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目的:研究健康志愿者单次口服和静脉输注雷贝拉唑20 mg后药动学特征及生物利用度。方法:20名男性健康志愿者,随机分成2组。第1周期分别接受单剂量静脉输注20 mg(输注时间30 min)和单次口服给药(2片,10 mg/片);经7 d清洗期后,2组志愿者接受交叉给药。结果:雷贝拉唑静脉给药后药动学参数如下:t1/2为(62.4±10.7)min,Cmax为(1 308.6±266.4)ng/ml,总清除率为(0.21±0.05)L/min,AUC0-τ和AUC0-∞分别为(99.6±21.9)mg.min/L和(102.4±23.3)mg.min/L。口服给药后t1/2为(64.2±15.5)min,Cmax为(508.3±180.2)ng/ml,Tmax为229.5 min,Cl为(0.31±0.10)L/min,AUC0-τ和AUC0-∞分别为(69.5±20.0)mg.min/L和(70.6±20.2)mg.min/L。结论:雷贝拉唑在健康志愿者体内的生物利用度为70.1%,雷贝拉唑口服给药的总清除率显著大于静脉给药时的总清除率(P<0.01)。
Objective: To study the pharmacokinetics and bioavailability of rabeprazole 20 mg single oral and intravenous infusion in healthy volunteers. Methods: Twenty male healthy volunteers were randomly divided into two groups. The first cycle received single-dose intravenous infusion of 20 mg (infusion time 30 min) and a single oral administration (2, 10 mg / tablet); after 7 d wash period, two groups of volunteers received cross-over . Results: The pharmacokinetic parameters of rabeprazole after intravenous administration were as follows: t1 / 2 was (62.4 ± 10.7) min, Cmax was (1 308.6 ± 266.4) ng / ml and the total clearance rate was (0.21 ± 0.05) min, AUC0-τ and AUC0-∞ were (99.6 ± 21.9) mg.min / L and (102.4 ± 23.3) mg.min / L, respectively. After oral administration, t1 / 2 was (64.2 ± 15.5) min, Cmax was (508.3 ± 180.2) ng / ml, Tmax was 229.5 min, Cl was 0.31 ± 0.10 L / min, AUC0-τ and AUC0-∞ (69.5 ± 20.0) mg.min / L and (70.6 ± 20.2) mg.min / L. CONCLUSIONS: The bioavailability of rabeprazole in healthy volunteers was 70.1%. The overall clearance of rabeprazole orally administered was significantly greater than that of intravenous (P <0.01).