Zeng Hua-Ting, Guo Jian, Liu Cong-Yan, Xu Ting, Li Rui-Yun, Chen Yan
Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine Nanjing 210028, China Multi-component of Traditional Chinese Medicine and Microecology Research Center,Jiangsu Provincial Academy of Chinese Medicine Nanjing 210028, China.
Multi-component of Traditional Chinese Medicine and Microecology Research Center,Jiangsu Provincial Academy of Chinese Medicine Nanjing 210028, China.
Zhongguo Zhong Yao Za Zhi. 2020 Aug;45(16):3844-3851. doi: 10.19540/j.cnki.cjcmm.20200522.304.
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.
基于质量源于设计（QbD）理念优化淫羊藿苷-薏苡仁油微乳（IC-MEs）的处方及制备工艺。采用水相滴定法制备IC-MEs。首先，评估可能影响IC-MEs质量的风险因素。然后采用Plackett-Burman设计筛选出对指标有显著影响的处方因素和工艺参数。最后，采用Box-Behnken设计优化IC-MEs的处方比例。通过风险评估和Plackett-Burman设计，确定了三个处方因素[载药效率、混合油（薏苡仁油-三丁酸甘油酯）与混合表面活性剂（HS15-RH40）的比例以及加水量]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的预测性。最佳处方如下：载药效率为0.92%，混合油（薏苡仁油-三丁酸甘油酯）与混合表面活性剂（HS15-RH40）的比例为4∶6，加水量为5.7 mL。按照该处方制备IC-MEs，其1周后的包封率为92.45%±1.00%。因此，基于QbD理念优化IC-MEs的处方和工艺参数可提高其稳定性，为IC-MEs的后续开发提供一定参考价值。
