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.
Highlights
White pepper (Piper nigrum L.), known as “the king of spices,” is important in daily diet which helps digestion and eliminates odor and greasiness [1]
The t1/2 of puerarin was increased and CL was reduced in the presence of white pepper, there was no statistical significance (P > 0.05). These results indicated that the pharmacokinetic profiles of puerarin given by intravenous administration were changed by pretreatment with white pepper given orally, while it was not altered by piperine
Pretreatment with pepper delayed the t1/2 and reduced the CL of puerarin as compared with control. These findings indicated that pepper could inhibit elimination of puerarin given intravenously, which might be due to the decrease in renal excretion or suppression of cytochrome P450 (CYP450) enzymatic metabolizing activities
Summary
White pepper (Piper nigrum L.), known as “the king of spices,” is important in daily diet which helps digestion and eliminates odor and greasiness [1]. This spice has been used as herbal medicines, preservatives, dietary supplements, and fragrances [2]. Piperine (1-piperoyl piperidine), an active ingredient in white pepper, has numerous biological effects such as anti-inflammatory, antioxidant, antimutagenic, and antitumor activities [2, 4]. Piperine has been reported to promote the bioavailability of drugs such as curcumin [5], phenytoin [6], propranolol, and theophylline [7]. Its bioenhancement is due to its inhibitory activity on drug metabolizing enzymes and/or P-glycoprotein mediated drug efflux [8, 9]
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