黄连血中移行成分经时变化规律探讨

Investigation of Time Change Rule of Compositions Derived from Coptidis Rhizoma Absorbed into the Blood

摘要:

目的: 通过分析黄连血中移行成分的经时变化规律,明确黄连体内的直接作用物质基础及体内代谢过程.方法: 采用中药血清药物化学方法研究黄连进入体内后化学成分的分布、数目、存在状态(原型成分或代谢产物)及其随时间的变化.结果: 认定了黄连给药后9个血中移行成分中的5个成分(表小檗碱、药根碱、黄连碱、巴马汀、盐酸小檗碱);除2号峰经分析认定为代谢产物外,其他色谱峰均是以原型形式进入体内而存在.3,4,5,6,7,8,9号峰被吸收入血后,在一定时间内血药浓度达峰值(120 min),达峰时间均较长,而后随着血液循环在体内消除.3,4号峰吸收入血后,血药浓度降低,但相对含量呈上升趋势,说明有其他成分向其转化.结论: 黄连血中移行成分中主体成分在给药后60 min可检测到,120 min达峰值,240 min时的含量与60 min时相当;少量成分存在其他成分向其转化的特点.通过给药后血中移行成分分析可确定药物在体内直接作用的物质,根据该移行成分的经时变化规律可建立中药的科学给药方案及配伍用药方案.

Abstract:

Objective:Through studying time change rule of compositions derived from Coptidis Rhizoma absorbed into the blood, to clear in vivo directly effective substance and metabolic process of Coptidis Rhizoma. Method: Serum pharmacochemistry method was adopted to study distribution, number and state(prototype components or metabolites) of chemical compositions from Coptidis Rhizoma absorbed into the body, then investigate its variation with time. Result: This study determined five components(epiberberine, jateorhizine, coptisine, palmatine and berberine hydrochloride) among these nine components from Coptidis Rhizoma absorbed into the body;in addition to peak 2 identified as metabolites by analysis, other peaks were in prototype form into the body.After peak 3, 4, 5, 6, 7, 8, 9 were absorbed into the blood, blood drug concentration reached its peak in a certain period of time(120 min), peak time was longer, and then was eliminated with the blood circulation in the body.After peak 3 and 4 were absorbed into the blood, blood drug concentration decreased, but their relative contents were increased, which indicated conversion of other components to them. Conclusion: Main components of compositions derived from Coptidis Rhizoma absorbed into the blood can be detected at 60 min after administration, they reach peak value at 120 min, their contents at 240 min are similar to these at 60 min;minor components can be transformed from other components.Effective components directly in the body may be determined by analyzing components of drugs from serum after taking medicines orally, scientific administration and combination scheme of traditional Chinese medicine can establish by according to change rule of components from serum after taking medicines orally.