Antibiotic activity in serum following single and repeated oral administration of sodium fusidate in volunteers.

摘要: The pharmacokinetics of antibiotic activity were investigated in 10 healthy, female volunteers receiving a single oral dose sodium fusidate (500 mg) followed after 48 h by repeated dosing 250 mg b.i.d. for 5 consecutive days. By use turbidimetry, drug-related serum was determined and expressed as fusidic acid equivalents. After dosing, the peak concentrations (mean ± SE): 30 ±3 μg/ml 27 μg/ml, respectively (NS), trough concentration at steady state 8.4 1.8 μg/ml. experimental predicted accumultion ratios 2.1 0.1 versus 1.6 0.2, (P<0.16). model independent method, terminal elimination half-lives estimated to be 11 1 13 2h doses, (NS). total clearances 2.0 0.4 l/h 0.2 doses (P<0.11). Model dependent pharmacokinetic parameters also obtained fitting two-compartment open median which, with respect half-life clearance, gave values close those observed approach. Safety-wise, biochemical within normal range. However, statistically significant increase ASAT decrease leucocytes observed. tolerability drug good only minor adverse events rere reported.