花红片中槲皮素的药动学-药效学相关性初步研究

Studies on Correlation Between Pharmacokinetics and Pharmacodynamics Characteristics of Quercetin from Huahong Tablets

目的：研究化红片的药效学与其主要成分槲皮素的药动学，探讨其药动学与药效学相关性。方法：采用醋酸扭体法和热板法观察花红片对小鼠的镇痛作用，高效液相色潜法测定花红片中有效成分槲皮素在小鼠体内的血药浓度，以效应-时间、效应-血药浓度曲线进行相关分析；采用WittNonlin软件对药物效应．血药浓度进行PK—PD模型拟合。结果：花红片在1-3h发挥较强的镇痛作用，与槲皮素血药浓度．时间曲线的达峰时间相比其具有一定的滞后性。痛阈提高百分率和血药浓度之间的关系符合简单的最大效应模型；镇痛抑制率和血药浓度之间的关系符合效应抑制模型。结论：花红片有明显的镇痛作用，其药效学与槲皮素药动学是相关的。

Objective： To study pharmacodynainic of Huahong tablets and its main component-quercetin＇s pharmacokinetics in vivo in order to investigate the preliminary correlation of pharmacokineties and pharmacodynamics （PK-PD）. Method： Analgesie effect of Huahong tablets was studied by the writhing testinduced by acetic acid and hot plate method in mice, the serumconcentration of quercetin as Huahong tablets active ingredient was determined by HPLC assay, and correlation analysis on effect-time curve and effect-blood concentration curve; PK-PD model were fitted on drug effect-plasma concentrations with WinNonlin software. Result： Huahong tablets have a significant analgesic effect between 1 and 3 hours, compared with the peak time of the concentration-time curve of quercetin, analgesic effect was lag certainly. Conclusion： Huahong tablets have a significant analgesic effect, pharmacodynamics of Huahong tablets and its main component-quercetin＇s pharmacokinetics are relevant. The relationship between increment percentage of analgesic threshold and plasma concentrations can meet the simple maximum effect PK-PD model; the relationship between inhibition rate of analgesia and plasma concentrations meet the simple maximum effect PK-PD model.