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目的:考察醋柴胡对龙胆苦苷在小鼠体内分布的影响,探讨醋柴胡肝引经作用机制。方法:将192只雄性昆明种小鼠随机分为4组,包括龙胆苦苷空白组和龙胆苦苷-醋柴胡低、中、高剂量组,分别于0.08,0.25,0.5,0.75,1,1.5,2,4 h(每个时间点6只动物)采集血浆、肝、心、脾、肺、肾组织,预处理后利用HPLC-MS/MS测定药物含量,分析其药动学过程,以相对摄取率(Re)和相对综合靶向效率(RTE)评价醋柴胡对龙胆苦苷在小鼠体内分布的影响。结果:不同剂量醋柴胡均可增加龙胆苦苷在肝脏的RTE,低、中、高剂量醋柴胡组肝脏的RTE分别为0.25,0.13,0.33。但并不增加龙胆苦苷肝内摄入,而是显著减少药物在其他组织的分布。结论:醋柴胡通过减少龙胆苦苷在其他组织分布达到增加肝RTE的作用。
Objective: To investigate the effect of vinegar on the distribution of gentiopicroside in mice, and to explore the mechanism of the introduction of vinegar, Bupleurum root. Methods: Ninety-two male Kunming mice were randomly divided into 4 groups, including gentiopicroside blank group and gentiopicroside-acerolactam low, medium and high dose groups, respectively, at 0.08,0.25,0.5,0.75, The plasma, liver, heart, spleen, lung and kidney tissues were collected at 1, 1.5, 2 and 4 h (6 animals at each time point). The drug content was determined by HPLC-MS / MS after pretreatment and the pharmacokinetics The effect of gentiana on the distribution of gentiopicroside in mice was evaluated by the relative uptake rate (Re) and relative comprehensive efficiency (RTE). Results: Different dosages of Bupleurum chinense increased the RTE of gentiopicroside in the liver. The RTEs of low, middle and high doses of Bupleurum chinense were 0.25,0.13 and 0.33, respectively. But did not increase the intrahepatic ingestion of gentiopicroside, but significantly reduced the distribution of the drug in other tissues. Conclusion: Bupleurum vinegar can increase the hepatic RTE by reducing the distribution of gentiopicroside in other tissues.