田甜, 李园园, 吴家胜, 王天明, 李安宁, 吴迪, 孙晓菲, 石荣, 马越鸣. 小鼠体内金芪降糖胶囊多成分药代动力学研究J. 药学学报, 2025, 60(4): 1084-1092. DOI: 10.16438/j.0513-4870.2024-0812
引用本文: 田甜, 李园园, 吴家胜, 王天明, 李安宁, 吴迪, 孙晓菲, 石荣, 马越鸣. 小鼠体内金芪降糖胶囊多成分药代动力学研究J. 药学学报, 2025, 60(4): 1084-1092. DOI: 10.16438/j.0513-4870.2024-0812
TIAN Tian, LI Yuan-yuan, WU Jia-sheng, WANG Tian-ming, LI An-ning, WU Di, SUN Xiao-fei, SHI Rong, MA Yue-ming. Multi-component pharmacokinetics of Jinqi Jiangtang Capsule in miceJ. Acta Pharmaceutica Sinica, 2025, 60(4): 1084-1092. DOI: 10.16438/j.0513-4870.2024-0812
Citation: TIAN Tian, LI Yuan-yuan, WU Jia-sheng, WANG Tian-ming, LI An-ning, WU Di, SUN Xiao-fei, SHI Rong, MA Yue-ming. Multi-component pharmacokinetics of Jinqi Jiangtang Capsule in miceJ. Acta Pharmaceutica Sinica, 2025, 60(4): 1084-1092. DOI: 10.16438/j.0513-4870.2024-0812

小鼠体内金芪降糖胶囊多成分药代动力学研究

Multi-component pharmacokinetics of Jinqi Jiangtang Capsule in mice

  • 摘要: 金芪降糖方源自经典方剂千金黄连丸, 是最常用的治疗糖尿病的中药复方。金芪降糖胶囊(Jinqi Jiangtang Capsule, JQJTC) 为其临床常用剂型之一, 但其体内多成分的药动学规律尚不清楚。本研究首先建立了稳定、可靠的小鼠血浆与肝脏中JQJTC多成分的超高效液相色谱–三重四级杆串联质谱法(UPLC-MS/MS) 定量分析方法; 并测定了2型糖尿病小鼠灌胃给予JQJTC后16种成分在血浆和肝脏中浓度变化, 分析了动力学规律。结果表明, 建立的UPLC-MS/MS方法符合生物样品测定的要求; 小鼠灌胃给予JQJTC后, 生物碱类成分、有机酸类成分、黄酮类及皂苷类成分均可吸收入血, 16种成分的吸收与消除速度、向肝脏的转运速度和暴露水平存在明显差异; 且生物碱类成分、毛蕊异黄酮苷及苷元、芒柄花素和环黄芪醇在肝脏中的暴露显著高于在血浆中的暴露。研究结果为JQJTC进一步的药效物质研究提供了基础。所有实验动物的使用已获得上海中医药大学实验动物伦理委员会批准(批准号: PZSHUTCM2401310001)。

     

    Abstract: Jinqi Jiangtang Capsule (JQJTC) is one of the commonly used dosage forms of Jinqi Jiangtang formula, derived from the classic Qianjin Huanglian Pill, which is widely used in the treatment of diabetes mellitus. However, its pharmacokinetics is not still unclear. In this study, a stable and reliable method for the quantitative analysis of multiple components from JQJTC in mouse plasma and liver was established by ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Then, the concentration changes of 16 components from JQJTC in plasma and liver of type 2 diabetic mice were determined and the kinetics was analyzed. The results demonstrated that the established UPLC-MS/MS method met the requirements for the determination of biological samples. The alkaloids, organic acids, flavonoids, and saponins were absorbed into mouse blood after JQJTC was administered by gavage, and there were significant differences in the rates of absorption, transport into liver and elimination and exposure levels of 16 components in plasma and liver. And the exposure of alkaloids, calycosin-7-glucoside and its glycosides, formononetin, and cycloastragenol in the liver were significantly higher than that in the plasma. The results provided a basis for further research on the pharmacodynamic substances of JQJTC. The use of all experimental animals has been approved by the Ethics Committee of Laboratory Animal of Shanghai University of Traditional Chinese Medicine (No. PZSHUTCM2401310001).

     

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