Abstract
Sultamicillin (CP-49,952), a new mutual pro-drug is hydrolysed during enteral absorption to release ampicillin and sulbactam—a β-lactamase inhibitor. 500 mg and 250 mg doses of sultamicillin and 250 mg doses of ampicillin were each given orally, 8 hourly for 7 days to six healthy male volunteers. The pharmacokinetics of sulbactam and ampicillin were compared by measuring their levels in serum and urine following the first dose of each course, and just before and 1 h after the first dose on days 3 and 7.