Effect of corticosteroid binding globulin on the pharmacokinetics of prednisolone in rats

Pharm Res. 1995 Jun;12(6):902-4. doi: 10.1023/a:1016225423795.


Purpose: The effect of exogenous corticosteroid binding globulin (CBG) on the pharmacokinetics of intravenous prednisolone was determined in rats to test the "free hormone hypothesis."

Methods: A dose of CBG to yield 95% binding with 1000 ng/ml of prednisolone in vitro in rat plasma or saline was administered before dosing 2 mg/kg of prednisolone hemisuccinate or methylprednisolone intravenously. Drug concentrations in plasma samples were assayed by HPLC.

Results: Single administration of CBG decreased apparent prednisolone clearance by 56% (155 to 66 ml/min/kg) and reduced apparent VSS by 35% (4.1 to 2.7 L/kg) (p < 0.001). Methylprednisolone pharmacokinetics, studied as a negative control because the drug does not bind to CBG, did not change.

Conclusions: The corticosteroid bound to CBG does not appear to be available for removal by clearance organs.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Injections, Intravenous
  • Male
  • Methylprednisolone / pharmacokinetics
  • Prednisolone / pharmacokinetics*
  • Protein Binding / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Time Factors
  • Transcortin / pharmacology*


  • Transcortin
  • Prednisolone
  • Methylprednisolone