Pharmacokinetics and pharmacodynamics of injectable dex-rabrazole for healthy people

Mingjie YU; Fengjun SUN; Lirong XIONG; Lin CHENG; Qin DAI; Xiaochuan LI; Shu ZHANG; Xiaoqing YUAN; Yongchuan CHEN

doi:10.16016/j.1000-5404.202103050

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Pharmacokinetics and pharmacodynamics of injectable dex-rabrazole for healthy people

更新时间：2026-01-09

- Pharmacokinetics and pharmacodynamics of injectable dex-rabrazole for healthy people
- Journal of Third Military Medical University Vol. 43, Issue 17, Pages: 1696-1702(2021)
- 作者机构：
- 作者简介：
- 基金信息：
  
  the Science and Technology Innovation Special Project of Social Undertakings and People's Livelihood Security of Chongqing(CSTC2017shmsA130043)
- DOI：10.16016/j.1000-5404.202103050
  CLC：
- Received：05 March 2021，
  
  Published：15 September 2021
- 稿件说明：
移动端阅览
Mingjie YU, Fengjun SUN, Lirong XIONG, et al. Pharmacokinetics and pharmacodynamics of injectable dex-rabrazole for healthy people[J]. Journal of Third Military Medical University, 2021, 43(17): 1696-1702.
DOI：

Mingjie YU, Fengjun SUN, Lirong XIONG, et al. Pharmacokinetics and pharmacodynamics of injectable dex-rabrazole for healthy people[J]. Journal of Third Military Medical University, 2021, 43(17): 1696-1702. DOI： 10.16016/j.1000-5404.202103050.

摘要

目的

探讨不同剂量注射用右旋雷贝拉唑钠在健康受试者体内的药代动力学和药效学特征

并评价其安全性。

方法

采用随机、开放、阳性药对照试验设计

筛选40例健康受试者分为4组（

=10）

分别静脉滴注注射用右旋雷贝拉唑钠10 mg/qd（10 mg/qd右旋组）、10 mg/q12h（10 mg/q12h右旋组）、20 mg/q12h（20 mg/q12h右旋组）和注射用雷贝拉唑钠20 mg/q12h（20 mg/q12h消旋组）

于第1、5天给药后监测胃内24 h pH值

并用液-质联用(LC-MS/MS)法测定血液中右旋雷贝拉唑浓度

数据用WinNonlin7.0和SAS9.4软件分析处理。

结果

受试者第1、5天20 mg/q12h右旋组的主要药代动力学参数：C

max

为(1.70±0.46)、(1.74±0.49)μg·mL

-1

AUC

0-t

为(2.19±0.59)、(2.21±0.51) h·μg·mL

-1

高于其他3组；T

max

为(0.51±0.03)、(0.50±0.00)h

与其他3组相当；T

1/2

为(1.93±0.73)、(1.82±0.67)h

高于10 mg/qd右旋组和10 mg/q12h右旋组

稍低于20 mg/q12h消旋组。用药第1、5天后20 mg/q12h右旋组胃内pH

4.0的时间百分比为(82.27±10.13)%、(93.16±5.84)%

高于其他3组；20 mg/q12h消旋组胃内pH

4.0的时间百分比高于10 mg/qd右旋组和10 mg/q12h右旋组。20 mg/q12h右旋组出现1例1件轻度不良事件（大腿后侧酸痛）

自行好转

各组均未出现严重不良事件。

结论

注射用右旋雷贝拉唑钠20 mg/q12h的药代动力学和药效学效果较好

且健康受试者服药后安全性良好。

Abstract

Objective

To study the pharmacokinetic and pharmacodynamic characteristics of dex-rabeprazole for injection at different doses in healthy subjects and to evaluate its safety.

Methods

A randomized

open

positive drug control trial design was adopted in this study. Forty healthy subjects were divided into 4 groups (

=10)

and underwent intravenous infusion of dex-rabeprazole at 10 mg/qd

10 mg/q12h

20 mg/q12h and rabeprazole sodium 20 mg/q12h

respectively. The intragastric pH va

lue was monitored for 24 h on the first and fifth days after administration. Liquid chromatography with tandem mass spectrometry (LC-MS/MS) was used to determine the blood dex-rabeprazole concentration. WinNonlin7.0 and SAS9.4 software was conducted to analyze and process the obtained data.

Results

The pharmacokinetic parameters on the first and fifth days of the subjects after intravenous infusion of dex-rabeprazole 20 mg/q12h were C

max

1.70±0.46 and 1.74±0.49 μg·mL

-1

and AUC

0-t

2.19±0.59 and 2.21±0.51 μg·mL

-1

(significantly higher than the other 3 groups); T

max

0.51±0.03 and 0.50±0.00 h (similar to the other 3 groups); and T

1/2

1.93±0.73 and 1.82±0.67 (higher than the 10 mg/qd and 10 mg/q12h groups and slightly lower than the rabeprazole sodium 20 mg/q12h). The percentage of time with intragastric pH value

4.0 after the first and fifth days of medication was (82.27±10.13)% and (93.16±5.84)% in the dex-rabeprazole 20 mg/q12h group

statistically higher than those in the other 3 groups. The percentage was also higher in the rabeprazole sodium 20 mg/q12h group than the 10 mg/qd and 10 mg/q12h groups. One case from the dex-rabeprazole 20 mg/q12h group experienced mild adverse event (pain in the back of the thigh) and relieved after that spontaneously. No serious adverse events were observed in each group.

Conclusion

Injectable dex-rabeprazole shows good pharmacokinetic and pharmacodynamics effects

and has sound safety to healthy subjects.

关键词

Keywords

references

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