Abstract

Puerariae Lobatae Radix, known as Gegen in Chinese, is widely used to treat cardiovascular diseases, diabetes, and many other chronic illnesses. Flavonoids are the main active components in Gegen and are found in high concentrations in soybeans. Few studies, however, have focused on the effects of flavonoid-rich food on the absorption of Gegen. Here, we report an in vivo pharmacokinetic study on rats to explore the effects of soybean milk on the absorption of Gegen and an in vitro Ussing chamber study of puerarin intestinal transmembrane absorption. Area under the plasma concentration-time curve (AUC0–t) and maximum plasma concentration (Cmax) values of puerarin in rats were significantly decreased after drinking soybean milk, when taking Gegen decoction or a Gegen patent medicine (P < 0.01). In the Ussing chamber experiment, cumulative transmission (Qtn) after 2 h and apparent permeability coefficient (Papp) were lower in the puerarin-daidzin and puerarin-soybean milk solution groups than in the puerarin group. Daidzin in soybean milk inhibited the transmembrane transport of puerarin, resulting in decreased bioavailability of puerarin in Gegen. The results of this study strongly suggest that Gegen should not be taken with flavonoid-rich food, particularly soybean products.

Highlights

  • Numerous studies have shown that simultaneous administration with food either promotes or inhibits drug absorption, altering pharmacokinetics (PK) and/or pharmacodynamics of drugs [1,2,3,4,5,6]

  • Puerarin plasma concentrations were significantly higher in Gegen decoction group (G group) than in GS group rats at most time points

  • Clearance of puerarin in rats was accelerated after drinking soybean milk, with mean resident time (MRT) and t1/2 decreasing and Vz/F and CLz/F values of puerarin increasing

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Summary

Introduction

Numerous studies have shown that simultaneous administration with food either promotes or inhibits drug absorption, altering pharmacokinetics (PK) and/or pharmacodynamics of drugs [1,2,3,4,5,6]. The United States Food and Drug Administration (FDA) issued a guideline in 2002 stating recommendations for the design and methodology of studies on food-drug interactions [7]. These studies are critical in evaluating the appropriate dosing, timing, and formulation of new western drug candidates. Chemical constituents of traditional Chinese medicines (TCMs) are complex. Many of these compounds are present in food eaten daily

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