不同剂量注射用泮托拉唑钠在健康人体内的药代动力学和药效学研究

李晓宇; 尚圣兰; 熊丽蓉; 孙凤军; 向荣凤; 邱学文; 喻明洁; 王若茜; 陈勇川

doi:10.16016/j.1000-5404.201802146

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不同剂量注射用泮托拉唑钠在健康人体内的药代动力学和药效学研究

药学 | 更新时间：2026-01-09

- 不同剂量注射用泮托拉唑钠在健康人体内的药代动力学和药效学研究
- Pharmacokinetics and pharmacodynamics of pantoprazole sodium at different doses in healthy volunteers
- 第三军医大学学报 2018年40卷第17期页码：1613-1618
- 作者机构：
- 作者简介：
- 基金信息：
  
  重庆市社会事业与民生保障科技创新专项项目(CSTC2017shmsA130043)
- DOI：10.16016/j.1000-5404.201802146
  中图分类号：
- 收稿：2018-02-27，
  
  纸质出版：2018-09-15
- 稿件说明：
移动端阅览
李晓宇, 尚圣兰, 熊丽蓉, 等. 不同剂量注射用泮托拉唑钠在健康人体内的药代动力学和药效学研究[J]. 第三军医大学学报, 2018,40(17):1613-1618.

Xiaoyu LI, Shenglan SHANG, Lirong XIONG, et al. Pharmacokinetics and pharmacodynamics of pantoprazole sodium at different doses in healthy volunteers[J]. Journal of Third Military Medical University, 2018, 40(17): 1613-1618.
李晓宇, 尚圣兰, 熊丽蓉, 等. 不同剂量注射用泮托拉唑钠在健康人体内的药代动力学和药效学研究[J]. 第三军医大学学报, 2018,40(17):1613-1618. DOI： 10.16016/j.1000-5404.201802146.

Xiaoyu LI, Shenglan SHANG, Lirong XIONG, et al. Pharmacokinetics and pharmacodynamics of pantoprazole sodium at different doses in healthy volunteers[J]. Journal of Third Military Medical University, 2018, 40(17): 1613-1618. DOI： 10.16016/j.1000-5404.201802146.

摘要

Abstract

Objective

To investigate the pharmacokinetic and pharmacodynamic properties of pantoprazole sodium at different doses of injection and explore its safety in healthy Chinese volunteers.

Methods

A single center

randomized

open

and parallel controlled trial was designed for this study. Twenty healthy subjects were screened by a stratified randomization method for men and women to receive multiple doses of pantoprazole sodium of 40 and 80 mg (twice daily for 5 consecutive days)

respectively. The intragastric pH value was monitored 24 h after administration.S-(-)-pantoprazole sodium concentration was determined by liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS). The data were analyzed by WinNonlin 6.4 software and SAS software respectively.

Results

After the first intravenous infusion of pantoprazole sodium

the main pharmacokinetic parameters of S-(-)-pantoprazole after 40 and 80 mg groups were as follows: C

max

were 2.37±0.61 and 4.56±0.89 μg/mL; AUC

(0-t)

4.96±3.26 and 10.16±3.16 μg·h/mL; AUC

(0-∞)

5.17±3.68 and 10.34±3.35 μg·h/mL; t

1/2

1.67±0.76 and 1.75±0.57 h; and T

max

0.50±0.01 and 0.53±0.08 h. After 5 days'

continuous administration

the main pharmacokinetic parameters were as follows: C

max

were 2.30±0.62 and 4.50±0.71 μg/mL; AUC

(0-t)

5.02±3.85 and 10.75±3.82 μg·h/mL; AUC

(0-∞)

5.26±4.35 and 10.98±4.10 μg/mL·h; C

min

0.03±0.08 and 0.05±0.07 μg/mL; t

1/2

1.72±0.78 and 1.80±0.64 h; and T

max

0.52±0.04 and 0.50±0.00 h. After the first day of treatment

the both groups had (38.6±20.9)% and (46.9±16.5)%

respectively of time with gastric juice pH

and (25.5±20.6)% and (32.7±7.9)% respectively with pH

6. In 5 d after the administration

the time percentage of gastric juice pH

4 was (69.6±15.4)% and (80.2±16.6)%

respectively

and it of pH

6 was (48.3±13.7)% and (49.7±15.7)%

respectively.

Conclusion

The pantoprazole sodium for injection is in accordance with the linear pharmacokinetic characteristics in healthy volunteers. Compared with the pharmacodynamic parameters of 2 doses

the inhibitory effect of 80 mg dose group is better than that of 40 mg dose group

and the higher dose is safer. It is recommended of 80 mg q12 h in clinical practice.

关键词

Keywords

references

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