正交试验优选瑞戈非尼固体分散体的处方工艺

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英文篇名：Formula Optimization of Regorafenib Solid Dispersion by Orthogonal Test 作者：刘正平 ; 王明森 ; 李大伟 ; 孙慧娟 ; 王丽丽 ; 张新房 ; 张建强 英文作者：Liu Zhengping;Wang Mingsen;Li Dawei;Sun Huijuan;Wang Lili;Zhang Xinfang;Zhang Jianqiang;Shandong Provincial Key Laboratory of Biopharmaceuticals,Shandong Academy of Pharmaceutical Sciences;Shandong Mingren Freda Pharmaceutical Co.Ltd.;Shandong Provincial Key Laboratory of Transmucosal and Transdermal Drug Delivery Technologies,Shandong Freda Pharmaceutical Group Co.Ltd.; 关键词：瑞戈非尼 ; 固体分散体 ; 正交试验 ; 溶出度 英文关键词：Regorafenib;;Solid dispersion;;Orthogonal test;;Dissolution 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;山东明仁福瑞达制药股份有限公司;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; 出版日期：2016-06-05 出版单位：中国药师 年：2016 期：v.19 基金：山东省科技发展计划项目(编号:2014GZX221002) 语种：中文; 页：ZYSG201606009 页数：5 CN：06 ISSN：42-1626/R 分类号：30-34

摘要

目的:优选瑞戈非尼固体分散体的处方工艺。方法:在对瑞戈非尼固体分散体的载体及药物/载体重量比进行初步研究的基础上,采用正交试验进一步对固体分散体的处方工艺进行考察,按L9(34)正交表进行试验设计,考察药物/载体重量比、水浴温度和超声时间3个因素对溶出度及溶解度的影响。结果:采用溶剂法,以PVP K30为载体,药物/载体重量比为1∶7,超声4 min,水浴温度为30℃。通过差示扫描量热法和X-射线衍射法考察得到瑞戈非尼固体分散体的稳定性良好,30min溶出度高达90%以上。结论:该工艺稳定,重复性好,可用于瑞戈非尼固体分散体的制备。
        Objective: To optimize the formula of regorafenib solid dispersion. Methods: On the basis of preliminary studies on the carrier and drug / carrier ratio,an orthogonal test was used to study the formula of regorafenib solid dispersion. The orthogonal table of L9( 34) was designed to study the drug/carrier ratio,ultrasound time and bath temperature. Results: Regorafenib solid dispersion was prepared by a solvent method with polyvinylpyrrolidone K30 as the carrier. The drug / carrier ratio was 1 ∶ 7,the ultrasound time was 4min,and the bath temperature was 30℃. Regorafenib solid dispersion showed good stability confirmed by differential scanning calorimetry and X-ray diffraction. The dissolution in 30 min reached above 90 %. Conclusion: The preparation process is stable and reproducible,which can be used to prepare regorafenib solid dispersion.

引文

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