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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
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Molecules 2014, 19(5), 5624-5633; https://doi.org/10.3390/molecules19055624
Received: 28 March 2014 / Revised: 28 April 2014 / Accepted: 28 April 2014 / Published: 30 April 2014
(This article belongs to the Section Natural Products Chemistry)
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. View Full-Text
Keywords: linarin; piperine; P-glycoprotein; intestinal permeability; pharmacokinetics linarin; piperine; P-glycoprotein; intestinal permeability; pharmacokinetics
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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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