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Molecules 2014, 19(5), 5624-5633; doi:10.3390/molecules19055624

Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats

School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China
Author to whom correspondence should be addressed.
Received: 28 March 2014 / Revised: 28 April 2014 / Accepted: 28 April 2014 / Published: 30 April 2014
(This article belongs to the Section Natural Products)
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Although linarin possesses diverse pharmacological activities, its poor oral bioavailability has been a concern for further development. The present study aimed to demonstrate the feasibility of improving the oral absorption of linarin in rats with a bioenhancer‒piperine. First, the intestinal permeability of linarin in the presence and absence of verapamil or piperine was investigated using an in situ single-pass rat intestinal perfusion method. A significant increase in the Peff when co-perfused with verapamil or piperine indicated that piperine effectively inhibited P-glycoprotein mediated efflux of linarin. Then, the pharmacokinetic profiles of linarin in rats after oral administration of linarin (50 mg/kg) alone and in combination with piperine (20 mg/kg) were determined using a validated LC–MS/MS method. The results showed that piperine increased the plasma exposure (AUC) of linarin by 381% along with an increase in the Cmax by 346% and the Tmax from 0.05 h to 0.2 h. The present study revealed that piperine significantly enhanced the oral absorption of linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of linarin.
Keywords: linarin; piperine; P-glycoprotein; intestinal permeability; pharmacokinetics linarin; piperine; P-glycoprotein; intestinal permeability; pharmacokinetics
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Feng, X.; Liu, Y.; Wang, X.; Di, X. Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats. Molecules 2014, 19, 5624-5633.

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