Pharmacokinetics of cloprednol in healthy volunteers

Kinetic data for the synthetic corticoid cloprednol were determined in 8 healthy male volunteers after single oral doses (20 mg). Maximal plasma levels (Cmax) of 426 +/- 116 ng/ml occurred within 101 +/- 44 min after oral intake. Cloprednol plasma levels declined monoexponentially after oral administration. Total apparent plasma clearance was 4.07 +/- 0.72 ml/min/kg and apparent clearance of unbound cloprednol was 9.75 +/- 0.8 ml/min/kg. Plasma protein binding was 74 to 94%. Volume of distribution at steady-state was 0.81 +/- 0.14 l/kg for total cloprednol and 1.99 +/- 0.33 l/kg for unbound drug. The results presented in this study characterize the kinetics of total and unbound cloprednol for the first time.