The results of the pharmacokinetic studies of Carsil, performed on laboratory animals and healthy volunteers after oral administration in doses of 0.20 and 100 mg/kg, and intravenous administration in doses of 20, 40 and 100 mg/kg, indicated an intensive distribution of the drug in the human body. The low plasma levels of Carsil detected resulted from its rapid passage from the plasma to the other body fluids and tissues.
In studies with 14C-labeled silybin (the principal ingredient of silymarin), highest levels of silybin were detected in the liver, and rather insignificant amounts in the kidneys, lungs, heart and other organs.
Carsil is eliminated predominantly with bile in the form of conjugates, and insignificant amounts with urine. Thirty-five percent of the dose administered is excreted with bile for 24 hours, after a single oral dose of 20 mg/kg Carsil.
The above pharmacokinetic features of Carsil favor its therapeutic activity in the therapy of liver diseases.
The comparison of the major pharmacokinetic parameters of Carsil indicates that proportionality between the dose administered and the plasma level detected exists with doses of 40 mg/kg.
This is an indication that administration of very high single doses of the drug is not justified.
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