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Safety, tolerability, pharmacokinetics and pharmacodynamics of dexlansoprazole injection in healthy Chinese subjects

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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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Authors and Affiliations

  1. Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China

    Yue-Qi Li, Hong-Wen Zhang, Lu-Ning Sun, Hui-Wen Jiao, Li-Yuan Yu, Lei Yu, Zi-Qing-Yun Yuan, Ling Meng & Yong-Qing Wang

  2. Department of Pharmacy, Jiangsu Shengze Hospital, Suzhou, 215228, China

    Yong-Qing Wang

  3. Department of Analytical Chemistry, China Pharmaceutical University, Nanjing, 210009, China

    Zheng-Yu Yan & Hui-Wen Jiao

  4. Department of Gastroenterology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China

    Mei-Feng Wang

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  1. Yue-Qi Li
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  11. Yong-Qing Wang
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Correspondence to Lu-Ning Sun or Yong-Qing Wang.

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Zheng-Yu Yan co-first authors

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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

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