【作者】 童荣生；

【导师】 彭成；

【作者基本信息】 成都中医药大学 ， 中药学， 2010， 博士

【摘要】 目的：比较半夏泻心汤及其苦降药组指纹图谱的不同,主要成分含量的变化,药动学、药效学的差别以及两者的关联性,以期从药队有效成分层面揭示半夏泻心汤的配伍原理。方法：通过体外主要成分含量测定和指纹图谱的研究,比较半夏泻心汤及其苦降药组的主要成分含量和指纹图谱的不同；通过半夏泻心汤及其苦降药组水提醇沉液中黄芩苷、黄芩素、小檗碱、巴马汀在正常大鼠和胃肠动力障碍大鼠体内的药代动力学特征的研究,比较两者主要成分的药代动力学差异；通过观察半夏泻心汤及其苦降药组对正常大鼠和胃肠动力障碍大鼠胃排空、小肠推进、胃肠激素(Gas、MTL、SS、VIP)等指标的影响,比较两者药效作用的差别,并且进行了半夏泻心汤及其苦降药组药动学和药效学的关联性分析,以期从药队有效成分层面揭示半夏泻心汤的配伍原理。结果：1、半夏泻心汤水提醇沉液中的小檗碱、巴马汀、黄芩苷含量明显高于苦降药组水提醇沉液中的含量。2、半夏泻心汤的指纹图谱与苦降药组是有一定差别的,但共有色谱峰峰面积占半夏泻心汤总峰面积的98.18%。3、半夏泻心汤中黄芩苷、黄芩素、小檗碱、巴马汀在正常大鼠和胃肠动力障碍大鼠体内的AUC(0-∞)较苦降药组更大、Cmax更高,黄芩苷、小檗碱、巴马汀的Tmax更快,t1/2z更短。4、半夏泻心汤及其苦降药组均有促进正常大鼠和胃肠动力障碍大鼠胃排空和小肠推进的药效作用,且对胃肠激素有一定的调节趋势。5、半夏泻心汤及其苦降药组中黄芩苷、黄芩素、小檗碱、巴马汀在血清中的含量与正常大鼠和胃肠运动障碍大鼠胃排空和小肠推进有一定的相关性。结论：苦降药组是半夏泻心汤中重要的组成部分,在半夏泻心汤中起主要作用；黄芩苷、黄芩素、小檗碱、巴马汀是半夏泻心汤及其苦降药组调节胃肠运动的主要有效成分；半夏泻心汤在有效成分含量、体内代谢特征和药效作用方面均优于苦降药组,体现出全方的配伍优势。更多还原

【Abstract】 Objective:To reveal the compatibility principle of Pinelliae Decoction for Purging Stomach-Fire in the level of active component, we observed variance of key components assaying and diversity of pharmacokinetics, pharmacodynamics and their relevance, compared Pinelliae Decoction for Purging Stomach-Fire with its bitter drugs for purgation.Methods:We used the research methods of key components assaying and finger printing, and compared Pinelliae Decoction for Purging Stomach-Fire with its bitter drugs for purgation. We observed the pharmacokinetics characteristic of baicalin, baicalein, berberine, palmatine in normal rats and stomachal dyskinesis rats and compared Pinelliae Decoction for Purging Stomach-Fire with its bitter drugs for purgation. We researched gastric emptying and small intestine propulsion and gut hormone (Gas, MTL, SS and VIP), and observed the pharmacodynamic action, and compared Pinelliae Decoction for Purging Stomach-Fire with its bitter drugs for purgation. We observed the relevance of pharmacokinetics and pharmacodynamics, compared Pinelliae Decoction for Purging Stomach-Fire with its bitter drugs for purgation. All researches were useful of revealing the compatibility principle of Pinelliae Decoction for Purging Stomach-Fire in the level of active component.Results:1. The contents of berberine, palmatine, baicalin in Pinelliae Decoction for Purging Stomach-Fire were obviously higher than its bitter drugs for purgation.2. The HPLC finger printings of Pinelliae Decoction for Purging Stomach-Fire and its bitter drugs for purgation have small distinction. Their chromatographic peak area owned by both was 98.18% in all peak area.3. The AUC (0-∞) and Cmax of baicalin, baicalein, berberine, palmatine in Pinelliae Decoction for Purging Stomach-Fire were higher than the bitter drugs for purgation in normal rats and stomachal dyskinesis rats. The Tmax and tl/2z of baicalin, berberine, and palmatine were longer.4. Pinelliae Decoction for Purging Stomach-Fire and its bitter drugs for purgation had auxoaction on gastric emptying and small intestine propulsion, and had much regulate tendency on gut hormone in normal rats and stomachal dyskinesis rats. Pharmacodynamic action of Pinelliae Decoction for Purging Stomach-Fire was better than it bitter drugs for purgation.5. The contents of baicalin, baicalein, berberine, palmatine in serum had associativity with auxoaction on gastric emptying and small intestine propulsion in normal rats and stomachal dyskinesis rats.Conclusions:The bitter drugs for purgation are fundamental ingredient and have main effect in Pinelliae Decoction for Purging Stomach-Fire. Baicalin, baicalein, berberine, palmatine are fundamental active components of regulating gastrointestinal function in Pinelliae Decoction for Purging Stomach-Fire and its bitter drugs for purgation. The active component content and pharmacokinetics characteristic and pharmacodynamic action in Pinelliae Decoction for Purging Stomach-Fire are more preponderant than the bitter drugs for purgation, which reflect the preponderance of compatibility in whole preparation.更多还原