A pharmacokinetic and tolerance study of Ro13‐9904, a new cephalosporin antibiotic.

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Abstract
1 Six healthy male volunteers received a total of 2500 mg of a new cephalosporin antibiotic Ro13‐9904 by intramuscular injection in five divided doses at intervals of 12 h. 2 No significant systemic side‐ effects were observed and this was confirmed haematologically and biochemically. 3 The drug was distributed following intramuscular injection reaching a mean peak plasma concentration of 55 micrograms ml‐ 1 (range 46‐66) 1 to 2 h after the first injection. 4 Monoexponential elimination of drug was demonstrated. No significant difference was recorded in the plasma half‐life after the initial dose (mean 6.7 h) and at steady state (mean 6.7 h). The half‐life is long compared with other cephalosporin antibiotics. 5 On the basis of the observed half‐ life, steady state should be reached within 48 h. A mean peak plasma concentration of 74 micrograms ml‐1 (range 65‐87) was recorded at steady state. Steady state plasma concentrations of Ro13‐9904 with a dose of 500 mg every 13 h may be predicted from the pharmacokinetics of a single dose.