【作者】 马秋菊；

【导师】 于维萍；

【作者基本信息】 山东中医药大学 ， 中药学， 2008， 硕士

【摘要】 目的:研制中药复方制剂消脂通脉颗粒。方法与结果:采用超临界CO2萃取技术提取处方中莪术、炒白术、陈皮的有效成分挥发油,用正交试验,以挥发油收率为指标,优选超临界CO2萃取条件为:萃取压力为25Mpa、温度为45℃、时间为2.5h。为了防止挥发油的挥发损失,增加其稳定性,采用饱和水溶液恒温搅拌法,用β-环糊精对所得挥发油进行包合。以挥发油利用率、包合物收率、包合物含油率的综合评分为指标,用L9(34)正交实验考察的最佳包合条件是:挥发油与β-CD的比例为1:8、50℃包合1小时。处方药物的非挥发性有效成分为醇溶性成分,宜用乙醇提取。以醇提干浸膏得率和臣药泽泻中泽泻醇B23-乙酸酯含量的综合评分为指标,用正交实验优选醇提工艺,结果显示:以加8倍生药量的70%乙醇温浸(50℃)60 min作为第一次提取,第二次提取加6倍生药量的70%乙醇温浸(50℃)30 min为最佳。醇提液的回收乙醇、浓缩与干燥采用减压蒸馏与真空干燥。所得干浸膏含水量控制在4%以内,以达制粒要求。制剂成型工艺进行了最佳赋形剂的用量、矫味剂的用量、润湿剂乙醇的浓度的选择实验,确定薏苡仁细粉的用量为干浸膏重的40%,甜菊素为干浸膏重的5%,乙醇以80%为最佳。按照优选出的制备工艺,进行了三批制剂的中试研究,每批制剂投料量为每日处方量的80倍,进一步验证了优选工艺的稳定可行性。进行了制剂质量标准的研究,建立了半夏、大黄、威灵仙、炒白术、莪术的薄层色谱鉴别方法,斑点清晰,阴性无干扰。通过方法学考察试验,用HPLC法测定制剂中泽泻醇B23-乙酸酯和橙皮苷的含量,规定了含量限度。对样品进行了初步稳定性研究,室温条件下储存三个月,按制订的质量标准进行考察,结果都达到了要求,表明制剂稳定性良好。进行了制剂的药效学和毒理学研究,结果能显著降低家兔血清甘油三酯含量,能显著降低高脂血症大鼠的TC、HDL-C、LDL-C值,表明消脂通脉颗粒有显著的降脂作用,急性毒性试验表明本制剂低毒安全。结论:工艺及质量控制方法切实可行,稳定可靠,药效学及毒理学实验为临床应用提供了理论基础。更多还原

【Abstract】 Objective: The Preparation and Evaluation of the compound Chinese medicine Xiaozhitongmai. Methods: We extracted the volatile oil from Curcuma and Atractylodes macrocephala and Citri reticulatae by the Supercritical CO2 Fluid extraction.Using the yield of volatile oil as index,we selected the Optimum extraction conditions by the orthogonal test, which were 25MPa(the extracting pressure), 45℃(the extracting temperature ) ,2.5hour(the extracting time). Using the ultizision ratio of oil and the oil-beared ratio and the yield of inclusion compound as indexes , we selected the Optimum conditions for inclusion by the orthogonal test ,which were 1:8(w/w) (the ratio of oilβ-CD ), 50℃(the inclusion temperature),1hour(the inclusion time).To find the best condition of extracting the active constituents of Xiaozhitongmai Granule with alcohol, using the yield of alcohol extractive and content of AlisoB23-acetate as the detective indexes,we selected Optimum extracting conditions by The orthogonal text. Experiments showed best condition was Volume ratio of 1:8(w/w) (the ratio of herbs and 70% alcohol), extracting for 2 times(first times 60min,second times 30 min) and water temperature was 50℃.Extracting solution with alcohol was Concentrated by pressure-reduced distillation and dried in Vacuum dry box. and water-content of alcohol extractive was smaller than 4%. in the Preparation Process,Coix lachrymajobi was used as Cppropriate ,Steviosin was used to correct the taste and 80% alcohol was used as moistening agent.We carried out the dctermination methods of Pinellia Ternata、WeiLing- Xian、Rhubarb、Curcuma and Atractylodes macrocephala through TLC,and the speekles were clear and the negative contrast had no interference.The content of AlisoB23-acetate and Hesperidi was determined through HPLC in XiaoZhiTongMai granule.we studied the stability of Xiaozhitongmai granule,The result showed that the product quality keep stable when beening conserved in room temperature for three months. The study of Pharmacodynamics and toxicology indicated that it held obvious Lowering blood lipids effect and had no toxicity .Conclusion: The well-chosen technology was stable and feasible,the quality of the granule of Xiaozhitongmai can be controlled by the established containation testing method. The study on Pharmacodynamics and toxicology of the granule of Xiaozhitongmai offered a foundation to clinical use.更多还原