Effect of inflammatory bowel disease on absorption and disposition of prednisolone.

The pharmacokinetics and bioavailability of prednisolone after doses of oral prednisone and intravenous prednisolone were determined in seven patients receiving corticosteroids for treatment of inflammatory bowel disease in active disease and remission. Prednisone absorption and conversion to the active form of prednisolone was complete in both disease phases. Pharmacokinetic parameters for total and free (unbound) prednisolone did not differ significantly between disease phases. Differences in protein binding were observed between active disease and remission with the fractional binding of prednisolone to plasma proteins decreased in active disease. This may be accounted for by decreased plasma albumin concentrations in active disease. Alpha 1-acid glycoprotein concentrations were significantly higher in active disease but did not contribute to the overall binding of prednisolone.