Abstract
Purpose
This study was conducted to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of dexlansoprazole injection in healthy subjects.
Methods
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.
Results
Maximum plasma concentration (Cmax) and area under the concentration–time curve (AUC0-τ) for dexlansoprazole injection was dose-proportional over the range of 20–90 mg following a single intravenous administration. Total clearance and half-life (t1/2) 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%).
Conclusion
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.
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Acknowledgements
This project was sponsored by grants from the Priority Academic Program Development of Jiangsu Higher Education Institutions, National Natural Science Foundation of China (81673515, 81503160), Natural Science Foundation of Jiangsu Province (BK20161591), Six Talent Peaks Project in Jiangsu Province (2014-YY-001) and Key Talents of Medical Science in Jiangsu Province (H201108).
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Li, YQ., Yan, ZY., Zhang, HW. et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of dexlansoprazole injection in healthy Chinese subjects. Eur J Clin Pharmacol 73, 547–554 (2017). https://doi.org/10.1007/s00228-017-2206-6
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DOI: https://doi.org/10.1007/s00228-017-2206-6