【作者】 冯锁民；

【导师】 孙文基；

【作者基本信息】 西北大学 ， 中药学， 2007， 博士

【摘要】 本文由三部分组成，第一部分为杜仲化学成分的分离分析和高速逆流色谱在杜仲化学成分分离中的应用；第二部分为秦艽地上部分龙胆总苷的提取及薄膜衣片生产工艺和质量标准的研究；第三部分为清热消炎灵薄膜衣片质量标准和生产工艺的研究。在第一部分中，运用传统的柱层分离方法从杜仲树皮用有机溶剂萃取后的水层中分离得到七个化合物，分别是桃叶珊瑚苷、松脂醇二葡萄糖苷、中脂素二葡萄糖苷、丁香脂素二葡萄糖苷、橄榄脂素单糖苷、松脂醇单糖苷、地黄普内酯。研究了简便、快速、规模制备松脂醇二葡萄糖苷的新工艺。同时应用高效液相色谱法对杜仲原生皮与再生皮中松脂醇二葡萄糖苷的含量进行了测定，评价再生皮的质量，指出杜仲同一植株剥皮再生可进行两次，每次间隔不少于5年，第三次再生皮的有效成分有待提高。该研究为杜仲剥皮再生技术的开展提供了实验依据，解决了人们对再生皮质量的疑惑。通过对杜仲新鲜树皮在放置过程中桃叶珊瑚苷含量的测定，提示随着时间的推移，桃叶珊瑚苷的含量在逐渐降低。高速逆流色谱是近几年发展起来的新的分离技术，它具有分离过程短，效率高，样品预处理简单，操作方便，溶剂消耗少，可避免因不可逆吸附而引起样品损失等优点。我们采用该新技术从杜仲树皮的粗提物中，经一次分离得到纯度在95％以上的松脂醇二葡萄糖苷和丁香脂素二葡萄糖苷。该方法在国内外尚未见报道，研究论文被SCI收录。秦艽主要成分为龙胆苦苷，药用其地下部位的根，况且根的生长周期长，产量低，而每年都可收获的地上部分枝叶被弃去，造成浪费。为了扩大药用部位，节约资源，经研究地上部位龙胆苦苷的含量也在2％以上，完全符合药典要求。因此我们对秦艽地上部分龙胆苦苷的提取工艺进行了研究，从中提出符合要求的龙胆总苷，将其压制成片剂，并包成薄膜衣。对片剂生产工艺及质量标准做了研究，解决了该片剂生产过程中易吸潮结块和受热变软两大难题，并将其申报为国家五类新药。清热消炎灵薄膜衣片也是我们研制的一个新药，为中药复方制剂。由虎杖、蒲公英、半枝莲等组成，具有清热解毒之功效。对其制剂工艺和质量标准进行了研究。利用薄层层析对制剂中的药材进行定性鉴别，采用高效液相色谱对主要有效成分的含量进行控制，同时摸索了最佳的制粒、压片、包薄膜衣工艺，生产出完全合格的产品。更多还原

【Abstract】 This paper consists of three parts.The first fraction is extraction, isolation, purification and analysis of bioactive components in Eucommia ulmoides oliv (Duzhong), as well as application of high-speed countercurrent chromatography (HSCCC).The second part is made of the extraction of gentiopicroside in Qinjiao above ground part and its film-coated tablets preparation.The last section is studing on Qingre XiaoYanling film-coated tablets production and quality control standards.In the first part,we make use of traditional silica column chromatography method to carry out a systymatic research on the chemical constituts of the bark of Eucommia ulmoides oliv.Seven compounds were obtained from the process.They are aucubin, pinoresinol diglucoside (PDG), Medioresinoldiglucoside, syringaresinoldiglucoside (SDG), olivilglucoside, pinoresinol single-glucoside,loliolide. A new, simple, and rapid technique was established for isolation and purification of PDG from Duzhong.In order to evluate the reborn barks qulity,PDG content in three times reborn barks were determined.The result indicates that the girdling bark regeneration can be made twice,the time between the first and the second is not less than five years.The research also provides an experimental basis for the girdling bark regeneration technologies and solves people’s doubts about the quality of recycled bark.HSCCC is a liquid-liquid partition chromatography with a liquid stationary phase.lt has advantages of short separating process,high efficiency,simple preparation sample,convenient to operate,less solvent consumption,and eliminating irreversible adsorption.We employed the new technology in separation PDG and SDG from the crude extract of eucommia bark.The method yieded PDG and SDG over 95% purity in a single operation.To our knowledge, this is the first report and the paper about the test was accepted by SCI.Gentiopicroside is the main effective ingredients in Qinjiao underground root.Because of longer growth cycle,lower yields,we found new medicinal part in Qinjiao that was wasted every year aboveground.To our research,the content of gentiopicroside in Qinjiao overground part can meet the standard of Chinese Pharmacopoeia.So we studied the extraction technique of gentiopicroside from aboveground part of Qinjiao.The extraction was prepared into film-coated tablets.In the tablets production process,the two problems of absorbing moisture and caking softened were solved.In the last chapter,we researched the preparation and quality control standard of Qingre Xiaoyanling film-coated tablets.Thin layer chromatography (TLC) was used for identification,HPLC was employed for the contents of the main active ingredient.更多还原