Pharmacokinetics of Cyclosporine in Rats with Dextran Sulfate Sodium Induced Ulcerative Colitis

Liu Xiongzhi; Ye Yongfeng

doi:10.13407/j.cnki.jpp.1672-108X.2023.01.002

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Pharmacokinetics of Cyclosporine in Rats with Dextran Sulfate Sodium Induced Ulcerative Colitis

更新时间：2023-04-14

- Pharmacokinetics of Cyclosporine in Rats with Dextran Sulfate Sodium Induced Ulcerative Colitis
- Vol. 29, Issue 1, Pages: 4-8(2023)
- 作者机构：
  
  1. 重庆医科大学附属儿童医院,重庆,400014
  2. 中山大学附属第五医院,广东,珠海,519000
- 作者简介：
- 基金信息：
- DOI：10.13407/j.cnki.jpp.1672-108X.2023.01.002
  CLC：
- Published：2023，
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Liu Xiongzhi, Ye Yongfeng. Pharmacokinetics of Cyclosporine in Rats with Dextran Sulfate Sodium Induced Ulcerative Colitis. [J]. 29(1):4-8(2023)
DOI：

Liu Xiongzhi, Ye Yongfeng. Pharmacokinetics of Cyclosporine in Rats with Dextran Sulfate Sodium Induced Ulcerative Colitis. [J]. 29(1):4-8(2023) DOI： 10.13407/j.cnki.jpp.1672-108X.2023.01.002.

摘要

目的:探讨环孢素(CsA)在葡聚糖硫酸钠(DSS) 诱导溃疡性结肠炎( UC) 模型大鼠体内的药物代谢动力学( 药动学) 特征。方法:将12 只SPF 级SD 大鼠按随机数表法分为UC 模型组和正常对照组各6 只

UC 模型组大鼠给予5% DSS 连续自由饮用7 d 诱导建立UC 模型

正常对照组大鼠正常饲养。第8 天分别给予两组大鼠灌胃CsA 15 mg/ kg

并于给药前和给药后不同时间点采血

测定CsA 的血药浓度

比较两组大鼠主要药动学参数。结果:与正常对照组相比

UC 模型组CsA 的体内暴露强度增加

药时曲线下面积(AUC)增加35. 69%

半衰期延长34. 94%

体内滞留时间(MRT) 延长23. 17%

体内清除率下降28. 00%(P 均<0. 05)。结论:CsA 在大鼠体内的药动学会受到UC 状态的影响而导致CsA 吸收增加

代谢减慢

CsA 体内的暴露强度增加

其具体作用机制还需要进一步研究。本研究结论可为CsA 的安全用药研究提供参考。

Abstract

Objective: To investigate the pharmacokinetics of cyclosporine (CsA) in rats with ulcerative colitis (UC) induced by sodium glucan sulfate (DSS). Methods: Twelve rats were randomly divided into two groups: the control group (normal feeding) and the UC group (5% DSS free drinking for 7 days to induce the UC model). On the 8th day

rats in both groups were given CsA 15 mg/ kg by gavage. Blood collection was performed before and after the administration

the plasma concentration was detected and the main pharmacokinetic parameters were compared between groups. Results: Compared with the control group

the exposure intensity of CsA in the UC group was significantly increased

the area under the curve (AUC) was increased significantly by 35. 69%

the half-life was extended by 34. 94%

the retention time (MRT) was also extended by 23. 17%

and the drug elimination rate was decrease significantly by 28. 00% (P<0. 05). Conclusion: The pharmacokinetics of CsA in rats can be changed by UC disease status. Metabolism decline

half-life extension

and increased exposure intensity

may be related to the increased CsA absorption. This study provides references for the safe use of CsA in clinical.

关键词

环孢素溃疡性结肠炎药代动力学CYP3AP 糖蛋白

Keywords

cyclosporineulcerative colitispharmacokineticCYP3AP glycoprotein

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