Pharmacokinetics and rectal bioavailability of hydrocortisone acetate

J Pharm Sci. 1991 Sep;80(9):835-6. doi: 10.1002/jps.2600800906.

Abstract

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.

MeSH terms

  • Administration, Oral
  • Administration, Rectal
  • Administration, Topical
  • Adult
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / pharmacokinetics*
  • Biological Availability
  • Humans
  • Hydrocortisone / administration & dosage
  • Hydrocortisone / analogs & derivatives*
  • Hydrocortisone / pharmacokinetics
  • Injections, Intravenous
  • Male
  • Rectum / metabolism*

Substances

  • Anti-Inflammatory Agents
  • hydrocortisone acetate
  • Hydrocortisone