PHASE I STUDY OF SULBACTAM/CEFOPERAZONE (6-TIMES-ADMINISTRATION TRIAL)

Abstract

We did 6-times-administration trials of Sulbactam 1g/Cefoperazone 1g by intravenous drip infusions to 6 healthy volunteers. Drip infusions were done twice a day for 3 days.
In laboratory data, 2 volunteers had a few abnormal data before the trial. These data became normal during the trial in one case, and were stationary after the trial in the other. No abnormal data caused by this trial were recognized.
Disulfiram-like reaction was recognized in 5 volunteers who drank next day after the trial. No other side effect was recognized after 6-times-administrations of Sulbactam/Cefoperazone.
The peaks of serum concentration of both drugs were at the end of drip infusions, and those values were almost equal in each administrations. At 7 hours after drip infusions, Sulbactam serum levels were trace and Cefoperazone levels were about 4.5μg/ml. Urinary recovery ratio of 0-8 hours of Sulbactam was 90-95%, and that of Cefoperazone was about 25%. Any accumulation was not recognized after 6-times-administrations.