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目的:研究口服清脑宣窍方后在正常、脑中风急性期模型和恢复期模型下大鼠心脏药动学的变化。方法:按双侧颈动脉结扎并喂养2周作为恢复期模型,采用MCAO法制备急性期模型为模型组实验对象。口服给与清脑宣窍方有效组分6g.kg-1,各时间点取出心脏,洗去残血、匀浆、甲醇提取、离心后水溶,C18固相柱萃取,以亥茅酚苷为内标,用高效液相色谱法,选定203nm作为检测波长,同时测定有效组分栀子苷、人参皂苷Rg1、人参皂苷Rb1的浓度,并采用DAS1.0软件对各心脏药物浓度进行拟合分析。结果:栀子苷、人参皂苷Rg1在大鼠心脏内药动学过程均符合二室模型,人参皂苷Rb1符合一室模型。各物质Cmax、AUC值均表现为急性模型组>恢复模型组>正常组。结论:在选定的高效液相色谱条件下,3个有效组分,内标及心脏杂质分离良好,可用于3种成分的心脏组织含量测定。模型状态下的动物与正常状态下的动物,清脑宣窍有效组分的体内药动学过程有明显差异。
OBJECTIVE: To study the changes of pharmacokinetics in rats after oral administration of Qingnao Xuanxiongfang in the normal and stroke acute models and recovery models. METHODS: The bilateral carotid artery was ligated and fed for 2 weeks as the recovery model. The acute phase model was prepared using MCAO method as the model group experimental object. Oral administration of effective components of Qingnao Xuanxiong prescription (6g.kg-1). The heart was removed at each time point. The residual blood was washed, homogenized, extracted with methanol, and dissolved in water after centrifugation. C18 solid-phase column extraction was used to detect the hydrocortisone. Internal standard, high performance liquid chromatography, selected 203nm as the detection wavelength, simultaneous determination of the effective components of geniposide, ginsenoside Rg1, ginsenoside Rb1 concentration, and the use of DAS1.0 software for the concentration of each cardiac drug analysis. RESULTS: The pharmacokinetics of jasminoidin and ginsenoside Rg1 in rat heart were consistent with the two-compartment model, and ginsenoside Rb1 conformed to a one-compartment model. The Cmax and AUC values of all substances were expressed as acute model group> restored model group> normal group. Conclusion: Under the selected HPLC conditions, the three effective components, internal standard and heart impurities are well separated and can be used for the determination of heart tissue content of three components. There were significant differences in the in vivo pharmacokinetics of the effective components of Qingnao Xuanjing between animals in the model state and those in the normal state.