首页|白芥子穴位给药配伍对延胡索乙素药效动力学影响的研究

白芥子穴位给药配伍对延胡索乙素药效动力学影响的研究

扫码查看
原文链接
  • 万方数据
  • 维普
目的:探讨"冬病夏治"全方配伍和无白芥子配伍延胡索乙素在模型家兔"肺俞"穴皮下药代动力学特征及药代动力学-药效动力学(PK-PD)模型的相关性.方法:支气管哮喘模型家兔随机分成延胡索单方组、缺白芥子组、全方组,微透析技术收集14 h穴位皮下透析液,液相色谱-质谱法(Liquid Chromatography Mass Spectrometry,LCMS)法检测方中君药延胡索主要成分延胡索乙素浓度,获得药代动力学参数;酶联免疫吸附试验(ELISA)法检测对应时间点模型动物血清中IgE水平,获得药效学参数;对药动学、药效学参数进行PK-PD模型拟合.结果:白芥子配伍后的药峰浓度(Cmax)、药时曲线下面积(AUC0-t)、平均滞留时间(MRT0-t)均显著增加(P＜0.01,P＜0.01,P＜0.05),达峰时间(Tmax)提前(P＜0.01);"浓度-时间-效应"三维曲线表明,方中有白芥子配伍时,药效出现更快、消退更慢,起效时间晚于峰浓度,具有一定滞后性.结论:动力学参数、PK-PD模型结果表明,白芥子配伍能够改变"方中君药——延胡索的主要成分延胡索乙素穴位局部的皮下分布,促进方中君药有效成分快速吸收,延长滞留时间,在方剂中起到主药、改善其他药物分布的"双重"作用.
Pharmacokinetic Effect of the Compatibility of Sinapis alba Acupoint Administration with Tetrahydropalmatine
Objective:To explore the pharmacokinetic characteristics of the full compatibility of tetrahydropalmatine without sinapis alba in the subcutaneous administration of the"Fei Shu"acupoint in a model rabbit and investigate the correlation between phar-macokinetics-pharmacodynamics(PK-PD)according to the principle of"treating winter disease in summer".Methods:Bronchial asthma model rabbits were randomly divided into yanhusuo alone group,sinapis alba absence group,and full prescription group.Mi-crodialysis technique was used to collect subcutaneous dialysate at the"Fei Shu"acupoint for 14 hours.Liquid chromatography mass spectrometry(LCMS)was employed to detect the concentration of the main component tetrahydropalmatine which is the sover-eign medicine in a prescription,obtaining pharmacokinetic parameters.Enzyme-linked immunosorbent assay(ELISA)was per-formed to detect the IgE level in the serum of model animals at corresponding time points,obtaining pharmacodynamic parameters.PK-PD model fitting was conducted for pharmacokinetic and pharmacodynamic parameters.Results:After compatibility of sinapis alba,the peak concentration(Cmax),the area under the curve(AUC0-t)and the mean retention time(MRT0-t)significantly in-creased(P＜0.01,P＜0.01,P＜0.05)and the time to reach peak concentration(Tmax)was earlier(P＜0.01).The three-dimen-sional"concentration-time-effect"curve showed when sinapis alba was compatible,the drug effect appeared faster,disappeared more slowly,and the onset time was later than the peak concentration,indicating a certain lag.Conclusion:The pharmacokinetic parameters and PK-PD model results suggest that the compatibility of sinapis alba may change the subcutaneous distribution of the main component,tetrahydropalmatine,at the acupoint after administration.This promotes the rapid absorption of effective compo-nents of the sovereign drug and prolongs the residence time,playing a'dual'role as the principal drug and improving the distribu-tion of other drugs in the prescription.

Sinapis albaAcupoint drug administrationCompatibility studyTetrahydropalmatinePK-PD model"Treating winter disease in summer"Three-dimensional"concentration-time-effect"relationshipLagging curve

高远、李冀、韩东卫、周梦丹

展开 >

贵州中医药大学药学院,贵阳,550025

黑龙江中医药大学,哈尔滨,150040

贵州医科大学附属医院针灸科,贵阳,550001

白芥子 穴位给药 配伍研究 延胡索乙素 药代动力学-药效动力学模型 "冬病夏治"方 浓度-时间-效应"三维关系 滞后曲线

国家自然科学基金地区科学基金项目中国博士后科学基金面上资助项目

822608852020M670942

2024

10.3969/j.issn.1673-7202.2024.01.003

世界中医药
世界中医药学会联合会

世界中医药

CSTPCDCHSSCD北大核心
影响因子：1.266
ISSN：1673-7202
年,卷(期)：2024.19(1)
  • 22