Oral bioavailability of active principles from herbal products in humans. A study on Hypericum perforatum extracts...

The oral absorption of two known active principles of Hypericum perforatum, namely hyperforin and hypericin, was studied in an open, single dose, two-way, randomized, cross-over study involving 12 healthy subjects (six males and six females). Alcoholic Hypericum extract (300 mg, containing 5% hyperforin and 0.3 % hypericin) was administered in the morning after 12 hours fasting. The formulation was administered as softgel capsules containing, inter alia, soya oil together with the herbal extract. A second standard formulation in two piece hard gelatin capsules was also used for comparison purposes. Blood was sampled from the subjects at different times after drug administration and the plasma was analysed according to published analytical methods for the determination of hyperforin and hypericin. Peaks of plasma concentration, Cmax of hyperforin were 168.35 ng/ml +/- 57.79 for the soft gelatin formulation (CV=34.32, n=12) and 84.25 ng/ml +/- 33.51 for the hard gelatin capsule (CV=39.77, n=12). The Tmax values for hyperforin were 2.50 h +/- 0.83 for the soft gelatin formulation compared to 3.08 h +/- 0.79 for the reference formulation, whereas the total AUC were respectively 1482.7 h x ng/ml +/- 897.13 and 583.65 h x ng/ml +/- 240.29. As for hypericin, plasma levels were detectable in approximately half of the subjects treated. However also in this case the soft gelatin capsules exhibited a higher individual absorption when compared with the corresponding data for the hard gelatin capsules.