基于吸收机制和PK-PD模型的黔产荭草花药代动力学研究

荭草花为蓼科植物荭草的花序，是贵州省民间及少数民族常用药物，课题组在国家自然科学基金"基于体内直接作用物质的荭草药效物质基础研究"（30860366）中明确了荭草花是荭草抗心肌缺血的药用有效部位，具有比全株"荭草"更明显的抗心肌缺血作用，并完成了荭草花化学成分、有效组分及血清药物化学初步研究。本课题将在前期工作基础上，以UPLC-MS/MS为基本手段，从在体、离体器官和细胞水平多角度研究荭草花活性成分的小肠吸收特性，揭示其吸收机制，同时通过体内代谢研究，明确荭草花中各成分在体内的存在形式及其代谢途径，并结合心肌细胞氧化损伤模型开展多效应成分的PK-PD相关性研究，探讨荭草花在体内的动力学过程和产生药理效应的动态变化及其抗心肌缺血作用机制，揭示荭草花整体药动学特征，阐明体内与抗心肌缺血作用直接相关的物质，为荭草花创新药物研制和药用资源深度开发奠定科学依据。

The flowers of Polygonum orientale is a commonly used medicine of the folk and minority nationalities in Guizhou province , has the latent medicinal developing value. Our group had definite that the flowers is the medicinal parts of Polygonum orientale on Anti-Myocardial Ischemia through the National Natural Science Foundation "The study on effective substance of Polygonum orientale L."(30860366), and studied systematically on chemical constituents, pharmacological action and serum pharmacochemistry research. This research will regard the whole elements the starting point, analyze with UPLC-MS/MS, determination the intestinal permeability,characteristics of absorption of the main active ingredient of the flowers by organs and cellular level in vivo and vitro. Analysis the studies of metabolism in vivo to determine the form and its metabolism way and mechanism to component of the flowers. Establish multicomponent PK-PD model to determine the Pharmacokinetics and Pharmacodynamic to develop and validate the holistic pharmacokinetic properties.Through the above studies, the effective substance of the flowers on Anti-Myocardial Ischemia is elucidated which lay a theoretical and experimental foundation for mechanism and drug development of the flowers of Polygonum orientale L.