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目的研究清脑宣窍方有效组分栀子苷、人参皂苷Rg1、人参皂苷Rb1、三七皂苷R1在正常、脑中风急性期和恢复期状态下大鼠体内的药代动力学变化。方法按双侧颈动脉结扎并喂养2周制备中风恢复期模型,采用MCAO法制备中风急性期模型。灌服给予清脑宣窍方有效组分,血浆样品用C18固相柱萃取,以亥茅酚苷为内标,选用Agilent Eclipse XDB-C18色谱柱(4.6mm×250mm,5μm),流动相为乙腈-水二元梯度洗脱,柱温为30℃;流速为1.0mL/min;检测波长为203nm。采用DAS1.0软件对各血浆药物浓度进行拟和分析。结果栀子苷、人参皂苷Rg1、三七皂苷R1在大鼠体内药动学过程均属于二室模型,人参皂苷Rb1属于一室模型。各组分最高血药浓度(Cmax)、血药浓度时间曲线下面积(AUC)值均表现为急性模型组>恢复模型组>正常组。结论不同模型下动物对清脑宣窍方有效组分吸收不同,同等剂量下生物利用度顺序为急性模型组>恢复模型组>正常组。
Objective To study the pharmacokinetics of Qingzhi Xuanxiong prescription in vitro, including the effective components of geniposide, ginsenoside Rg1, ginsenoside Rb1, and notoginsenoside R1 in normal and stroke acute and recovery phases. Methods A stroke recovery model was prepared by bilateral carotid artery ligation and feeding for 2 weeks. The acute stroke model was prepared by MCAO. The effective components of Qingnaoxuanyufang were given by gavage. The plasma samples were extracted by C18 solid-phase column. The hydroquinone was used as the internal standard and Agilent Eclipse XDB-C18 column (4.6mm×250mm, 5μm) was used. The mobile phase was Acetonitrile-water binary gradient elution, column temperature 30°C; flow rate 1.0 mL/min; detection wavelength 203 nm. DAS 1.0 software was used for the simulation analysis of each plasma drug concentration. RESULTS: The pharmacokinetics of jasminoidin, ginsenoside Rg1, and notoginsenoside R1 in rat models belong to a two-compartment model. Ginsenoside Rb1 belongs to a one-compartment model. The highest plasma concentration (Cmax) of each component and the area under the curve of blood drug concentration time (AUC) were expressed as acute model group> restored model group> normal group. Conclusion Animals of different models have different absorption of effective components of Qingnao Xuanxiong Recipe. The order of bioavailability at the same dose is: acute model group> recovery model group> normal group.