Metabolism of a prednisolone compound in human under normal and pathological conditions.

A method has been presented for the quantitative determination of 21-deoxy-N-(N'-methyl-piperazinyl)-prednisolone (Depersolone), a water soluble corticosteroid, and one of its metabolites, prednisolone, in human urine. Following administration of 30 or 90 mg Depersolone i.v., the dynamic appearance of this hormone and the prednisolone metabolite, their biological half-lives and the effect of the synthetic corticosteroid on the excretion of grouped and individual 17-ketosteroids were determined. Results of experiments revealed a dose dependent excretion of the unchanged hormone and a biological half-life 12 to 23 h in control subjects. Prednisolone as a metabolite seems to play a minor role in Depersolone action. The excretion rate of Depersolone was greater and its half-life less than normal in hepatopathies. The dynamic appearance of the hormone was found slow in the urine of patients with prolonged corticosteroid therapy.