Pharmakokinetik und Metabolismus des 20-Hyroxyecdysons im Menschen

Ecdysteroids are steroid hormones, which occur in arhtropods and in plants. They are ingested in relevant amounts by humans. Several studies claim, that there is a significant effect on the human organism. Ecdysteroids are used in agriculture, for medication purposes and as doping agents. Actually they are not listed as a forbidden substance by the International Olympic Committee (IOC). Aim of this doctoral thesis was to examine basic pharmacological characteristics of ecdysteroids. 20 mg of 20-Hydroxyecdysone was given to a subject while urinary samples were collected during the following 48 hours for further analysis. Analysis was done by HPLC, for the selective proof of 20-Hydroxyecdysone EIA was used. LCMS was used for identification of the molecular structures. Due to this study it was possible to optimize sample preparation of urinary samples for different analytical procedures, to reveal pharmacokinetics of 20-Hydroxyecdysone in humans and to find at least one metabolite of this substance. Division between two solvents and following solid-phase extraction seemed to be the most suitable sample processing for analysis via TLC, HPTLC, HPLC and LCMS. Pharmacocinetics of 20-Hydroxyecdysone showed two peaks at four to five hours and 21 hours after ingestion. 6% of the ingested amount of 20-Hydroxyecdysone could be found as immunoreactive compounds in the urine. Concerning metasbolism, 20-Hydroxyecsyone itself and 14-Deoxy-20-Deoxyecdysone were found in samples four to five hours after oral admission. After 21 hours only 20-Hydroxyecdysone could be found as well as a substance whith a molecular weight 16 units higher than 20-hydroxyecdysone, probably due to hydroxylation.