Influence of Piperine on the Pharmacokinetics of Curcumin in Animals and Human Volunteers.

 

Planta Med. 1998; 64(4):353-6.

 

Curcuminoids, despite showing excellent activity in inhibiting the expression of inflammatory cytokines and inhibition of free radicals, due to its low bioavailability and rapid transformation in the body, has low medicinal application. In the present study bioavailability of Curcumin has been evaluated in presence of patented black pepper extract BioPerine® in both animals and humans.

 

Objective:

To see the effect of use the Piperine enriched black pepper extract on bioavailability of Curcuminoids in the body.

 

Study Design:

In the animal study, 96 albino wistar rats were divided in two sex and weight matched groups with one group being administered orally Curcumin and Piperine at the dosage 2 g/kg and 20 mg/kg, respectively while the other group received only Curcumin. Control rats received water only. Blood samples were collected from both groups at following time interval 0, 0.25, 0.5, 0.756, 1, 2, 3, 4, 5 and 6h.

Similarly 10 healthy male volunteers in a randomized crossover trial were administered Curcumin (2 g) and Curcumin (2 g) and Piperine (20 mg) combination to determine comparative bioavailability of Curcumin in both groups. The blood samples were drawn at 0.0, 0.25. 0.5, 1, 2, 3, 4, 5 and 6 h post administration.

The parameters evaluated during the trial (i.e. at baseline and at the end of the study) included fasting glucose level and lipid profile (total cholesterol, LDL-C, HDL-C and Triglycerides) along with liver and kidney function tests.

 

Results:

  • Animal study results showed that Piperine produced a higher serum concentration of Curcumin at 1 and 2 h (1.55 ±0.21 µg/ml and 1.5±0.25 µg/ml) than when Curcumin alone at 0.75 h (1.0 ±0.26 µg/ml) was administered.
  • The humans study showed that Piperine was well tolerated when given with Curcumin. The serum levels of Curcumin when given alone was very low or undetectable whereas when given with Piperine, the Curcumin showed the serum levels of 0.18±0.16 µg/ml with Cmax at 0.75h. The relative bioavailability of curcumin when Piperine was given was therefore 2000%. [Figure 1].

 

Conclusion:

Piperine enhances the oral bioavailability of curcumin in both animals and humans at doses which are devoid of adverse side effects. The bioavailability of curcumin in presence of Piperine was enhanced by 2000% in human. 

 

 

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