Vachharajani N N, Shyu W C, Mantha S, Park J S, Greene D S, Barbhaiya R H
Department of Metabolism, Bristol-Myers Squibb, Princeton, NJ 08543-4000, USA.
J Clin Pharmacol. 1998 May;38(5):433-6. doi: 10.1002/j.1552-4604.1998.tb04449.x.
This study was conducted to evaluate the effects of a high-fat meal on the oral bioavailability of an 300-mg irbesartan tablet in healthy male volunteers. Sixteen healthy young male volunteers participated in this single-center, open-label, single-dose, crossover study. Each volunteer received a single 300-mg irbesartan tablet under fasted conditions and 5 minutes after a high-fat breakfast, with administrations separated by a 7-day washout period. Serial blood samples were collected over a 72-hour period, and plasma samples were analyzed for irbesartan using a validated high-performance liquid chromatography/fluorescence procedure. Food had no statistically significant effects on the peak concentration (Cmax) and area under the concentration-time curve (AUC) of irbesartan. The presence of food was associated with a slightly prolonged time to maximum concentration (tmax) and half-life (t1/2), but the differences were not statistically significant. The results of this study indicate that food does not affect the bioavailability of irbesartan. Thus, irbesartan can be administered without regard to meals.
本研究旨在评估高脂餐对健康男性志愿者口服300毫克厄贝沙坦片的口服生物利用度的影响。16名健康年轻男性志愿者参与了这项单中心、开放标签、单剂量、交叉研究。每位志愿者在禁食条件下以及高脂早餐后5分钟各服用一片300毫克的厄贝沙坦片，两次给药间隔7天的洗脱期。在72小时内采集系列血样，使用经过验证的高效液相色谱/荧光法分析血浆样本中的厄贝沙坦。食物对厄贝沙坦的峰浓度（Cmax）和浓度-时间曲线下面积（AUC）无统计学显著影响。食物的存在与达峰时间（tmax）和半衰期（t1/2）略有延长有关，但差异无统计学意义。本研究结果表明，食物不影响厄贝沙坦的生物利用度。因此，厄贝沙坦给药无需考虑进餐情况。
