【作者】 崔维利；

【导师】 冯毅凡；

【作者基本信息】 广东药学院 ， 药剂学， 2008， 硕士

【摘要】 高良姜为姜科山姜属植物高良姜Alpinia officinarum Hance的干燥根茎。主要含有:挥发油类,黄酮类,二苯基庚烷类,苯丙素类,糖苷类及微量元素成分。具有温胃散寒,消食止痛作用,常用于脘腹冷痛,胃寒呕吐,嗳气吞酸的治疗。根据文献,高良姜中的二苯基庚烷类成分具有显著的镇痛作用,本实验据此研究一种新的用于局部镇痛的现代中药“高良姜DPH提取物凝胶剂”。本实验以1-苯基-7-（3’-甲氧基-4’-羟基）苯基-5-醇-3-庚酮（以下简称二苯基庚烷A）为指标对高良姜药材进行了筛选。采用超临界流体萃取技术对药材中有效部位进行提取,得到脂溶性成分高良姜超临界CO₂提取物（以下简称高良姜SFE提取物）,采用分子蒸馏技术对有效部位高良姜SFE提取物进行富集,得到高良姜二苯基庚烷类提取物（以下简称高良姜DPH提取物）,按单因素实验的方法,对富集工艺进行了优化,确定最佳工艺为:加热温度90℃时,真空度5Pa,将超临界萃取物预加热至60℃进料,转子刮膜的转速为260²80r·min^-1,流速2ml·min^-1。采用LC-MS分析技术对高良姜DPH提取物中的有效成分二苯基庚烷类进行确证,并对高良姜DPH提取物的质量控制方法进行了研究。通过动物实验确定了高良姜SFE提取物和富集后的高良姜DPH提取物的LD50值,分别为:1.338g/kg和10.64g/kg。并采用醋酸扭体法验证了高良姜DPH提取物的镇痛药效,高良姜DPH提取物的量效呈线性关系,ED50为464.4mg/kg。根据制剂原料的理化性质,结合凝胶剂本身的特点,优化了高良姜DPH提取物凝胶剂的制剂成型工艺。最佳工艺为:将卡波姆均匀撤于适量蒸馏水面上,静置,使之充分溶胀,配成3%的卡波姆水凝胶基质;将高良姜DPH提取物用无水乙醇溶解,依次加入氮酮、甘油、丙二醇、尼泊金乙酯混匀。将上述药液加入基质中,边加边搅拌,再缓慢滴加三乙醇胺,加水至足量,搅拌均匀,即得。对制剂的质量控制方法进行了研究,采用紫外分光光度法对制剂中主要有效成分二苯基庚烷类进行了含量测定,建立了制剂的质量标准草案,并对制剂的稳定性进行了考察。更多还原

【Abstract】 Rhizoma Alpiniae officinarum is drying plant rhizomes of Alpinia officinarum Hance. Mainly contains: Essential oils, flavonoids, diphenylheptane category, phenylpropanoid category, glycosides and trace constituents. With the effect of warming the middle warmer, cold-dispelling, promoting digestion, and alleviating pain, it commonly used for the treatment of abdominal psychroalgia, gastrofrigid vomiting,belching, etc. In recent years, both at home and abroad, studies of Galangal were mainly centered on flavonoids. In this experiment diphenylheptane constituents are studied, and a new modern medicine,“DPH Gel”for the treatment of pain is studied and prepared.In this experiment, with diphenyl heptane A as indicator, Galangal medicines were screened.Effective fraction in Chinese medicinal materials was extracted by supercritical fluid extraction technology and SFE extraction was obtained. Molecular distillation technology was used for further purification of SFE extraction from Rhizoma Alpiniae officinarum. By the method of single-factor experiment, purification process was optimized: temperature 90℃, the vacuum 5 Pa, super critical extraction pre-heated in 60℃, scraping membrane rotor speed 260 to 280 r·min^-1, flow rate 2 mL·min^-1.Effective fraction in extracts by molecular distillation technology （shorted as“DPH extracts”）were as identified through LC-MS. Quality control methods for DPH extracts were studied.Identified through animal experiments, the LD50 value of SFE extracts and DPH extracts were as follows: 1.3377 g / kg and 10.641 g / kg. And through acetic acid writhing test, the analgesic efficacy of Galangal extract was confirmed. A linear dose-effect relationship of Galangal extract was identified, which is ED50 464.39 mg·kg-1. Based on the physical and chemical properties of raw materials and the characteristics of gel, DPH gel formulations process was optimized. Optimum: Carbomer was uniformly sprinkled on the surface of distilled water, and standing to the full swelling, then 3% Carbomer hydrogel matrix is prepared. Galangal extract was dissolved into ethanol,then Azone,glycerin,propyleneglycol, and ethyl Nipagin were joined and blended into uniform solution. The solution was added in the matrix, stirring, then triethanolamine was slowly added. Stirring, water was added to prepare DPH Gel.Quality control methods for preparations were studied by ultraviolet spectrophotometry. Contents of main active ingredient in the preparation were determinated. Standards for quality control of the preparation were established.更多还原