Pharmacokinetic study of sulbactomax

Abstract

We have evaluated pharmacokinetics of a fixed dose combination (FDC) of ceftriaxone and sulbactam (2:1) or sulbactomax in eight healthy volunteers. A 1.5 g dose of sulbactomax, 1 g dose of ceftriaxone and 0.5 g sulbactam were given intravenously in a balanced two-ways cross-over study. Serially collected plasma sample was analyzed for ceftriaxone and sulbactam by high performance liquid chromatography (HPLC). The mean peaks of ceftriaxone and sulbactam concentrations in plasma were 152.06 ± 6.65 μg/ml and 21.32 ± 1.80 μg/ml, respectively and plasma half-lives for ceftriaxone and sulbactam were 5.2 ± 0.35 hr and 0.94 ± 0.038 hr, respectively. The AUC0-24 for ceftriaxone and sulbactam was 760.16 ± 27.68 μg.hr/ml and 20.74 ± 2.34 μg.hr/ml, respectively, with elimination rate constant of 0.133 ± 0.009 hr -1 and 0.732 ± 0.029 hr -1, respectively. The kinetics of ceftriaxone and sulbactum did not change in combination as compared to the alone treatment. Also, concentration of the ceftriaxone after 24 hr is higher than the minimum inhibitory concentration (MIC) of the most of the gram positive and gram negative bacteria indicating that one dose in a day is sufficient to treat the disease caused by these organisms.