Li Shu-Qi, Dong Shu, Su Zhi-Heng, Zhang Hong-Wu, Peng Jing-Bo, Yu Chang-Yuan, Zou Zhong-Mei
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China.
Guangxi Medical University, Nanning 530021, China.
Metabolites. 2013 Sep 30;3(4):867-80. doi: 10.3390/metabo3040867.
Chaihu-Shu-Gan-San (CSGS), a traditional Chinese medicine (TCM) formula containing seven herbal medicines, has been used in the clinical treatment of gastritis, peptic ulcer, irritable bowel syndrome and depression in China. In order to explore the interaction between naringin and other constituents in CSGS, the pharmacokinetic difference of naringin in rats after oral administration of CSGS aqueous extract and naringin alone was investigated. The pharmacokinetic parameters of naringin in rats were achieved by quantification of its aglycone, naringenin by LC-MS/MS method. The double peaks phenomenon was observed in both serum profiles of rats after orally administered CSGS aqueous extract and naringin alone. However, the T1/2b was significantly decreased in rats given CSGS aqueous extract compared with naringin alone, and the mean residence time (MRT) and the area under the serum concentration-time curve (AUC0-τ) were higher than those of naringin, which indicated that naringin in CSGS had higher bioavailability, longer term efficacy and somewhat faster metabolism and excretion than those of naringin. The results suggested that certain ingredients co-exist in CSGS could influence pharmacokinetic behavior of naringin. This also provides a reference for human studies.
柴胡疏肝散(CSGS)是一种含有七种草药的中药配方,在中国已被用于胃炎、消化性溃疡、肠易激综合征和抑郁症的临床治疗。为了探究柚皮苷与柴胡疏肝散中其他成分之间的相互作用,研究了大鼠口服柴胡疏肝散水提取物和单独口服柚皮苷后柚皮苷的药代动力学差异。通过液相色谱-串联质谱法(LC-MS/MS)对柚皮苷的苷元柚皮素进行定量分析,得出大鼠体内柚皮苷的药代动力学参数。在大鼠口服柴胡疏肝散水提取物和单独口服柚皮苷后的血清图谱中均观察到双峰现象。然而,与单独给予柚皮苷相比,给予柴胡疏肝散水提取物的大鼠的T1/2b显著降低,平均驻留时间(MRT)和血清浓度-时间曲线下面积(AUC0-τ)均高于柚皮苷,这表明柴胡疏肝散中的柚皮苷比单独的柚皮苷具有更高的生物利用度、更长的疗效以及更快的代谢和排泄速度。结果表明,柴胡疏肝散中某些共存成分可能会影响柚皮苷的药代动力学行为。这也为人体研究提供了参考。