Oral absorption and tolerance in man, of a new penem antibiotic, Sch 29482

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Abstract
The absorption and tolerance of Sch 29482 (SCH) has been studied in man. Twenty healthy male Caucasian volunteers were separated into two groups of ten each. Group I received single oral solution doses of 125, 500 and 1000 mg; group II received 250 and 750 mg. A 4-day period separated subsequent doses in the same subject. No significant drug-related adverse experiences were reported. Predosing and postdosing physical examination and electrocardiograms were normal and all laboratory values were within clinically acceptable limits. Both HPLC and microbiological assay techniques gave practically identical drug levels for all doses. Following oral administration of SCH, the drug was rapidly absorbed, Tmax equaling approximately l h. The elimination half-life of SCH ranged from 0.95 to 1.37 h. There were linear relationships between AUC and dose and between Cmax and dose, thereby establishing dose proportionality. At all doses, most of the SCH was excreted in the urine within 0–4 h following administration, indicating rapid excretion of the drug. The total excretion of unchanged SCH in the urine accounted for approximately 2% of the dose, regardless of the dose level administered, which suggests extensive metabolism of the drug. From the results of this study, it can be concluded that SCH in aqueous solution is well absorbed and tolerated at single doses up to 1000 mg.

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