糖醇类辅料的粉体学性质及直接压片工艺考察

目的:研究糖醇类辅料的粉体学性质、可压缩性和成型性,为糖醇类辅料在固体制剂过程中的应用提供参考。方法:选择5种常用的糖醇类辅料(赤藓糖醇、山梨糖醇、木糖醇、麦芽糖醇、甘露糖醇),测定其粉体学性质,如含水量、粒径及粒径分布、休止角、流速、松密度和振实密度等,使用XP1型感应压片机压片,采用片重差异、出片力、崩解时限、脆碎度、抗张强度等参数及其变化规律来评价糖醇类辅料的可压性和成型性。结果:5种糖醇的含水量均0.3%,赤藓糖醇的粒径最大、分布最均匀,麦芽糖醇的粒径最小、分布最不均匀。木糖醇的卡尔指数为15.68%,其他4种辅料的卡尔指数都在5%~15%,说明5种糖醇的流动性均较好。5种糖醇的片重差异都在规定的范围内。对于出片力,山梨糖醇完全可以满足生产的需求,甘露糖醇和赤藓糖醇也基本可以满足生产的需求。在5种糖醇中山梨糖醇的抗张强度最大,说明其成型性较好。不同压力下所有糖醇的崩解时限均650 s。山梨糖醇在各个压力下所制得片剂的脆碎度均1%,符合2015年版《中国药典》的要求,其他4种糖醇的脆碎度均不符合2015年版《中国药典》的要求。结论:得到了糖醇在不同压力下可压性和成型性的变化规律,在直接压片过程中不同糖醇表现出不同的优势,可为糖醇类辅料在固体制剂中的应用提供理论依据。

Investigation of Powder Properties and Direct Compression Process of Sugar Alcohols

Objective:To study on the powder properties,compressibility and moldability of sugar alcohols,and to provide reference for the application of sugar alcohols in solid preparation. Method:Five kinds of sugar alcohols were chosen,after determining the powder properties,such as water content,particle size and particle size distribution,angle of repose,flowability,bulk density and tap density,the powder was tableted at the same filling height,and the compressibility and moldability were evaluated by the tablet weight difference,ejection force,disintegration time,friability,tensile strength and their change rules as indexes. Result:The water contents of 5 kinds of sugar alcohols were below 0.3%,particle size of erythritol was maximum and particle size distribution was the most uniform,particle size of maltose alcohol was minimum and particle size distribution was the most nonuniform.The Carr index of xylitol was 15.68%,and the others were between 5%-15%,indicating that the 5 kinds of sugar alcohols had good flowability.Tablet weight variation of the 5 kinds of sugar alcohols within the prescribed limits.For the ejection force,sorbitol could meet the needs of production,mannitol and erythritol could basically meet the needs of production.Among 5 kinds of sugar alcohols,the tensile strength of sorbitol was the largest,which showed its moldability was good.The disintegration times of all sugar alcohols under different pressures were within 650 s.The friability of sorbitol at various pressures was <1%,it met the requirements of the 2015 edition of Chinese Pharmacopoeia,but friabilities of the other 4 kinds of sugar alcohols were not in accordance with the requirements of the 2015 edition of Chinese Pharmacopoeia. Conclusion:The regularity of compressibility and moldability of sugar alcohols under different pressures is obtained.Different kinds of sugar alcohols have different advantages in direct compression process,this study can provide a theoretical basis for the application of sugar alcohols in solid preparations.