胃肠舒片促胃肠动力的药效物质基础及药代动力学

Based on the qualitative analysis of fingerprint peaks, the chemical composition and structure of Weichangshu was identified by the methods of HPLC-MSn combined with NMR, MS, IR, UV. The active sites were screened by pharmacodynamics experiment. The active sites were screened by pharmacodynamics experiment followed the extraction of each part of Weichangshu. The chemical composition and structure was identified by the use of NMR, MS, IR, UV. Rat serum samples of different doses of Weichangshu after different time periods were analyzed of blood component by the use of HPLC-MSn. The chemical composition and structure was identified by the use of NMR, MS, IR, UV. The potential material was explicited by pharmacodynamics filtration. To definitude the potential material basis of the absorption into the blood through serum drug chemistry and pharmacodynamic research. To definitude the potential material basis of the absorption not into the blood through active component separation and pharmacodynamic research.The determined potential material of plasma and tissue screened by pharmacodynamic experiment was detected by HPLC-MSn to clear the multi-component pharmacokinetics and tissue distribution of Weichangshu tablets. The projec is of great significance that it will provide new ways of prevention and treatment for gastrointestinal disorder, and provide new ideas for research about the traditional Chinese medicine of improving gastrointestinal motility.

通过胃肠舒片指纹图谱指纹峰归属定性分析，用HPLC-MSn、NMR、MS、IR、UV技术鉴定化学成分与结构，药效学实验筛选活性部位。萃取胃肠舒片各部位，药效学实验筛选活性部位，用NMR、MS、IR、UV技术鉴定化学成分与结构。采集给大鼠不同剂量胃肠舒溶液的不同时间段血清样品，用HPLC-MSn分析血移成分，结合NMR、MS、IR、UV技术鉴定化学成分与结构，药效学实验筛选确定药效物质。通过血清药物化学与药效学相关研究，明确胃肠舒片吸收入血成分的药效物质基础，通过活性成分分离与药效学相关研究，明确胃肠舒片非入血成分的药效物质基础。采集给大鼠不同剂量胃肠舒溶液的不同时间段血浆及组织，用HPLC-MSn检测各时间段血浆及组织中经药效学实验筛选确定的药效物质，明确胃肠舒片药效物质多组分药代动力学。 本项目可为胃肠动力障碍性疾病提供防治新途径，为中药胃肠动力药研究提供新思路，具有重要理论意义。

用分析软件Xcalibur从胃肠舒图谱中找出111个化合物，其中37个化合物根据参考文献确定了名称。通过胃肠舒片指纹图谱指纹峰归属定性分析，对其中11个主要化合物进行了含量测定和结构鉴定。经药效学实验，将萃取的6个部位筛选出了3个活性部位，从3个活性部位分离并进行结构鉴定出14个活性成分。综合活性部位分离出的活性成分、指纹图谱中和血清药物化学所见的活性成分大黄素、甘草酸、大黄酸、甘草苷、芍药苷、芍药内酯苷、苯甲酰芍药苷、芦荟大黄素、大黄素甲醚、大黄酚、甘草素、异甘草素、羟基芍药苷和芒柄花素，进行药效学实验表明，14个成分均能显著促进胃肠动力，提示这14个成分是胃肠舒片促进胃肠动力的药效物质基础。通过对不同时间段血浆及组织检测确定的药效物质，明确了胃肠舒片药效物质多组分组合药代动力学及组织分布。.胃肠舒片体外指纹图谱和主要成分含量测定，对胃肠舒片的定量分析和质量控制提供了可靠依据。明确胃肠舒片促胃肠动力的药效物质基础，为开发新型胃肠动力药打下了坚实基础。明确胃肠舒片药效物质多组分组合药代动力学及组织分布，对胃肠舒治疗胃肠动力障碍性疾病的服药量和服药次数具有重要指导作用和理论意义。.本项目可为胃肠动力障碍性疾病提供防治新途径，为中药胃肠动力药研究提供了新思路，具有重要理论意义。