title: Oral bioavailability and disposition characteristics of irbesartan, an angiotensin antagonist, in healthy volunteers.
abstract: 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.
authors.affiliation: Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08540, USA.
authors.forename: N N
authors.initials: NN
authors.lastname: Vachharajani
authors.forename: W C
authors.initials: WC
authors.lastname: Shyu
authors.forename: T J
authors.initials: TJ
authors.lastname: Chando
authors.forename: D W
authors.initials: DW
authors.lastname: Everett
authors.forename: D S
authors.initials: DS
authors.lastname: Greene
authors.forename: R H
authors.initials: RH
authors.lastname: Barbhaiya
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000804:Angiotensin II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D057911:Angiotensin Receptor Antagonists; D019540:Area Under Curve; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000009:adverse effects / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D006207:Half-Life; D006801:Humans; D000077405:Irbesartan; D008297:Male; D013777:Tetrazoles / Q000009:adverse effects / Q000493:pharmacokinetics*
chemical_list: D057911:Angiotensin Receptor Antagonists; D001713:Biphenyl Compounds; D013777:Tetrazoles; D000804:Angiotensin II; D000077405:Irbesartan