Pharmacokinetics and rectal bioavailability of hydrocortisone acetate.
The pharmacokinetics and bioavailability of hydrocortisone after rectal administration of a hydrocortisone acetate foam was determined. Endogenous hydrocortisone was suppressed by dexamethasone administration. Plasma levels were compared with those observed after iv and oral administration. Only a very small part of the rectal dose (100 mg) was absorbed; the mean absolute bioavailability was 2%. There was substantial intersubject variability. Maximum hydrocortisone levels were reached after 2 h and averaged 35 ng/mL. These levels were 10-fold lower than those obtained after oral administration of a fivefold lower dose (20 mg) of hydrocortisone in the same subjects.
Möllmann
H
H
Department of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville 32610.
Barth
J
J
Möllmann
C
C
Tunn
S
S
Krieg
M
M
Derendorf
H
H
D000284:Administration, Oral; D000285:Administration, Rectal; D000287:Administration, Topical; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D006801:Humans; D006854:Hydrocortisone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D007275:Injections, Intravenous; D008297:Male; D012007:Rectum / Q000378:metabolism*
D000893:Anti-Inflammatory Agents; C021650:hydrocortisone acetate; D006854:Hydrocortisone