正交试验优选阿魏酸钠片粉末直压处方

Formulation Optimization of Sodium Ferulate Powder Directly-compressed Tablets by Orthogonal Experiment

目的:优选阿魏酸钠片粉末直接压片法处方,解决主药含量下降、片面易变色等湿法制粒工艺常见的问题。方法:采用粉末直接压片法制备阿魏酸钠片,用正交试验设计方法,以休止角、脆碎度及溶出度为指标筛选处方中乳糖、低取代羟丙基纤维素、硬脂酸镁的所占比例,并考察所得样品的片重差异、含量均匀度等相关指标及稳定性。结果:最佳制备处方中乳糖、低取代羟丙基纤维素、硬脂酸镁的所占比例分别为10.0%、3.0%、0.2%。3批样品的休止角分别为38.2°、39.7°、38.4°,脆碎度均为0.2%,溶出度分别为96.4%、96.7%、96.1%。所筛选处方粉末流动性好,片重差异、含量均匀度等指标均符合2010年版《中国药典》的相关规定。样品经6个月加速试验和室温长期留样考察,外观、含量、有关物质及溶出度均未发生明显变化。结论:优选的处方经济、操作简便,制备的阿魏酸钠片质量稳定、稳定性良好,适合工业化生产。

OBJECTIVE： To optimize the formulation of sodium ferulate powder directly-compressed tablets, and to deal with the common problems of wet granulation process, such as declining in the main drug content and the surface color of the tablet changing easily. METHODS： Sodium ferulate tablets were prepared by direct powder compression method. By orthogonal experimental design method, the proportion of lactose, low-substituted hydroxypropyl cellulose, magnesium stearate were screened with the angle of repose, friability and dissolution as indicators, and the piece weight variation of sample, content uniformity and other indicators were investigated. RESULTS： The optimal formulation included proportion of lactose, low-substituted hydroxypropyl cellulose, magnesium stearate were 10.0%, 3.0%, 0.2%. The angle of repose for 3 batches of samples were 38.2°, 39.7°, 38.4°; friability was 0.2%; dissolution were 96.4%, 96.7% and 96.1%, respectively. Screened formulation powder had good fluidity, and tablet weight differences, content uniformity degree and other indicators were in line with Chinese Pharmacopoeia （2010 edition）. After 6 months of accelerated test and room temperature retention samples investigation, appearance, content, related substances and dissolution degrees were not changed significantly. CONCLUSIONS： The preferred formulation is economical and simple in operation, and prepared sodium ferulate tablets are stable in quality with good stability, which are suitable for industrial production.