Untersuchungen zur Elimination von Silymarin bei cholezystektomierten Patienten

Abstract

The biliary elimination of silybin, the main component of Silymarin, was examined in 11 cholecystectomized patients with T-drainage after a 3 to 5 day-administration of 140 mg of silymarin (Legalon®, sugarcoated tablets) t. i. d. The elimination of silybin was measured in 12- or 24-h-intervals. Six of these 11 patients received in addition one day before and one day after the repeated dose-period a single dose of 140 mg silymarin, in order to test the influence of repeated application on the biliary elimination kinetic.

After repeated intake the steady state of silybin elimination was reached by the second day at the latest. The daily silybin quantities lay between 10 and 40 mg and were nearly independent of bile flow, which was subject to no great intraindividual variations.

Kinetic studies showed that after repeated intake of silymarin the elimination of silybin was approx. twice as high as that following the first single intake. This increased elimination, however, stopped after 12 h. 48 h after the last silymarin intake silybin excretion was very low and after 72 h silybin was no longer detectable in the bile. All these observation show, that silybin does not accumulate.

The silybin concentrations lay between 20 and 70 µg/ml of the day and the night bile (collecting intervals of 12 h) and correspond to the pharmacologically effective concentrations of 10^-5 and 10^-4 mol/l obtained in animal experiments. The intraindividual differences between the silybin concentrations in the day and night bile were relatively small, so that with the recommended doses therapeutically effective silybin concentrations can always be expected in the bile.

Key Word Index

Silybum marianum - Compositae - Silymarin - Silybin - Silychristin - Elimination - Cholezystektomierte Patienten