新型直压辅料的粉体学性质评价

目的:考察新型直压辅料的粉体学性质,为粉末直接压片技术中辅料的筛选提供参考。方法:以新型直压辅料的粒径分布、吸湿性、润湿性、流动性、可压性和润滑敏感度等为考察指标,初步评价7种新型直压辅料(直压型微晶纤维素AvicelPH101、AvicelPH102,喷雾干燥乳糖FastFlo316、Flowlac100,预混辅料LubriToseSD、Cellactose80,预胶化淀粉)的粉体学性质、稀释潜力及在粉末直接压片中的应用情况。结果:Cellactose80的粒径分布、流动性较好,抗张强度最大;Flowlac100的流动性最大;FastFlo316的流动性大,吸湿性小,润滑敏感度低,但出片力大;AvicelPH101、AvicelPH102可压性好,流动性不及喷雾干燥乳糖,且润滑敏感度高,不宜单独作为直接压片的辅料;LubriToseSD具有极好的流动性、可压性以及较好的自润滑能力;预胶化淀粉可压性较差,但流动性好,适合于黏性大、崩解时间长的物料的压片。结论:新型直压辅料具有很好的流动性和可压性,扩大了粉末直接压片辅料筛选范围,增加了粉末直接压片技术应用的可行性。

Micromeritics Evaluation of New Direct Compression Excipients

OBJECTIVE： To investigate micromeritics properties of new direct compression excipients, and to provide refer- ence for the selection of excipients in powder direct compression technology. METHODS： New direct compression excipients were evaluated with the distribution of particle size, hygroscopicity, wettability, fluidity, compressibility and lubricating sensitivity as in- dex. Micromeritics properties and dilution potential of 7 kinds of direct compression excipieuts （direct compression avicel as Av- icelPH101 and AvicelPH102, spray-dried lactose as FastFlo316 and Flowlacl00, premixing excipients as LubriToseSD and Celiac- tose-80, Pregelatinized starch） and the application of them in the direct pressure technology were all investigated. RESULTS： Mi- cromeritic properties of Cellactose-80 showed good distribution of particle size and fluidity, and maximum tensile strength; Flow- lac 100 had maximum fluidity; FastFlo316 had better fluidity, low hygroscopicity and lubrication sensitivity, but big ejection force; AvicelPH101 and AvicelPH102 had better compressibility and high lubrication sensitivity, but fluidity of them were not as good as spray-dried lactose, they could not be used as direct compression excipients alone; LubriToseSD had excellent fluidity, compress- ibility and good self-lubricating ability; pregelatinized starch had good fluidity but poor compressibility, so it was suitable for the compression of material which had high viscosity and long disintegration time. CONCLUSIONS： New direct compression excipi- ents have excellent liquidity and compressibility, They expand the selection scope of direct compression excipients, and enhance the feasibility of powder direct compression technology.