Comparison of Pharmacokinetics between Reduning Injection and Geniposide Monomer in Rats

ZHENG Wei-hua; WANG Yan-juan; LIANG Jia-jia; YANG Li-na; ZHANG Li-li; XIAO Wei; FU Xiao-huan; LI Fa-mei; XIONG Zhi-li

doi:10.11653/syfj2014030095

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Comparison of Pharmacokinetics between Reduning Injection and Geniposide Monomer in Rats

更新时间：2024-01-04

- Comparison of Pharmacokinetics between Reduning Injection and Geniposide Monomer in Rats
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 20, Issue 3, Pages: 95-99(2014)
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- DOI：10.11653/syfj2014030095
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- Published：2014
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ZHENG Wei-hua, WANG Yan-juan, LIANG Jia-jia, et al. Comparison of Pharmacokinetics between Reduning Injection and Geniposide Monomer in Rats [J]. Chinese journal of experimental traditional medical formulae, 2014, 20(3): 95-99.
DOI：

ZHENG Wei-hua, WANG Yan-juan, LIANG Jia-jia, et al. Comparison of Pharmacokinetics between Reduning Injection and Geniposide Monomer in Rats [J]. Chinese journal of experimental traditional medical formulae, 2014, 20(3): 95-99. DOI： 10.11653/syfj2014030095.

摘要

目的：建立RP-HPLC测定大鼠血浆中栀子苷质量浓度的方法，比较热毒宁注射液中栀子苷与栀子苷单体在大鼠体内的药动学特点。方法：将12只雄性SD大鼠随机等分成2组，分别尾静脉注射热毒宁注射液和栀子苷单体，于不同时间点眼眶采血，以紫丁香苷为内标，血浆用乙腈沉淀蛋白，流动相乙腈-水（14：86），经Agela C18色谱柱（4.6 mm×150 mm，5 μm）分离，检测波长238 nm，采用PhoenixTM WinNonlin 6.1软件计算药动学参数。结果：栀子苷在0.100~120 mg·L-1线性关系良好（r=0.998 7），定量下限0.100 mg·L-1，低、中、高质量浓度的血浆样品的提取回收率分别为（85.9±1.7）%，（96.6±2.3）%，（97.4±1.1）%。大鼠尾静脉注射给予热毒宁注射液和栀子苷单体后栀子苷在大鼠体内的药动学过程均符合二室模型，t1/2分别为（0.58±0.11），（0.55±0.20） h，MRT0-t分别为（0.41±0.05），（0.33±0.05） h，二者的主要药动学参数均无显著性差异。结论：建立的方法灵敏、快速、准确，适用于栀子苷在大鼠体内的药动学研究。热毒宁注射液中其他成分对栀子苷在大鼠体内药动学行为无显著性影响。

Abstract

Objective: To establish a RP-HPLC method to determine plasma concentration of geniposide in rats

and compare pharmacokinetic characteristics of geniposide in Reduning injection and geniposide monomer in rats. Method: Twelve male SD rats were divided into two groups randomly

which were injected Reduning injection and geniposide by tail vein

respectively.Orbital blood at different time points

with syringoside as internal standard

plasma was precipitated proteins with acetonitrile and centrifuged at 13 000 r·min-1 for 10 min.RP-HPLC analysis was performed on an Agela C18 column(4.6 mm×150 mm

5 μm) with acetonitrile-water(14:86) as mobile phase

main pharmacokinetics parameters were calculated with PhoenixTM WinNonlin 6.1 software. Result: Geniposide showed good linearity in 0.100-120 mg·L-1 with r=0.998 7

the lowest limit of quantization of geniposide was 0.100 mg·L-1

the mean extraction recoveries of plasma samples with low

medium and high concentration were (85.9±1.7)%

(96.6±2.3)% and (97.4±1.1)%

respectively.Concentration-time profiles of geniposide were fitted with the two-compartment model both for Reduning injection and geniposide monomer

t1/2 were (0.58±0.11) and (0.55±0.20) h

MRT0-t were (0.41±0.05) and (0.33±0.05) h

respectively

main pharmacokinetic parameters had no significant differences between Reduning injection and geniposide monomer. Conclusion: This developed method was sensitive

rapid and accurate for investigating pharmacokinetics of geniposide in rats.Experimental results showed that the other constituents in Reduning injection have no significant impact on pharmacokinetics of geniposide in rats.

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Related Institution

School of Life Sciences，Beijing University of Chinese Medicine

School of Pharmacy，Shanghai University of Traditional Chinese Medicine

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