五味子总木脂素的富集及微乳制备研究  

Enrichment of total lignans of Schisandrae Chinensis Fructus and preparation of microemulsion

作　　者：许煜晨 丁文文 赛那 刘晶[1] 尹东阁 刘曼婷 彭胡麟玥 王开心 杨玉畅 胡盼祥 倪健[1] 曲昌海[1] XU Yu-chen;DING Wen-wen;SAI Na;LIU Jing;YIN Dong-ge;LIU Man-ting;PENG Hu-linyue;WANG Kai-xin;YANG Yu-chang;HU Pan-xiang;NI Jian;QU Chang-hai(College of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 102488;College of Life Sciences,Beijing University of Chinese Medicine,Beijing 102488;College of Pharmacy,Inner Mongolia Medical University,Hohhot 010110)

机构地区：[1]北京中医药大学中药学院,北京102488 [2]北京中医药大学生命科学学院,北京102488 [3]内蒙古医科大学药学院,呼和浩特010110

出　　处：《中南药学》2022年第6期1287-1293,共7页Central South Pharmacy

基　　金：北京市自然科学基金面上项目(No.7202123)。

摘　　要：目的优化五味子的提取纯化工艺参数,得到较高含量的五味子总木脂素;并经制剂处方工艺优化,制备得到载药量高、稳定性良好的微乳制剂。方法采用回流提取、大孔树脂柱洗脱相结合的方法,对五味子木脂素成分进行富集;建立高效液相色谱法,以五味子醇甲等8种成分为指标,考察五味子提取物中总木脂素的含量,明确不同环节的成分转移率;采用超声乳化法制备五味子木脂素微乳,并通过单因素考察,对制剂处方和工艺进行研究。结果建立的8种木脂素成分同时测定的方法专属性、准确性和精密度等方法学考察均符合要求;五味子提取物总木脂素含量为60.85%,其中五味子醇甲等8种木脂素成分总含量为44.57%;以大豆油为油相,吐温-80为表面活性剂制备微乳,微乳的平均粒径为248.3 nm,平均载药量为2.44 mg·mL^(-1),pH值为6.5。结论建立的五味子提取物中8种成分同时测定方法准确可行,可用于其质量控制;提取纯化得到的总木脂素含量较高、重复性良好;制备的五味子微乳载药量较高、粒径均匀、稳定性良好,可为五味子总木脂素的进一步研究奠定基础。Objective To optimize the extraction and purification parameters of Schisandrae Chinensis Fructus to obtain a higher content of total lignans of Schisandrae Chinensis Fructus;and to prepare a microemulsion formulation with high drug loading and good stability.Methods The lignan components of Schisandrae Chinensis Fructus were enriched with the combination of reflux extraction and macroporous resin column elution.The content of lignan,and the transfer rate of components in different links were determined by HPLC.The microemulsion of Schisandra lignans was prepared by ultrasonic emulsification,and the formulation and the preparation process were studied with single factor investigation.Results The specificity,accuracy and precision of the established method for the simultaneous determination of 8 lignan components met the requirements.The total lignan content of the Schisandrae Chinensis Fructus extract prepared by the optimized extraction and purification was 60.85%.Among them,the total content of 8 lignans such as schisandrin A was 44.57%.With soybean oil as oil phase,and Tween-80 as the emulsifier surfactant,the microemulsion was prepared with an average particle size of 248.3 nm,and an average drug loading of 2.44 mg·mL^(-1),with pH of 6.5.Conclusion The established method for the simultaneous determination of 8 components in Schisandrae Chinensis Fructus extract is accurate and feasible,and can be used for its quality control.The total lignan content obtained by extraction and purification is high,with good repeatability.The prepared Schisandrae Chinensis Fructus microemulsion has high drug loading and uniformed particle size and good stability,which lays the foundation for further research on total lignans of Schisandrae Chinensis Fructus.

关 键 词：五味子 总木脂素 提取纯化 干眼症 微乳 

分 类 号：R283.6[医药卫生—中药学]