Oral bioavailability and disposition characteristics of irbesartan, an angiotensin antagonist, in healthy volunteers

J Clin Pharmacol. 1998 Aug;38(8):702-7. doi: 10.1002/j.1552-4604.1998.tb04809.x.


Absolute oral bioavailability and disposition characteristics of irbesartan, an angiotensin II receptor antagonist, were investigated in 18 healthy young male volunteers. Subjects received [14C] irbesartan as a 30-minute intravenous infusion (50 mg), [14C] irbesartan orally as a solution (50 mg or 150 mg), or irbesartan capsule (50 mg). Irbesartan was rapidly and almost completely absorbed after oral administration, and exhibited a mean absolute oral bioavailability of 60% to 80%. Mean total body clearance was approximately 157 mL/min, and renal clearance was 3.0 mL/min. Volume of distribution at steady state was 53 L to 93 L, and terminal elimination half-life was approximately 13 to 16 hours. Hepatic extraction ratio was low (0.2). There were no major circulating metabolites, and approximately 80% of total plasma radioactivity was attributable to unchanged irbesartan. Regardless of route of administration, approximately 20% of dose was recovered in urine and the remainder in feces.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adult
  • Angiotensin II / antagonists & inhibitors*
  • Angiotensin II / metabolism
  • Angiotensin Receptor Antagonists*
  • Area Under Curve
  • Biological Availability
  • Biphenyl Compounds / adverse effects
  • Biphenyl Compounds / pharmacokinetics*
  • Cross-Over Studies
  • Half-Life
  • Humans
  • Irbesartan
  • Male
  • Tetrazoles / adverse effects
  • Tetrazoles / pharmacokinetics*


  • Angiotensin Receptor Antagonists
  • Biphenyl Compounds
  • Tetrazoles
  • Angiotensin II
  • Irbesartan