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Molecules 2017, 22(10), 1587; doi:10.3390/molecules22101587

Influence of Jiegeng on Pharmacokinetic Properties of Flavonoids and Saponins in Gancao

Jiangsu Key Laboratory of Pediatric Respiratory Disease, Institute of Pediatrics, Nanjing University of Chinese Medicine, Nanjing 210023, China
Jiangsu Engineering Research Center for Efficient Delivery System of TCM, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
The first two authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 19 August 2017 / Revised: 14 September 2017 / Accepted: 19 September 2017 / Published: 21 September 2017
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Jiegeng Gancao decoction, which is composed of Jiegeng and Gancao at a weight ratio of 1:2, was widely used for treating pharyngalgia and cough for thousands of years. Our previous work indicated that Gancao could increase the systemic exposure of platycodin D and deapio-platycodin D, two main components in Jiegeng. However, whether Jiegeng could alter the pharmacokinetics of the main compounds in Gancao is still unknown. Thus, the purpose of this study was to compare the oral pharmacokinetics of flavonoids and saponins from Gancao alone vs. after co-administration with Jiegeng. Furthermore, Caco-2 cell transport and fecal hydrolysis were investigated to explain the altered pharmacokinetic properties. Pharmacokinetics results suggested that the bioavailability of liquiritin, isoliquiritin, glycyrrhizin and its metabolite, glycyrrhetinic acid, could be improved while bioavailability of liquiritigenin and isoliquiritigenin deteriorated when co-administered with Jiegeng. The Caco-2 transport study showed no significant difference of the Papp values of the main components in Jiegeng Gancao decoction when compared with those in Gancao decoction (p > 0.05). The in vitro metabolism study suggested that saponins and flavonoids glycosides in Gancao were influenced and the metabolic characteristics of most ingredients were consistent with pharmacokinetic results, such as liquiritin and glycyrrhetinic acid. The hydrolysis of liquiritigenin and glycyrrhizin observed with fecal lysate in vitro appeared consistent with the oral pharmacokinetics. Based on experiments, the pharmacokinetic profiles of six components in Gancao were influenced by Jiegeng. The metabolic process might partially contribute to the altered pharmacokinetic behavior. The metabolism of some components of Gancao appeared to be inhibited when coadministered with Jiegeng, possibly by the Jiegeng constituent platycodin. View Full-Text
Keywords: Radix platycodonis; Glycyrrhiza uralensis Fisch; pharmacokinetics; absorption; metabolism Radix platycodonis; Glycyrrhiza uralensis Fisch; pharmacokinetics; absorption; metabolism

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Mao, Y.; Peng, L.; Kang, A.; Xie, T.; Xu, J.; Shen, C.; Ji, J.; Di, L.; Wu, H.; Shan, J. Influence of Jiegeng on Pharmacokinetic Properties of Flavonoids and Saponins in Gancao. Molecules 2017, 22, 1587.

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