1985 Volume 59 Issue 7 Pages 749-765
Multiple oral, doses of sultamicillin, a linked ester of ampcillin and β-lactamase inhibitor, sulbactam, were given to healthy male volunteers and its safety, pharmacokinetics and effects on intestinal flora were investigated. The results are summarized as follows.
The subjects enrolled in the study were 10 male healthy volunteers and received an oral dose of 375 mg of sultamicillin twice a day 15 days. Six of them were administered, with an interval of six months, 500 mg of ampcillin by the same method for comparison.
As side effects presumably related to the drug administration, two cases, a case in each of the sultamicillin and ampicillin groups, developed transient diarrhea. No specific abnormality was found in the laboratory tests which were performed brfore, during and after treatment. Serum levels and urinary excretion of ampcillin and sulbactam after the initial dosing of sultamicillin were closely alike with each other. As compared with administration of ampcillin alone, the time to reach a peak serum level was shorter and the maximum serum concentrations were higher suggesting a good absorbability of sultamicillin. There was noted, however, no significant difference in the half-life between the two drugs. After sultamicillin was administered, more than 60% of the given dose of both ampcillin and sulbactam were excreted, showing about three times as high recovery rate as that attained as administered ampcillin alone. There was observed no significant difference in the serum levels and urinary excretion between days of 1, 8 and 15 of drug administration. The changes in intestinal flora were minimal in either case of sultamicillin or ampicillin administration and the only change commonly observed in both cases was an increase of candida species. In two cases, one in each of the sultamicillin and ampicillin groups, a slight decrease of anerobes was observed but this change returned to the pre-treatment conditions on the 9th day after completion of drug administration.
