[Comparative pharmacokinetics of paracetamol in humans following single oral and rectal administration (author's transl)].
The pharmacokinetic behaviour of N-acetyl-p-aminophenol (paracetamol) after single dose applications of 500 mg and 1000 mg dosages in the form of liquids, tablets and suppositories was compared. The estimation of the pharmacokinetic constants by a simultaneous curve fitting with a direct search procedure, based on an open two-compartment model, showed for the liquid as well as for the tablet formulation a good conformable and dosage proportional behaviour of the relative bioavailability. In opposite to the oral application, the suppositories had a significantly reduced invasion kinetics with a comparable elimination kinetics characterized by a lowering of Cmax and an increase of Tmax-values with comparable AUCs. The calculation of collapse-coefficients showed, with the exception of one suppository formulation, for all administrations a pharmacokinetic behaviour deviating from an open one-compartment model. The clinical consequences resulting from the pharmacokinetic behaviour of the different galenic formulations and routes of administrations are discussed.
D000082:Acetaminophen / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D000284:Administration, Oral; D000328:Adult; D006801:Humans; D007700:Kinetics; D008297:Male; D012007:Rectum; D013488:Suppositories; D013997:Time Factors
D013488:Suppositories; D000082:Acetaminophen
Vergleichende Humanpharmakokinetik von Paracetamol nach oraler und rektaler Einmalapplikation.