White Pepper and Piperine Have Different Effects on Pharmacokinetics of Puerarin in Rats

Abstract

This study attempted to explore the effects of white pepper and its major component piperine on puerarin administered to rats. Pharmacokinetic parameters of puerarin in rats were determined by oral administration (400 mg/kg) or intravenous injection (40 mg/kg) of puerarin, pretreated with or without white pepper and piperine given orally. Compared to the control group given oral puerarin only, the combined use of piperine (10 or 20 mg/kg) increased the C max of puerarin by 1.30-fold or 1.64-fold and the AUC0–∞ by 133% or 157%, respectively. In contrast, coadministration of white pepper (125 or 250 mg/kg) decreased oral absorption of puerarin to 83% or 74%, respectively. On the other hand, pretreatment with piperine orally did not alter the intravenous pharmacokinetics of puerarin, while the AUC of puerarin after intravenous administration was increased by pretreatment with white pepper. The results indicate that pretreatment with piperine or pepper exerts different effects on pharmacokinetics of puerarin administrated via intragastric and intravenous routes. Therefore, it is suggested that the combined application of piperine or white pepper with puerarin should be carefully monitored for potential diet-drug interactions.

Piperine-A Major Principle of Black Pepper: A Review of Its Bioactivity and Studies

“…Also, piperine in the form of pro-nanolipospheres was found to be efficient in overcoming the limitations of variable and low oral bioavailability of cannabinoids tetrahydrocannabinol and cannabidiol [159]. Piperine increases the bioavailability of emodin in rats [160], linarin [161], β-lactam antibiotics [162], fexofenadine [163], ginsenoside Rh2 [164], (-)-epigallocatechin-3-gallate [165], puerarin [166], oxyphenylbutazone [167] and diltiazem [168]. In a study on human cancer cell line (monolayers of Caco-2 cells), Bhardwaj et al [169] found piperine to be an inhibitor of both human P-glycoprotein and CYP3A4, and that it also inhibited transport of the P-glycoprotein substrates digoxin and cyclosporine.…”

Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats

“…Therefore, due to the dual inhibitory effect on both enzymes and membrane transporters, PIP was considered as a potent bioavailability enhancer for the substrates of CYP 3As and P-gp such as rosuvastatin, peurarin, diltiazem, domperidone etc. [19][20][21][22][23].…”

“…However, for most of the herb-drug interaction studies, the pharmacokinetic study only focused on the determination of western drugs such as DOX, whereas the pharmacokinetics profile of PIP has barely been investigated. Since PIP is also bioactive and usually used in relatively high dose (10 or 20 mg/kg) in combination therapy with western drugs, it is of great importance to monitor its concentrations in order to avoid potential toxicities induced by food-drug or herb-drug interactions [20,21]. Although the plasma concentrations of PIP and DOX have been separately determined by UFLC-ESI-MS/MS or LC-MS/MS [10,28], they were never quantified simultaneously in the previous studies.…”

Pharmacokinetic Interaction between Magnolol and Piperine in Rats

“…The dose levels of piperine have been selected based on our previous pharmacokinetic studies [9]. The dose of magnolol was chosen based on the clinical use and our preliminary experiment.…”

“…Stability was checked by comparing the measured results with those of the freshly prepared samples of the same concentration under different storage conditions: short-term stability at room temperature for 4 h; long-term stability at -20 °C for 7 days; after three freezethaw cycles [9,10].…”