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Comparative Pharmacokinetics of Naringin in Rat after Oral Administration of Chaihu-Shu-Gan-San Aqueous Extract and Naringin Alone

机译:柴胡-疏肝-甘-三水提取物和单独柚皮苷口服后大鼠柚皮苷的比较药代动力学

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摘要

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 T1/2β 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.
机译:含有七种草药的中药配方茶(Chuhu-Shu-Gan-San,CSGS)已在中国用于胃炎,消化性溃疡,肠易激综合症和抑郁症的临床治疗。为了研究柚皮苷与CSGS中其他成分之间的相互作用,研究了口服CSGS水提取物和柚皮苷单独后大鼠体内柚皮苷的药代动力学差异。柚皮苷在大鼠中的药代动力学参数通过LC-MS / MS方法定量测定其苷元,柚皮苷。口服CSGS水提取物和柚皮苷单独给药后,在大鼠血清中均观察到双峰现象。然而,与单独的柚皮苷相比,CSGS水浸提液大鼠的T1 /2β明显降低,并且平均停留时间(MRT)和血清浓度-时间曲线下面积(AUC0-τ)均比柚皮苷高。这表明与柚皮苷相比,CSGS中的柚皮苷具有更高的生物利用度,更长期的功效以及更快的代谢和排泄。结果表明,CSGS中某些成分共存可能会影响柚皮苷的药代动力学行为。这也为人类研究提供参考。

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