FREE AND BOUND 17-HYDROXYCORTICOSTEROIDS IN PLASMA AND URINE FOLLOWING A RAPID INTRAVENOUS INJECTION OF PREDNISOLONE-HEMISUCCINATE AND PREDNISONE-GLYCINATE

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Abstract
The maximum level of free plasma 17-hydroxycorticosteroids (17-OHCS) in 21 human subjects was observed 30 minutes following prednisolone hemisuccinate (Ph) and 15 minutes following prednisone glycinate (Pg), and the half- life was 175 minutes and 170 minutes, respectively. Bound plasma 17-OHCS reached the maximum level within 15-30 minutes after pH, possibly through a rapid glucuronidation at C-21. Pg caused only a slight increase of bound plasma 17-OHCS, which may indicate that glycine conjugation inhibits glucuronidation. Maximum excretion of free and bound 17-OHCS appeared in the urine within 8 hours, the free form being greater than the bound form. A clearance delay was occasionally noticed in patients with kidney disease.