results may provide suggestion for other low-dose tablet formulation design.更多还原