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Purpose: The objective of this study was to evaluate the safety, pharmacokinetics, and pharmacodynamics of S-(−)-pantoprazole (PPZ) sodium injections following single and multiple intravenous doses in healthy Chinese subjects.Methods: The dosage groups were set as followed: 20 mg of single and multiple intravenous administration of S-(−)-PPZ, 40 mg of single and multiple intravenous administration of S-(−)-PPZ or pantoprazole, and 80 mg of single dosage group of S-(−)-PPZ. Subjects were sampled for pharmacokinetic analysis and were monitored for 24-h intragastric pH prior to and 48-h intragastric pH after administration for the pharmacodynamic study. The pharmacokinetic and pharmacodynamic parameters were compared between S-(−)-PPZ and PPZ. Safety was evaluated on the basis of adverse events, vital signs, laboratory tests, and physical examination.Results: All adverse events were mild and of limited duration. Maximum plasma concentration and area under the concentration-time curve for S-(−)-PPZ were dose proportional over the range of 20–80 mg following a single intravenous administration. Elimination rate constant and half-life observed statistical difference from a single dose to multiple doses in 40 mg of S-(−)-PPZ groups. After administration of a single dose, the mean 24-h intragastric pH value was observed higher in 80-mg group than in 40- and 20-mg groups. Slightly increase of intragastric pH was found after a single dose of 40 mg S-(−)-PPZ than 40 mg PPZ; however, the differences were not statistically significant.Conclusions: Twice daily of 40 mg S-(−)-PPZ sodium injections is effective in achieving satisfying acid inhibition. Compared with plasma R-(+)-PPZ levels, most subjects presented more potent and prolonged suppression of gastric acid of S-(−)-PPZ, while a few subjects showed faster metabolic rate of S-(−)-PPZ in vivo. [ABSTRACT FROM AUTHOR]

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 (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%). 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. [ABSTRACT FROM AUTHOR]