BIOAVAILABILITY OF ORAL PENICILLINS IN THE HORSE - A COMPARISON OF PIVAMPICILLIN AND AMOXICILLIN

The pharmacokinetics of ampicillin and amoxicillin following intravenous administration at a dose rate of 15 and 10 mg/kg respectively were studied in four healthy adult horses. Pharmacokinetics of pivampicillin and amoxicillin were studied after oral administration to four healthy adult horses. Pivampicillin, a prodrug of ampicillin, was administered orally to starved and fed horses at a dose rate of 19.9 mg/kg, which is equivalent on a molecular basis to 15 mg/kg ampicillin. Amoxicillin was administered orally to starved horses only, at a dose rate of 20 mg/kg. Ampicillin and amoxicillin concentrations in plasma, synovial fluid and urine were determined. Mean biological half-life of intravenously administered ampicillin and amoxicillin was 1.72 and 1.43 h respectively, whilst the distribution volume (V(ss)) appeared to be 0.180 and 0.192 1/kg. Orally administered pivampicillin and amoxkillin were rapidly absorbed. A maximum concentration in plasma of 3.80-mu-g/ml was reached 2 h after administration of pivampicillin to starved horses; in fed horses a maximum concentration of 5.12-mu-g/ml was reached 1 h after administration. After oral administration of amoxicillin a maximum concentration of 2.03-mu-g/ml was reached after 1 h. The (absolute) bioavailability of pivampicillin administered orally was 30.9% in starved horses and 35.9% in fed horses. The bioavailability of amoxicillin administered orally was 5.3% in starved horses.