Pharmacokinetics Analysis of Geniposidic Acid in Normal and Cholestatic Rats

CHEN Hao; MIN Jian-bin; HUANG Xiao-tao; LIU Chang-hui; MI Sui-qing; WANG Ning-sheng

doi:10.13422/j.cnki.syfjx.2015170075

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Pharmacokinetics Analysis of Geniposidic Acid in Normal and Cholestatic Rats

更新时间：2024-01-04

- Pharmacokinetics Analysis of Geniposidic Acid in Normal and Cholestatic Rats
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 21, Issue 17, Pages: 75-78(2015)
- 作者机构：
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- DOI：10.13422/j.cnki.syfjx.2015170075
  CLC： R285.5
- Published：2015
- 稿件说明：
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CHEN Hao, MIN Jian-bin, HUANG Xiao-tao, et al. Pharmacokinetics Analysis of Geniposidic Acid in Normal and Cholestatic Rats[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(17): 75-78.
DOI：

CHEN Hao, MIN Jian-bin, HUANG Xiao-tao, et al. Pharmacokinetics Analysis of Geniposidic Acid in Normal and Cholestatic Rats[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(17): 75-78. DOI： 10.13422/j.cnki.syfjx.2015170075.

摘要

目的: 京尼平苷酸(GPA)具有利胆作用

研究该成分在胆汁淤积病理模型状态下体内代谢过程的差别。方法: 大鼠随机分为正常组和α-萘异硫氰酸酯(ANIT剂量100 mg·kg-1)诱导胆汁淤积模型组

给予不同剂量GPA(高、中、低剂量分别为100

25 mg·kg-1)。采用蛋白沉淀法对大鼠血浆进行处理

建立以绿原酸为内标的HPLC-UV检测方法

流动相乙腈-0.5%冰乙酸(28:72)

检测波长238 nm

利用Stata12.0软件拟合房室模型并计算各组大鼠的药动学参数。结果: ANIT造胆汁淤积模型成功率>95%。与正常组相比

胆汁淤积模型降低了GPA在体内的消除速率常数(Ke)

延长了在体内的平均驻留时间(MRT0-t)和半衰期(t1/2)

提高了药时曲线下面积AUC0-t和AUC0-∞。结论: 该分析方法满足了京尼平苷酸体内药物分析的要求

胆汁淤积模型可降低京尼平苷酸的消除和排泄。

Abstract

Objective: Geniposidic acid (GPA) can promote bile acid excretion

its metabolism process difference was studied in cholestatic model for development clinical role. Method: Rats were divided into the normal group and the cholestatic model group induced by α-naphthyl isothiocyanate (ANIT

dose of 100 mg·kg-1)

different doses of GPA were administered (high

medium and low doses of 100

25 mg·kg-1).GPA and chlorogenic acid were extracted from plasma by protein precipitation

separated on phenomenex C18 column with a mobile phase of acetonitrile and water containing 0.5% acetic acid with rate of (28: 72)

detection wavelength was at 238 nm.Stata12.0 was adopted to fit compartment model and calculate pharmacokinetic parameters. Result: ANIT cholestasis model made a success rate of more than 95%.Compared with the normal group

rat with cholestasis model might reduce Ke and increase T1/2 of GPA in vivo

and might extend the mean residence time (MRT0-t) in vivo

also might improve AUC0-t and AUC0-∞. Conclusion: This analytical method is suitable and reliable for in vivo analysis of GPA

cholestasis model can reduce elimination and excretion of GPA.

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Related Institution

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

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