Sun Lili, Ding Feifei, You Guangjiao, Liu Han, Wang Meng, Ren Xiaoliang, Deng Yanru
School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China.
Pharmaceutics. 2017 Dec 29;10(1):4. doi: 10.3390/pharmaceutics10010004.
JinQi Jiangtang (JQJT) tablets, a Chinese patent medicine approved by the State Food and Drug Administration, are composed of Coptidis Rhizoma, Astragali Radix, and Lonicerae Japonicae Flos, and have a significant effect on diabetes. Coptidis Rhizoma is monarch drug in the prescription. The aim of the present study was to investigate and compare the pharmacokinetics of multiple ingredients from JQJT tablets and Coptidis Rhizoma extract (CRE) following oral administration in rats. Five alkaloids: coptisine chloride, epiberberine chloride, berberine chloride, jatrorrhizine chloride, and palmatine chloride, were simultaneously determined in rat plasma using established and validated ultra-high performance liquid chromatography mass spectrometry (UPLC-MS/MS). Significant pharmacokinetic differences were observed for the five alkaloids after a single administration of CRE and JQJT tablets. Compared with CRE, the C values of palmatine chloride and jatrorrhizine chloride were decreased significantly, the AUC values of four alkaloids (all except jatrorrhizine chloride) were notably decreased, and the mean residence times of all five alkaloids were significantly decreased after administration of JQJT tablets. The results indicated that the absorption characteristics of the five alkaloids from Coptidis Rhizoma would be influenced by the compatibility of Astragali Radix or Lonicerae Japonicae Flos from JQJT tablets, such that absorption was inhibited and elimination was accelerated. In conclusion, the developed strategy was suitable for the comparison of five alkaloids from JinQi Jiangtang tablets and its monarch drug, which could be valuable for compatibility studies of traditional Chinese medicines.
津芪降糖（JQJT）片是一种经国家食品药品监督管理总局批准的中成药，由黄连、黄芪和金银花组成，对糖尿病有显著疗效。黄连是该方剂中的君药。本研究的目的是研究并比较大鼠口服津芪降糖片和黄连提取物（CRE）后多种成分的药代动力学。采用已建立并验证的超高效液相色谱-质谱联用（UPLC-MS/MS）法同时测定大鼠血浆中的五种生物碱：盐酸黄连碱、表小檗碱、盐酸小檗碱、盐酸药根碱和盐酸巴马汀。单次给予CRE和津芪降糖片后，观察到这五种生物碱存在显著的药代动力学差异。与CRE相比，给予津芪降糖片后，盐酸巴马汀和盐酸药根碱的C值显著降低，四种生物碱（除盐酸药根碱外）的AUC值显著降低，且五种生物碱的平均驻留时间均显著缩短。结果表明，黄连中五种生物碱的吸收特性会受到津芪降糖片中黄芪或金银花配伍的影响，从而抑制吸收并加速消除。总之，所建立的方法适用于比较津芪降糖片中五种生物碱及其君药，这对中药配伍研究具有重要价值。
