Li Yue-Qi, Yan Zheng-Yu, Zhang Hong-Wen, Sun Lu-Ning, Jiao Hui-Wen, Wang Mei-Feng, Yu Li-Yuan, Yu Lei, Yuan Zi-Qing-Yun, Meng Ling, Wang Yong-Qing
Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China.
Department of Analytical Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
Eur J Clin Pharmacol. 2017 May;73(5):547-554. doi: 10.1007/s00228-017-2206-6. Epub 2017 Jan 31.
This study was conducted to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of dexlansoprazole injection in healthy subjects.
Dexlansoprazole (20-90 mg) or lansoprazole (30 mg) was administrated intravenously to healthy male and female volunteers. All the subjects were sampled for pharmacokinetic (PK) analysis and 64 of them were monitored for 24-h intragastric pH prior to and after administration in the pharmacodynamic (PD) study.
Maximum plasma concentration (C) and area under the concentration-time curve (AUC) for dexlansoprazole injection was dose-proportional over the range of 20-90 mg following a single intravenous administration. Total clearance and half-life (t) was independent of dose, and ranged from 4.69 L/h to 5.85 L/h and from 1.24 h to 2.17 h, respectively. A single dose of dexlansoprazole (30 mg) resulted in higher gastric pH compared to that of lansoprazole, evidenced by a mean 24-h gastric pH of 6.1 ± 1.2 (lansoprazole: 5.4 ± 1.1) and 24-h gastric pH > 6 post drug dose holding time of 64.2 ± 21.0% (lansoprazole: 49.5 ± 21.5%).
Dexlansoprazole injection was safe and well tolerated for up to 5-day repeated intravenous administration dose of 30 mg. The recommended dosage for dexlansoprazole injection is 30 mg for an adequate gastric acid control.
本研究旨在评估右兰索拉唑注射液在健康受试者中的安全性、耐受性、药代动力学和药效学。
将右兰索拉唑（20 - 90毫克）或兰索拉唑（30毫克）静脉注射给健康的男性和女性志愿者。所有受试者均进行药代动力学（PK）分析采样，其中64名受试者在药效学（PD）研究中于给药前后监测24小时胃内pH值。
单次静脉给药后，右兰索拉唑注射液的最大血浆浓度（C）和浓度 - 时间曲线下面积（AUC）在20 - 90毫克范围内与剂量成正比。总清除率和半衰期（t）与剂量无关，分别为4.69升/小时至5.85升/小时和1.24小时至2.17小时。单剂量右兰索拉唑（30毫克）导致的胃内pH值高于兰索拉唑，平均24小时胃内pH值为6.1±1.2（兰索拉唑：5.4±1.1）以及给药后24小时胃内pH值> 6的时间占比为64.2±21.0%（兰索拉唑：49.5±21.5%）可证明这一点。
右兰索拉唑注射液在重复静脉给药剂量达30毫克、为期5天的情况下是安全且耐受性良好的。右兰索拉唑注射液的推荐剂量为30毫克，以实现充分的胃酸控制。
