The medicinal properties of curcumin obtained from Curcuma longa L. ca
nnot be utilised because of poor bioavailability due to its rapid meta
bolism in the liver and intestinal wall, In this study, the effect of
combining piperine, a known inhibitor of hepatic and intestinal glucur
onidation, was evaluated on the bioavailability of curcumin in Fats an
d healthy human volunteers. When curcumin was given alone, in the dose
2 g/kg to rats, moderate serum concentrations were achieved over a pe
riod of 4 h. Concomitant administration of piperine 20 mg/kg increased
the serum concentration of curcumin for a short period of 1-2h post d
rug. Time to maximum was significantly increased (P < 0.02) while elim
ination half life and clearance significantly decreased (P < 0.02), an
d the bioavailability was increased by 154%. On the other hand in huma
ns after a dose of 2g curcumin alone, serum levels were either undetec
table or very low. Concomitant administration of piperine 20 mg produc
ed much higher concentrations from 0.25 to 1 h post drug (P < 0.01 at
0.25 and 0.5 h; P < 0.001 at 1 h), the increase in bioavailability was
2000 %. The study shows that in the dosages used, piperine enhances t
he serum concentration, extent of absorption and bioavailability of cu
rcumin in both rats and humans with no adverse effects.