Vachharajani N N, Shyu W C, Chando T J, Everett D W, Greene D S, Barbhaiya R H
Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08540, USA.
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.
在18名健康年轻男性志愿者中研究了血管紧张素II受体拮抗剂厄贝沙坦的绝对口服生物利用度和处置特征。受试者接受[14C]厄贝沙坦静脉输注30分钟（50毫克）、[14C]厄贝沙坦口服溶液（50毫克或150毫克）或厄贝沙坦胶囊（50毫克）。口服给药后，厄贝沙坦迅速且几乎完全吸收，平均绝对口服生物利用度为60%至80%。平均全身清除率约为157毫升/分钟，肾清除率为3.0毫升/分钟。稳态分布容积为53升至93升，终末消除半衰期约为13至16小时。肝提取率较低（0.2）。没有主要的循环代谢物，约80%的血浆总放射性归因于未变化的厄贝沙坦。无论给药途径如何，约20%的剂量在尿液中回收，其余在粪便中回收。
