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Effects of Piperine, Cinnamic Acid and Gallic Acid on Rosuvastatin Pharmacokinetics in Rats
Author(s) -
Basu Sudipta,
Jana Snehasis,
Patel Vandana B.,
Patel Hitesh
Publication year - 2013
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.4894
Subject(s) - piperine , pharmacokinetics , gallic acid , pharmacology , chemistry , bioavailability , oral administration , rosuvastatin , excretion , grapefruit juice , medicine , biochemistry , antioxidant
The purpose of this study was to investigate the potential pharmacokinetic interactions with natural products (such as piperine (PIP), gallic acid (GA) and cinnamic acid (CA)) and rosuvastatin (RSV) (a specific breast cancer resistance protein, BCRP substrate) in rats. In Caco 2 cells, the polarized transport of RSV was effectively inhibited by PIP, CA and GA at concentration of 50 μM. After per oral (p.o.) coadministration of PIP, CA and GA (10 mg/kg) significantly increased intravenous exposure (AUC last ) of RSV (1 mg/kg) by 73.5%, 62.9% and 53.3% ( p < 0.05), respectively than alone group (control). Compared with the control (alone) group, p.o. coadministration of PIP, CA and GA (10 mg/kg) significantly increased the oral exposure (AUC last ) of RSV (5 mg/kg) by 2.0‐fold, 1.83‐fold ( p < 0.05) and 2.34 ‐fold ( p < 0.05), respectively. Moreover, the cumulative biliary excretion of RSV (5 mg/kg, p.o.) was significantly decreased by 53.3, 33.4 and 39.2% at the end of 8 h after p.o. co‐administration of PIP, CA and GA (10 mg/kg), respectively. Taken together, these results indicate that the natural products such as PIP, CA and GA significantly inhibit RSV transport in to bile and increased the plasma exposure (AUC last ) of RSV. Copyright © 2012 John Wiley & Sons, Ltd.