中心复合设计-效应面法优化阿瑞匹坦纳米胶囊的处方

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英文篇名：Formula Optimization of Aprepitant Nanocapsules by Central Composite Design-response Surface Methodology 作者：王明森 ; 刘正平 ; 张菊红 ; 孙慧娟 ; 侯良玉 ; 张建强 英文作者：Wang Mingsen;Liu Zhengping;Zhang Juhong;Sun Huijuan;Hou Liangyu;Zhang Jianqiang;Shandong Provincial Key Laboratory of Biopharmaceuticals,Shandong Academy of Pharmaceutical Sciences.;Shandong Freda Pharmaceutical Group Co.Ltd,Shandong Provincial Key Laboratory of Mucosal and Transdermal Drug Delivery Technologies;Shandong Tianhao Chemical Enjnearing Design Co.ltd.; 关键词：阿瑞匹坦纳米胶囊 ; 中心复合设计 ; 效应面法 ; f_2因子 英文关键词：Aprepitant;;Central composite design;;Response surface methodology;;f_2 factor 中文刊名：ZYSG 英文刊名：China Pharmacist 机构：山东省药学科学院山东省生物药物重点实验室;山东福瑞达医药集团公司山东省黏膜与皮肤给药技术重点实验室;山东天浩工程设计有限公司; 出版日期：2018-02-05 出版单位：中国药师 年：2018 期：v.21 基金：山东省科技发展计划项目(编号:2014GZX221002) 语种：中文; 页：ZYSG201802011 页数：5 CN：02 ISSN：42-1626/R 分类号：43-47

摘要

目的:优化阿瑞匹坦纳米胶囊的处方。方法:采用中心复合设计-效应面法,以羟丙基纤维素(HPC-SL)和十二烷基硫酸钠(SDS)的用量为因素,以阿瑞匹坦在15 min、30 min的溶出度和40℃,75%相对湿度(RH)条件下加速6个月后30 min的溶出度为指标,用二次多项式模型分别描述各指标与因素的关系,绘制效应面图,各指标效应面二维等高线图的重叠部分,即为最佳处方区域,选择最佳处方,并采用f_2因子法评价体外溶出曲线的相似性。结果:二次多项式模型拟合的相关系数和可信度较高,最佳处方各指标的实测值在预期范围内。结论:采用中心复合设计-效应面法优化的阿瑞匹坦纳米胶囊符合要求,为下一步的放大生产提供了依据。
        Objective: To optimize the formula of aprepitant nanocapsules. Methods: The central composite design – response surface methodology was used. The amounts of hydroxg propyl cellulose( HPC-SL) and sodium dodecyl sulfate( SDS) were set as the independent variables; the dissolution of aprepitant capsules at 15 min and 30 min,and the dissolution after accelerated at 40℃ and 75% RH for 6 months were set as the dependent variables. Quadratic polynomial mathematic models were used to evaluate the relationship between the independent and the dependent variables. According to the mathematic models,an effect graph was drawn. The optimized formula was chosen from the overlap of the contour graphs of the dependent variables. The similarity of in vitro dissolution curve was evaluated by using f_2 factor. Results: The correlation coefficient of quadratic polynomial mathematic model and the reliability was high. The measured values of the optimized formula were within the expected ranges. Conclusion: Aprepitant nanocapsules with the optimized formula by central composite design-response surface methodology meet the requirements. The results can provide evidence for the next industrial production.

引文

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