Resorption, Verteilung und Galle-Ausscheidung einiger 3H-markierter Derivate des Helveticosols
SchlüsselwörterHerzglykosid Radioaktive Markierung Pharmakokinetik Arzneimittelmetabolismus Resorption
Absorption, Tissue Distribution and Biliary Excretion of some 3H-labelled Derivatives of Helveticosol.
Absorption was calculated from the percentage of the injected radioactivity which disappeared within two hours from an intestinal loop. With helveticosol as well as its mono- and dimethylether, there was a good agreement between this estunate of absorption and that derived from the relation of equiactive doses on intravenous and intraduodenal application. The absorption of diacetyl- and di-propionyl-helveticosol was less than expected from their activity on enterai application. This was explained by hydrolysis into more active metabolites.
The distribution volume, calculated from the content of the body and the blood level, was lower after intraduodenal than after intravenous application. This was difficult to explain since there was no difference in the distribution coefficients of liver and heart and between the metabolites found in the blood after intravenous infusion or intraduodenal injection. There was no significant difference between the distribution volume after intraportal and intravenous infusion of monomethyl-helveticosol.
Biliary excretion was measured after intravenous and intraduodenal administration and correlated with the mean blood and tissue levels. The glycosides which were best absorbed from the intestine were excreted most rapidly in the bile.
Key-WordsCardioglycoside Labelled Compound Drug Metabolism Pharmacokinetics Absorption Gastrointestinal
Unable to display preview. Download preview PDF.
- Dost, F.H., u. E. Gladtke: Ein Verfahren zur Ermittlung der Bilanz einverleibter Stoffe ohne Kenntnis der Ausscheidung. Z. klin. Chem. 1, 14 (1963).Google Scholar
- Fleishman, D.G., and V.V. Glazunow: An external standard as a means of determining the efficiency and background of a liquid scintillator. Pribory i Tekhn. Eksperim. 7, 55 (1962).Google Scholar
- Hayes, F.N., A.G. Schrodt, and J.A. Gibbs: Application of external standardization to automatic liquid scintillation counting, in Advances in Tracer Methodology, Ed. S. Rothschild, Vol. 3, Proc. 9th and 10th Symp. on Advances in Tracer Methodology, New York: Plenum Publ. Corp. 1966.Google Scholar
- Schöninger, E.: Eine mikroanalytische Schnellbestimmung von Halogen in organischen Substanzen. Mikrochim. Acta 1955, 123.Google Scholar