Bioavailability of a new liquid formulation of penicillin V (Isocillin syrup) and the influence of ethanol on bioavailability of penicillin V.
In an open, randomized four-way crossover study, four different formulations of penicillin V each containing 1.2 mega units were tested: A) new liquid formulation of Isocillin syrup, B) new liquid formulation of Isocillin syrup plus ethanol, C) commercially available penicillin V syrup containing ethanol as solubilizer and D) Isocillin film tablets. Six male and eight female healthy volunteers participated in the study. Serum concentration and urinary excretion of penicillin V were measured by HPLC or bioassay. The new liquid formulation of Isocillin syrup showed highest Cmax and AUC values. Correspondingly, urinary excretion of the new liquid formulation of Isocillin syrup was highest (38% of the given dose). Mean pharmacokinetic data of the new liquid formulation of Isocillin syrup were: tmax (h) = 0.81, Cmax (mg/l) = 9.92, AUC0-8h (mgh/l) = 13.67, lambda z (h) = 0.68, Cltot/f (ml/min) = 964. Ethanol (4.6%) had no absorption-enhancing effects. From a clinical point of view, all four formulations investigated in this trial showed serum concentrations well above bactericidal concentrations (greater than 1 mg/l) for more than 3 h. Although the interindividual variability of serum levels was high, the levels observed would guarantee therapeutic efficacy against penicillin sensitive bacterial strains.
Bauer
B
B
Department of Clinical Research, Hoechst AG, Frankfurt, FRG.
Malerczyk
V
V
Roethig
H J
HJ
D000328:Adult; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D000431:Ethanol / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D010404:Penicillin V / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine
D000431:Ethanol; D010404:Penicillin V