Abstract
The purpose of the present study was to assess the effect of resveratrol (RSV) on the pharmacokinetics of naproxen (NAP) in rats. A single dose of RSV 30mg/kg was administered once during treatment phase. A single dose of NAP 25mg/kg was administered after RSV treatment. The blood samples were collected after NAP dosing at predetermined time intervals and analyzed by HPLC. In comparison with the control, RSV pretreatment significantly enhanced maximum plasma concentration (Cmax), area under the curve (AUC), and half life (t1/2) and significantly decreased apparent oral clearance (CL/F) and apparent volume of distribution (Vd/F), while there was no significant change observed in time to reach maximum concentration (tmax) of NAP. The results suggest that the altered pharmacokinetics of NAP might be attributed to RSV-mediated inhibition of CYP1A2 enzyme. Therefore, combination therapy of NAP along with RSV may represent a novel approach to reduce dosage and results in reduced gastrointestinal side effects of NAP.
Highlights
Naproxen (NAP) (6-methoxy-α-methyl-2-napthalene acetic acid) is a non –steriodal anti-inflammatory drug effective in rheumatoid arthritis (Bowers et al.1975) and as analgesic (Ruedy and Mcullongh 1973)
Naproxen is oxidised to 6-0-desmethylnaproxen (6-DMN) and conjugated to naproxen acyl glucuronide and 6-0-desmethylnaproxen acylglucuronide (6-DMNG)
Our results suggest that oral administration of RSV significantly altered the pharmacokinetics and enhanced the bioavailability of naproxen through the inhibition of CYP1A2 enzyme in rats
Summary
Naproxen (NAP) (6-methoxy-α-methyl-2-napthalene acetic acid) is a non –steriodal anti-inflammatory drug effective in rheumatoid arthritis (Bowers et al.1975) and as analgesic (Ruedy and Mcullongh 1973). Naproxen is eliminated following biotransformation to glucuroconjugated and sulphate metabolites which are excreted in urine, with only a small amount of the drug being eliminated unchanged. The excretion of the 6-0-desmethylnaproxen metabolite conjugate may be tied to renal function, as accumulation occurs in end-stage renal disease. The combination of NAP along with RSV could be an alternative in the treatment of inflammatory diseases. NAP is an important anti-inflammatory drug with widespread use, and its administration receiving long-term therapy with herbal compounds or dietary supplements containing RSV may occur. The aim of this study was to evaluate the effect of RSV treatment on the pharmacokinetics of NAP in rats
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