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Influence of Piperine on the Pharmacokinetics of Curcumin in Animals and Human Volunteers
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1998
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Curcumin’s therapeutic potential is limited by poor bioavailability due to rapid hepatic and intestinal metabolism. Researchers sought to determine whether co‑administration of piperine could enhance curcumin bioavailability in rats and healthy volunteers. Piperine, a known inhibitor of hepatic and intestinal glucuronidation, was administered alongside curcumin to evaluate its pharmacokinetic impact. In rats, piperine increased serum curcumin levels, prolonged Tmax, reduced clearance, and raised bioavailability by 154 %; in humans, it elevated undetectable or low serum levels to measurable concentrations within 0.25–1 h and boosted bioavailability by 2000 %, with no adverse effects.
The medicinal properties of curcumin obtained from Curcuma longa L. cannot be utilised because of poor bioavailability due to its rapid metabolism in the liver and intestinal wall. In this study, the effect of combining piperine, a known inhibitor of hepatic and intestinal glucuronidation, was evaluated on the bioavailability of curcumin in rats and healthy human volunteers. When curcumin was given alone, in the dose 2 g/kg to rats, moderate serum concentrations were achieved over a period of 4 h. Concomitant administration of piperine 20 mg/kg increased the serum concentration of curcumin for a short period of 1-2h post drug. Time to maximum was significantly increased (P<0.02) while elimination half life and clearance significantly decreased (P<0.02), and the bioavailability was increased by 154%. On the other hand in humans after a dose of 2g curcumin alone, serum levels were either undetectable or very low. Concomitant administration of piperine 20 mg produced much higher concentrations from 0.25 to 1h post drug (P<0.01 at 0.25 and 0.5h; P < 0.001 at 1 h), the increase in bioavailability was 2000%. The study shows that in the dosages used, piperine enhances the serum concentration, extent of absorption and bioavailability of curcumin in both rats and humans with no adverse effects.