title: Safety, tolerability, pharmacokinetics and pharmacodynamics of dexlansoprazole injection in healthy Chinese subjects.
abstract: OBJECTIVE
  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%).
  
  
  CONCLUSIONS
  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.
authors.affiliation: Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China.
authors.forename: Yue-Qi
authors.initials: YQ
authors.lastname: Li
authors.affiliation: Department of Analytical Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
authors.forename: Zheng-Yu
authors.initials: ZY
authors.lastname: Yan
authors.affiliation: Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China.
authors.forename: Hong-Wen
authors.initials: HW
authors.lastname: Zhang
authors.affiliation: Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China. sunluning0521@aliyun.com.
authors.forename: Lu-Ning
authors.initials: LN
authors.lastname: Sun
authors.affiliation: 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.
authors.forename: Hui-Wen
authors.initials: HW
authors.lastname: Jiao
authors.affiliation: Department of Gastroenterology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China.
authors.forename: Mei-Feng
authors.initials: MF
authors.lastname: Wang
authors.affiliation: Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China.
authors.forename: Li-Yuan
authors.initials: LY
authors.lastname: Yu
authors.affiliation: Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Yu
authors.affiliation: Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China.
authors.forename: Zi-Qing-Yun
authors.initials: ZQ
authors.lastname: Yuan
authors.affiliation: Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China.
authors.forename: Ling
authors.initials: L
authors.lastname: Meng
authors.affiliation: Research Division of Clinical Pharmacology, First Affiliated Hospital with Nanjing Medical University, Nanjing, 210029, China. wangyongqing@jsph.org.cn.|Department of Pharmacy, Jiangsu Shengze Hospital, Suzhou, 215228, China. wangyongqing@jsph.org.cn.
authors.forename: Yong-Qing
authors.initials: YQ
authors.lastname: Wang
mesh_terms: D019540:Area Under Curve; D002681:China; D064748:Dexlansoprazole / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D005260:Female; D005750:Gastric Juice / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D054328:Proton Pump Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D054328:Proton Pump Inhibitors; D064748:Dexlansoprazole
keywords: Dexlansoprazole injection; Pharmacodynamic; Pharmacokinetic; Safety; Tolerability