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目的利用药动参数结合药效综合指标开展白芍总苷体外抗炎时效相关性评价研究,为探讨其临床合理利用提供前期实验基础。方法取SD大鼠灌服白芍总苷提取液(290mg·kg~(-1))后,以HPLC-TOF-MS法测定不同采血时间点血浆中芍药内酯苷、芍药苷浓度,根据药时曲线计算药动学参数;以TNF-α、IL-6和NO的综合指标为考察对象,开展不同时间点含药血浆体外药效评价研究;将体内药动与体外药效相结合开展时效相关性分析,评价白芍总苷作用规律及特点。结果白芍总苷中芍药苷和芍药内酯苷的T_(max)分别为60、30min,C_(max)为1860.7、895.8μg·ml~(-1);白芍总苷含药血浆浓度(尤其是芍药苷)与小鼠单核巨噬细胞体外炎症模型抑制率之间呈良好的相关性。结论实验明确了白芍总苷体内代谢与药效的变化规律,为其临床合理使用及新药开发提供基础。
OBJECTIVE To evaluate the anti-inflammatory and anti-inflammatory effects of total glucosides of paeony on the basis of comprehensive pharmacokinetic parameters and pharmacokinetic parameters, and to provide pre-experimental basis for exploring its clinical rational utilization. Methods SD rats were drenched with total paeony glycoside extract (290 mg · kg -1) and determined by HPLC-TOF-MS method. The concentrations of laccolide and paeoniflorin in plasma were determined by HPLC- Time curve of pharmacokinetic parameters; to TNF-α, IL-6 and NO comprehensive index as the object of study to carry out in different time points drug-containing plasma pharmacodynamics evaluation; combination of pharmacokinetics and in vitro pharmacodynamics to carry out aging Correlation analysis, evaluation of the law and characteristics of total glucosides of paeony. Results The T_ (max) of paeoniflorin and paeoniflorin in total glucosides of Paeonia were 60 and 30 min, respectively, and the max values of C_ (max) were 1860.7 and 895.8 μg.ml ~ (-1) Especially paeoniflorin) and mouse monocyte-derived macrophage inflammatory model in vitro inhibition rate was a good correlation. Conclusion The experiment clearly defined the changes of the metabolism and efficacy of total glucosides of paeony, providing the basis for its clinical rational use and new drug development.