附子总生物碱在阳虚便秘模型大鼠体内的整合药动学分析

李燕; 彦培傲; 赵梦杰; 袁岸; 龚小红; 赵梦君; 李芸霞; 彭成

doi:10.13422/j.cnki.syfjx.2017010079

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附子总生物碱在阳虚便秘模型大鼠体内的整合药动学分析

药物代谢 | 更新时间：2024-01-04

- 附子总生物碱在阳虚便秘模型大鼠体内的整合药动学分析
- Integrated Pharmacokinetics of Total Alkaloids from Aconiti Lateralis Radix Praeparata in Rats with Constipation Due to Insufficiency of Spleen-Yang and Kidney-Yang
- 中国实验方剂学杂志 2017年23卷第1期页码：79-84
- 作者机构：
- 作者简介：
- 基金信息：
  
  国家自然科学基金项目（81373943，81573583）;四川省杰出青年基金项目（2013JQ0018）;四川省科技厅省青年科技创新研究团队专项（2014TD0007，2015TD0028）
- DOI：10.13422/j.cnki.syfjx.2017010079
  中图分类号： R-332;R256.23
- 纸质出版日期：2017
- 稿件说明：
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李燕, 彦培傲, 赵梦杰, 等. 附子总生物碱在阳虚便秘模型大鼠体内的整合药动学分析[J]. 中国实验方剂学杂志, 2017,23(1):79-84.

LI Yan, YAN Pei-ao, ZHAO Meng-jie, et al. Integrated Pharmacokinetics of Total Alkaloids from Aconiti Lateralis Radix Praeparata in Rats with Constipation Due to Insufficiency of Spleen-Yang and Kidney-Yang[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(1): 79-84.
李燕, 彦培傲, 赵梦杰, 等. 附子总生物碱在阳虚便秘模型大鼠体内的整合药动学分析[J]. 中国实验方剂学杂志, 2017,23(1):79-84. DOI： 10.13422/j.cnki.syfjx.2017010079.

LI Yan, YAN Pei-ao, ZHAO Meng-jie, et al. Integrated Pharmacokinetics of Total Alkaloids from Aconiti Lateralis Radix Praeparata in Rats with Constipation Due to Insufficiency of Spleen-Yang and Kidney-Yang[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(1): 79-84. DOI： 10.13422/j.cnki.syfjx.2017010079.

摘要

目的：研究大黄蒽醌类成分与附子总生物碱组分配伍灌胃后，附子总生物碱在阳虚便秘模型大鼠体内的整合药动学特征。方法：将大鼠分正常组和便秘组，后者依次灌胃附子总生物碱（19.2 mg·kg-1）和大黄蒽醌类成分（38.4 mg·kg-1），采用UHPLC-Q/TOF-MS测定7种成分（乌头碱、新乌头碱、次乌头碱、苯甲酰乌头原碱、苯甲酰新乌头原碱、苯甲酰次乌头原碱、乌头原碱）在不同时间点的血药浓度，流动相乙腈-0.1%甲酸水溶液梯度洗脱，流速0.25 mL·min-1，检测波长200~400 nm，电喷雾离子化源，正离子模式检测，绘制药-时曲线，计算整合药动学参数。结果：与正常组比较，便秘组乌头碱、次乌头碱、苯甲酰乌头原碱、苯甲酰新乌头原碱、苯甲酰次乌头原碱和乌头原碱的整合药动学参数药峰浓度（Cmax）和药-时曲线下面积（AUC0-∞）升高，代谢加快；新乌头碱的AUC0-∞与正常大鼠相近，半衰期（t1/2）延长，其在正常大鼠体内代谢更快。结论：附子总生物碱整合药动学数据仍具有明显的药动学过程特征，且与7种生物碱类成分各自的药动学特征基本一致，可表达上述生物碱类成分整体的药代动力学行为。

Abstract

Objective: To investigate in vivo integrated pharmacokinetic characteristics of total alkaloids from Aconiti Lateralis Radix Praeparata in rats with constipation due to insufficiency of spleen-Yang and kidney-Yang after compatibility with anthraquinones from Rhei Radix et Rhizoma. Method: Rats were equally divided into the normal group and the constipation group.Extracts including 19.2 mg·kg-1 of total alkaloids from Aconiti Lateralis Radix Praeparata and 38.4 mg·kg-1 of anthraquinones from Rhei Radix et Rhizoma were given to the constipation group

respectively.UHPLC-Q/TOF-MS was established to determine plasma concentration of seven ingredients at different time points

several concentration-time curves were drawn and pharmacokinetic parameters were calculated and integrated. Result: In addition to mesaconitine

the maximum plasma concentration (Cmax) and the area under the plasma concentration-time curve in all time points (AUC0-∞) of six alkaloids (aconitine

hypaconitine

benzoylaconitine

benzoylmesaconine

benzoylhypaconitine and aconine) were higher

and the metabolism was faster in the constipation group than these in the normal group.Compared with the constipation group

the metabolism of mesaconitine in the normal group was faster

because its t1/2 was shorter

but its AUC0-∞ was similar to each other. Conclusion: At the same time

integrated pharmacokinetic characteristics of total alkaloids in Aconiti Lateralis Radix Praeparata are basically consistent with these of seven alkaloids

it can represent the integrated pharmacokinetic behavior of the above alkaloids.

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