Pharmacokinetics of pivampicillin and ampicillin in man

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Abstract
The absorption of orally administered pivampicillin, an ester that hydrolyzes to ampicillin in vivo, was studied in healthy males and compared to ampicillin administered intravenOusly, intramuscularly, and orally. Using intravenous ampicillin as the reference, pharmacokinetic analyses were performed on data of ampicillin concentrations in sera and urine. All doses were expressed as molar equivalents of anhydrous ampicillin. Following single oral doses of 500 mg, absorption of pivampicillin (P), ampicillin anhydrous (AA), and ampicillin trihydrate (AH) was estimated to be 82%, 53% and 49%, respectively. In a second panel, absorption was 89% after a 500 mg oral dose of pivampicillin and 85% after a 616 mg dose of ampicillin sodium solution administered intramuscularly. Orally, maximum absorption rates occurred in 1 hour; they were approximately 300, 150, and 120 mg per hour for P, AA and AH, respectively. Intramuscularly, peak absorption rates of 500 mg per hour were observed in 15 minutes; these high rates were maintained for a shorter period. There appears to be some diminution in pivampicillin absorption with increasing doses; the absorption increases in a ratio of 1:1.85:3.34 for doses of 250, 500, and 1,000 mg, respectively. Renal clearances and serum half‐lives for pivampicillin were the same as those for ampicillin.

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