[Clinical pharmacology of Bacampicillin in comparison to Ampicillin (author's transl)]

Equimolecular doses of Ampicillin and Bacampicillin were administrated orally, of Ampicillin also by i.v. injection to 10 healthy adult volunteers (cross over study). By comparison of areas under serum level curves after i.v. and oral administration absorption rate of Bacampicillin which is hydrolysed rapidly to Ampicillin in the body was determined as 95%. Peaks of serum levels after 0.8 g. Bacampicillin administered orally were higher (15,9 microgram/ml) and earlier (after 60 min) than after 0.556 g. Ampicillin administered orally (3.5 microgram/ml after 150 min). Concentrations of Ampicillin in skin blister fluid 1 h after i.v. injection of Ampicillin were 20 times higher than after oral administration of Ampicillin and 3-4 times higher than after oral administration of Bacampicillin; after 3 and 4 hours skin blister levels after i.v. injection were only a half of skin blister levels after oral administration of Bacampicillin. Determination of antibiotic concentrations in saliva and tears showed similar relations. Since higher peaks in serum resulted in higher concentrations in the extravascular space Bacampicillin which is absorbed compeltely and more rapidly should be prefered for oral administration.