摘要
基于质量源于设计(QbD)理念优化淫羊藿素-薏苡仁油微乳(IC-MEs)的处方配比及制备工艺。采用水滴定法制备IC-MEs。评估可能影响IC-MEs质量的风险因素,采用Plackett-Burman设计筛选影响处方及工艺的显著性参数,并通过Box-Behnken设计优化IC-MEs的处方配比。风险评估和Plackett-Burman试验确定了药辅比、混合油相(薏苡仁油-甘油三丁酸酯)与混合表面活性剂(HS15-RH40)的比例、加水量3个处方因素为影响IC-MEs的关键因素。Box-Behnken设计建立的回归模型具有良好预测性,并确定IC-MEs的最佳处方为药辅比为0.92%,混合油相(薏苡仁油-甘油三丁酸酯)与混合表面活性剂(HS15-RH40)的比例为4∶6,加水量为5.7 mL。经试验验证,最佳制剂处方1周后的包封率为92.45%±1.00%。基于QbD理念优化的IC-MEs处方及工艺参数,有助于提高IC-MEs的质量稳定性,为其今后的开发应用提供了实验基础。
To optimize the formulation and preparation process of icaritin-coix seed oil microemulsion(IC-MEs)based on quality by design(QbD)concept.IC-MEs were prepared by water titration.Firstly,the risk factors that may affect the quality of IC-MEs were evaluated.Then Plackett-Burman design was used to screen out prescription factors and process parameters that had a significant effect on the indicators.Finally,Box-Behnken design was used to optimize the prescription ratio of IC-MEs.Through the risk assessment and Plackett-Burman design,three formulation factors[drug loading efficiency,the ratio of mixed-oil(coix seed oil-Glycerol tributyrate)to mixed-surfactant(HS15-RH40)and water addition]were determined as the key factors affecting IC-MEs.The regression model established by Box-Behnken design had a good predictability.The optimal formula was as following:the drug loading efficiency of 0.92%,the ratio of mixed-oil(coix seed oil-glycerol tributyrate)to mixed-surfactant(HS15-RH40)of 4∶6,and the water addition of 5.7 mL.According to this prescription,IC-MEs were prepared,and its encapsulation efficiency after 1 week was 92.45%±1.00%.Therefore,the stability of IC-MEs could be improved by optimizing prescription and process parameters of IC-MEs based on the QbD concept,which can provide certain reference value for the future development of IC-MEs.
作者
曾华婷
郭健
刘聪燕
许婷
李瑞云
陈彦
ZENG Hua-ting;GUO Jian;LIU Cong-yan;XU Ting;LI Rui-yun;CHEN Yan(Affiliated Hospital of Integrated Traditional Chinese and Wextern Medicine,Nanjing Unixersity of Chinese Medicine,Nanjing 210028,China;Multi-component of Traditional Chinese Medicine and Microecology Research Center,Jiangsus Prouincial Acadeny of Chirnese Medicine,Nanjing 210028,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2020年第16期3844-3851,共8页
China Journal of Chinese Materia Medica
基金
国家自然科学基金项目(81873016)
江苏省科教强卫医学重点人才项目(ZDRCA2016036)。
