【作者】 刘波；

【导师】 朱盛山；

【作者基本信息】 广东药学院 ， 药剂学， 2008， 硕士

【摘要】 目的为了寻找优质的三七药材开展实验,建立三七总皂苷提取工艺和检测方法,揭示复方丹参缓释片三七四种皂苷成分体外释放行为,阐明四种皂苷的释药模式,实现指标成分的均衡释放。方法1.以三七中的三七皂苷R1、人参皂苷Rg1、Re、Rb1四种皂苷作为指标成分,采用TLC法、HPLC法定性和HPLC法定量对广西、云南两种产地的三七药材质量进行评价,优选三七药材;2.以四种皂苷的提取率为评价指标,采用单因素法确定回流法、渗漉法和超声提取法各因素较优水平,采用正交试验法确定三种提取方法各自最佳条件,对比三种方法的最优条件,选择提取率最高的一种方法,即三七总皂苷最佳提取工艺;3.以四种皂苷为指标成分,采用HPLC法对缓释片和普通片不同时间的溶出样品进行检测,拟合释药曲线。结果1.广西、云南两产地三七药材的TLC图谱中,对照品和供试品相同Rf值处出现相同颜色的斑点;HPLC特征图谱中,两种产地的三七药材9个主要吸收峰保留时间均能一一对应,相应吸收峰峰形相近,但四种皂苷含量有较大差异,四种皂苷的峰面积比(广西:云南)分别为:153.0%、117.6%、90.4%和129.9%。2.三七总皂苷最佳提取工艺:0.64倍量的溶剂1浸泡药材(20-40目)1h,10倍量溶剂2回流2次,每次1h;四种皂苷的平均提取率为:92.47%,平均干膏率为:20.20%。3.体外溶出结果表明:复方丹参缓释片中四种皂苷成分在1-10h内释放均衡,释放曲线接近Higuchi方程;普通复方丹参片中四种皂苷成分在40min内释放完全。结论1.本文选广西为复方丹参制剂中三七药材的产地来源;2.建立的三七总皂苷的提取工艺能应用于中试试验及工业化生产,且符合制备复方丹参缓释制剂的要求;3.本文首次采用HPLC法同时测定了复方丹参缓释片和普通复方丹参片中四种皂苷成分的含量,为两种片剂的质量检测提供了更有力的手段;4.复方丹参缓释片中三七四种指标成分在1-10h内释放均衡,实现了均衡释放的目标。更多还原

【Abstract】 Purpose To seek for better Sanqi medicinal material which is fit to experiment, establish the extraction technology of total saponinses and determination method, reveal the release behavior in vitro of 4 saponinses of Sanqi in Compound Danshen Sustained-Release Tablet, illustrate the release mode of 4 saponinses, realize well-balanced release of target ingredient.Method1. 4 saponinses (notoginsenoside R1,ginsenoside Rg1,ginsenoside Re and ginsenoside Rb1) in Sanqi are chosen as target ingredients, and the quanlity of Sanq is from Guangxi and Yunnan is evaluated by qualitative of TLC and HPLC and by quantitative of HPLC, and finally the paper choose the better medicinal material.2. The paper choose the concent of 4 saponinses and the stem plaster rate as evaluation standed, and use single-factor test in determining the better level of Reflux method、percolation method and ultrasonic extraction method, and use orthogonal test in determining the best extraction condition of 3 method above, and finally choose the best extraction technology.3. The paper chooses the concent of 4 saponinses as evaluation standed, and use HPLC in determining the dissolution sample in different time point in Compound Danshen Sustained-releaseTablet and common Compound Danshen Tablet, and finally determines the release mode.Result1. Reference substance and sample appear the same colour dot in the same Rf; The chromatography fingerprints of Sanqi from two different habits have 9 major peaks shared, and the peak area of Guangxi is relatively bigger.,and the proportion of peak area of 4 saponinses(Guangxi : Yunnan) are relatively 153.0%、117.6%、90.4% and 129.9%。2. The best extraction technology of Sanqi total saponinses is as follows: the volume, Concentration and time of the soaking are relatively 2 times of sanqi,solvent 1 and 1h;the Concentration of solvent 2 is 95%,the volume of ethanol is 10,the times is 2 and the extrcation time is 1h.;The average extraction rate of 4 saponinses is 92.47% and the average stem plaster rate is 20.20%.3. The result show that: 4 saponins of Sanqi in Compound Danshen Sustained-release Preparation have a well-balanced release behavior in 1h to 10h with Higuchi release model; 4 saponins of Sanqi in common Compound Danshen Tablet release completely in 40 min.Conclusion1. The paper choose Guangxi as habit resource of Sanqi medical material in Compound Danshen Sustained-Release Tablet;2. The extraction technology of Sanqi total saponinses can be used in pilot test and industrial production, and a better repeatability are all fit for the standed of Compound Danshen Sustained-release Preparation.3. The paper use HPLC in determining the 4 saponinses concent of Compound Danshen Sustained-release Tablet and common Compound Danshen Tablet for the first time, and provide effective determining method for quanlity control.4. 4 saponins of Sanqi in Compound Danshen Sustained-release Preparation have a well-balanced release behavior in 1h to 10h, and realize the purpose of well-balanced release.更多还原