Yu-Jie Hou, Kang-Ning Xiao, Jian-Yun Bi, Xin-Jun Zhang, Xin-Rui Li, Yu-Qing Wang, Ming Su, Xin-Ru Sun, Hui Zhang, Bo-Yang Wang, Li-Jie Wang, Shan-Xin Liu
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引用次数: 0
摘要
本研究基于药代动力学理论,研究了白花蛇舌草素、芍药苷、乌药苷、乌药皂苷在正常大鼠和发热大鼠体内的药代动力学特征,总结了大黄素在正常大鼠和发热大鼠体内的吸收和消除规律,为大黄素的进一步开发和临床应用提供参考。在正常大鼠和模型大鼠胃内给药后,分别于不同时间点从眼底静脉丛抽取血样。采用超高效液相色谱-三重四极杆质谱(UPLC-MS/MS)技术测定不同时间点血液中各种物质的浓度。使用药代动力学软件 DAS 2.0 计算各成分的药代动力学参数。结果表明,4 种成分在各自的范围内具有良好的线性关系,方法学考察结果符合要求。采用 DAS 2.0 非室模型计算了 C_(max)、T_(max)、t_(1/2)、AUC_(0-t)、AUC_(0-∞)和 MRT_(0-t)等药代动力学参数。与正常组相比,模型组 4 种成分的 C_(max) 和 AUC_(0-t) 均显著增加。正常组与模型组的药代动力学特征存在明显差异,说明在不同的生理状态下,大黄素的吸收和消除可能会受到机体内环境变化的影响。
[Pharmacokinetics study of Dayuanyin in normal and febrile rats].
Based on the pharmacokinetics theory, this study investigated the pharmacokinetic characteristics of albiflorin, paeoniflorin, wogonoside, and wogonin in normal and febrile rats and summarized absorption and elimination rules of Dayuanyin in them to provide reference for further development and clinical application of Dayuanyin. Blood samples were taken from the fundus venous plexus of normal and model rats after intragastric administration of Dayuanyin at different time points. The concentration of each substance in blood was determined by ultra performance liquid chromatography-triple quadrupole mass spectrometry(UPLC-MS/MS) technique at different time points. DAS 2.0, a piece of pharmacokinetics software, was used to calculate the pharmacokinetic parameters of each component. The results show that the 4 components had good linear relationship in their respective ranges, and the results of methodological investigation met the requirements. The pharmacokinetic parameters of C_(max), T_(max), t_(1/2), AUC_(0-t), AUC_(0-∞), and MRT_(0-t) were calculated by the DAS 2.0 non-compartmental model. Compared with those in the normal group, C_(max) and AUC_(0-t) of the 4 components in the model group were significantly increased. There were significant differences in the pharmacokinetic characteristics between the normal and model groups, suggesting that the absorption and elimination of Dayuanyin may be affected by the changes of internal environment of the body in different physiological states.