[Bioavailability of etilefrine from Thomasin and Thomasin sustained-release tablets].
In 6 healthy volunteers absorption and elimination of etilefrine were studied in cross-over after intake of 20 mg each of a solution (A) and tablet (B) (Thomasin) or after intake of 25 mg as a sustained-release tablet (C; Thomasin retard). Etilefrine and its sulfoconjugate were measured by the GC technique in plasma and urine. From the data obtained the AUC-(plasma) and CUE-values (urine) were calculated. Peak plasma levels of 10 to 25 (A) and 6 to 13 ng . ml-1 were observed 30 min after intake. The concentrations decreased to the lower detection limit (less than 2 ng . ml-1) 2 h after intake. Plasma peak levels of 5 ng . ml-1 were measured 1-2 h after intake of the sustained-release form (C). The etilefrine plasma level decreased more slightly (C) than after intake of the other formulations (A, B). The etilefrine conjugate reached plasma peak concentrations of 600 ng . ml-1 1 h (A, B) or 2 h (C) after intake. A mean bioavailability of 70 and 58 per cent (Thomasin) or of 78 and 108 per cent (Thomasin retard) was calculated by comparison of the corresponding AUC- and CUE-values of the total etilefrine.
Haustein
K O
KO
Hüller
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G
D000328:Adult; D001682:Biological Availability; D002849:Chromatography, Gas; D003692:Delayed-Action Preparations; D005039:Etilefrine / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D005260:Female; D006801:Humans; D007700:Kinetics; D008297:Male; D010656:Phenylephrine / Q000031:analogs & derivatives*; D013607:Tablets
D003692:Delayed-Action Preparations; D013607:Tablets; D010656:Phenylephrine; D005039:Etilefrine
Zur Bioverfügbarkeit von Etilefrin aus Thomasin- und Thomasin retard-Tabletten.