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

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