Urinary excretion of prednisolone following intravenous administration in humans

The urinary excretion of prednisolone was studied in eight normal human volunteers (two women and six men) following intravenous (16, 32, 48 and 64 mg) doses. Urine prednisolone concentrations were determined by a high performance thin layer chromatographic method (HPTLC). The overall mean prednisolone elimination half life in urine following all the intravenous doses as determined by the rate and sigma minus plots was 1.13 +/- 0.25 hour. This was independent of dose and shorter than that found in plasma (4.10 +/- 1.00 s.d. hour). The overall mean percentage of dose excreted unchanged in urine was 16.7 +/- 5.8% following all intravenous and oral doses respectively. About 80% of this amount was excreted within the first 4 hours of the intravenous administration. Renal clearance of prednisolone decreased with time by the first order kinetic (r = 0.790) and its overall value following all IV doses was 0.0183 +/- 0.0103 (s.d.) l/h/kg. The metabolic clearance remained constant with increasing doses from 16 to 64 mg (0.0883 +/- 0.0306 s.d. l/h/kg). From this study it was concluded that a definitive account of the renal elimination of prednisolone and its possible metabolites warrant further investigation. The fraction of the dose excreted unchanged was relatively small and variable suggesting that prednisolone elimination occurs mainly by metabolism.