Tenero D M, Martin D E, Ilson B E, Boyle D A, Boike S C, Carr A M, Lundberg D E, Jorkasky D K
SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406, USA.
Ann Pharmacother. 1998 Mar;32(3):304-8. doi: 10.1345/aph.17188.
To assess the effect of ranitidine on the pharmacokinetics of eprosartan in healthy male volunteers.
Single-center, randomized, open-label, two-period, period-balanced, crossover study.
Seventeen healthy men aged 19 to 43 years.
In each period (separated by a > or = 7 d washout), subjects received a single 400-mg oral dose of eprosartan alone, or a single oral dose of eprosartan 400 mg and ranitidine 150 mg on day 4 after 3 days of ranitidine 150 mg twice daily. Serial pharmacokinetic samples were obtained for up to 24 hours following eprosartan dosing.
Plasma and urine eprosartan concentrations during each treatment session.
Eprosartan maximum concentration (Cmax), the AUC from time-zero to the last quantifiable concentration (AUC0-t), and renal clearance (Cl(r)) values were approximately 7%, 11%, and 4% lower, respectively, when administered with ranitidine compared with eprosartan alone. The 95% CIs for the ratio of eprosartan plus ranitidine compared with eprosartan alone were 0.81 to 1.07, 0.77 to 1.03, and 0.64 to 1.43, for Cmax, AUC0-t, and Cl(r), respectively, indicating no statistically significant difference between regimens.
Repeated doses of ranitidine did not have a marked effect on the single-dose pharmacokinetics of eprosartan.
评估雷尼替丁对健康男性志愿者中依普罗沙坦药代动力学的影响。
单中心、随机、开放标签、两期、周期平衡的交叉研究。
17名年龄在19至43岁之间的健康男性。
在每个周期（间隔≥7天的洗脱期），受试者分别接受单剂量400mg口服依普罗沙坦，或在每日两次服用150mg雷尼替丁3天后，于第4天接受单剂量400mg依普罗沙坦和150mg雷尼替丁。在依普罗沙坦给药后长达24小时内获取系列药代动力学样本。
每次治疗期间血浆和尿液中依普罗沙坦的浓度。
与单独使用依普罗沙坦相比，联合使用雷尼替丁时，依普罗沙坦的最大浓度（Cmax）、从零时间到最后可定量浓度的曲线下面积（AUC0-t）和肾清除率（Cl(r)）值分别降低了约7%、11%和4%。依普罗沙坦加雷尼替丁与单独使用依普罗沙坦相比，Cmax、AUC0-t和Cl(r)的95%置信区间分别为0.81至1.07、0.77至1.03和0.64至1.43，表明各治疗方案之间无统计学显著差异。
重复剂量的雷尼替丁对依普罗沙坦单剂量药代动力学无明显影响。
