Pharmacokinetics, intestinal absorption and microbial metabolism of single platycodin D in comparison to Platycodi radix extract

Jinjun Shan; Jiashuang Zou; Tong Xie; An Kang; Wei Zhou; Haishan Deng; Yancao Mao; Liuqing Di; Shouchuan Wang

Articles

Abstract

Pharmacognosy Magazine,2015,11,44,750-755.

DOI:10.4103/0973-1296.165576

Published:September 2015

Type:Original Article

Authors:

Author(s) affiliations:

Jinjun Shan¹, Jiashuang Zou², Tong Xie³, An Kang², Wei Zhou³, Haishan Deng³, Yancao Mao², Liuqing Di¹, Shouchuan Wang³
¹ Jiangsu Key Laboratory of Pediatric Respiratory Disease, Institute of Pediatrics; Jiangsu Engineering Research Center for Efficient Delivery System of TCM, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
² Jiangsu Engineering Research Center for Efficient Delivery System of TCM, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
³ Jiangsu Key Laboratory of Pediatric Respiratory Disease, Institute of Pediatrics, Nanjing 210023, China

Abstract:

Background: Platycodi radix, the dried root of Platycodon grandiflorum A. DC, has been widely used as food and herb medicine for treating cough, cold and other respiratory ailments, and platycodin D (PD) is one of the most important compounds in Platycodi Radix. Objective: The purpose of this study was to compare the pharmacokinetic characteristics, intestinal absorption and microbial metabolism of PD in monomer with that in Platycodi radix extract (PRE). Materials and Methods: In the pharmacokinetic study, the concentrations of PD in rat plasma were determined by ultra-performance liquid chromatography-tandem mass spectrometry and the main pharmacokinetic parameters were calculated by data analysis software (DAS). Besides, in vitro Caco-2 cells and fecal lysate were performed to investigate the intestinal absorption and metabolism, respectively. Results: The results from pharmacokinetics showed that the area under the curve, the peak concentration the time to reach peak concentration and mean residence time of PD in PRE were enhanced significantly compared with that in single PD. Caco-2 cells transport study indicated that the absorption of PD both in monomer and in PRE were poor owning that the permeability of PD were <1/10 ⁶ cm/s. The hydrolysis degree of PD in PRE was significantly lower than that in monomer PD in fecal lysate, which might be illustrated by the other ingredients in PRE influenced the hydrolysis of PD via gut microbiota. Conclusion: These findings indicated that the difference of microbial metabolism, not apparent absorption in intestine for PD between in monomer and in PRE contributed to their pharmacokinetic difference.