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目的:研究花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,高效液相色谱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WinNonlin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1~3 h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 the pharmacodynamics and the pharmacokinetics of its main component quercetin, and to explore the correlation between its pharmacokinetics and pharmacodynamics. Methods: The analgesic effect of Conundrum on mice was observed by acetic acid writhing method and hot plate method. The plasma concentration of quercetin in Conundrum was determined by high performance liquid chromatography (HPLC) Effect-serum concentration curve correlation analysis; using WinNonlin software for drug effect - blood concentration PK-PD model fitting. Results: The radix plexus tablets had a strong analgesic effect at 1 ~ 3 h, which had some hysteresis compared with the peak time of quercetin plasma concentration - time curve. The relationship between the percentage increase in pain threshold and plasma concentration was in line with the simple maximal effect model. The relationship between analgesic inhibition and plasma concentration was consistent with the model of effect suppression. Conclusion: The red tablets have a significant analgesic effect, and its pharmacodynamics is related to quercetin pharmacokinetics.