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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。
OBJECTIVE: To determine the direct substance of action and the metabolic process in the body of Rhizoma Coptidis by analyzing the regularity of migration of Rhizoma Coptidis. Methods: The distribution, number, existing state (prototypical components or metabolites) of chemical constituents of Rhizoma Coptidis after entering into the body were studied by serum medicinal chemistry method and their changes with time. Results: Five components (epiberberine, jatrorrhizine, palmatine, berberine) of the nine blood components in the blood after the administration of berberine were identified. Except for the No. 2 peak, it was identified as Metabolites, the other peaks are based on the prototype into the body and exist. 3, 4, 5, 6, 7, 8 and 9 peaks were absorbed into the blood, within a certain period of time the peak plasma concentration (120 min), the peak time is longer, and then with the blood circulation in the body to eliminate . 3,4 peak absorption into the blood, plasma concentration decreased, but the relative content increased, indicating that there are other components to their conversion. CONCLUSION: The main constituents in the migratory component of Coptis chinensis can be detected at 60 min after administration, reaching the peak at 120 min. The content at 240 min is comparable with that at 60 min. The minor components have the characteristics of other components being transformed into them. Through the analysis of blood components in the blood after administration, it is possible to determine the substance that acts directly on the body in the body. According to the variation of the migration component over time, a scientific dosing scheme and a compatible dosing scheme of the traditional Chinese medicine can be established.