Pharmacokinetics and Tissue Distribution of Baicalin Magnesium Salt Freeze-dried Powder for Injection in Rats

Peng JIN; Jing LI; Cui-zhe LIU

doi:10.13422/j.cnki.syfjx.20190103

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Pharmacokinetics and Tissue Distribution of Baicalin Magnesium Salt Freeze-dried Powder for Injection in Rats

Drug Metabolism | 更新时间：2021-02-09

- Pharmacokinetics and Tissue Distribution of Baicalin Magnesium Salt Freeze-dried Powder for Injection in Rats
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 25, Issue 10, Pages: 102-108(2019)
- 作者机构：
  
  承德医学院，河北省中药研究与开发重点实验室，河北　承德　 067000
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.20190103
  CLC： R22; R24; R28; R969.1; C37
- Received：27 June 2018，
  
  Published Online：17 October 2018，
  
  Published：20 May 2019
- 稿件说明：
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Peng JIN, Jing LI, Cui-zhe LIU. Pharmacokinetics and Tissue Distribution of Baicalin Magnesium Salt Freeze-dried Powder for Injection in Rats[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(10): 102-108.
DOI：

Peng JIN, Jing LI, Cui-zhe LIU. Pharmacokinetics and Tissue Distribution of Baicalin Magnesium Salt Freeze-dried Powder for Injection in Rats[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(10): 102-108. DOI： 10.13422/j.cnki.syfjx.20190103.

摘要

目的：

研究尾静脉注射黄芩苷镁盐后药物在大鼠体内的药代动力学和组织分布特征，比较黄芩苷镁盐和黄芩苷的药代动力学差异。

方法：

大鼠尾静脉注射黄芩苷镁盐和黄芩苷后，在不同时间点眼眶取血，采用HPLC测定各时间点的药物浓度，绘制药-时曲线，利用DAS 3.0软件计算药代动力学参数，应用SPSS 19.0软件进行统计学分析。尾静脉注射黄芩苷镁盐后，于不同时间点检测药物在心、肝、脾、肺、肾中的质量分数。

结果：

当黄芩苷镁盐给药剂量为25～100 mg·kg

－1

时，药时曲线下面积AUC

和AUC

0-∞

与剂量呈良好的线性关系(

0.95)，而其他药代动力学参数各剂量组间大部分无明显差异。与黄芩苷等摩尔剂量组比较，黄芩苷镁盐中剂量组的平均驻留时间(MRT

)显著增高。静脉注射黄芩苷镁盐0.25 h后各组织中药物浓度最高，至0.75 h时目标成分质量分数迅速降低，其中肾脏中分布最多，其次是肺，在心、肝和脾中分布量较少。

结论：

注射给药后，黄芩苷镁盐能迅速在体内分布且快速消除，其主要从肾脏排泄。

Abstract

Objective:

To study on the pharmacokinetics and tissue distribution of baicalin magnesium salt in rats after tail vein injection

and compare pharmacokinetic differences between baicalin magnesium salt and baicalin.

Method:

After tail vein injection of baicalin magnesium salt and baicalin

orbital blood was collected at different time points.The drug concentration was measured by HPLC

the drug concentration-time curve was plotted

the pharmacokinetic parameters were calculated with DAS 3.0 software

SPSS 19.0 software was used for statistical analysis.At the same time

the drug distribution in heart

liver

spleen

lung and kidney was measured at different time points after tail vein injection of baicalin magnesium salt.

Result:

When the dose of baicalin magnesium salt was 25-100 mg·kg

-1

area under the curve(AUC

and AUC

0-∞

) showed a good linear relationship with the dose(

0.95)

but most of the other pharmacokinetic parameters had no significant difference between different dose groups.The mean residence time(MRT

) of medium dose group of baicalin magnesium salt was significantly higher than that of equal molar dose group of baicalin.After intravenous injection of baicalin magnesium salt

the drug concentration was the highest in each tissue at 0.25 h

and the concentration of target component decreased rapidly at 0.75 h. The distribution of target component in kidney was the most

followed by lung.

Conclusion:

After injection

the baicalin magnesium salt can be rapidly distributed and quickly eliminated

in vivo

which is mainly excreted from the kidney.

关键词

Keywords

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Related Institution

School of Life Sciences，Beijing University of Chinese Medicine

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Institute of Chinese Materia Medica，China Academy of Chinese Medical Sciences

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