目的 分析不同配比“黄连-苦参”药对的特征性成分量-质变化相关性，为该药对的量-效相关性及临床应用提供合理的用量比例参考。方法 采用HPLC法，建立不同配比9批“黄连-苦参”药对（5∶1、4∶1、3∶1、2∶1、1∶1、1∶2、1∶3、1∶4、1∶5），建立药对HPLC特征指纹图谱及其特征性成分含量测定方法，分析9组样品成分的差异性与相关性。结果 9种配比的黄连-苦参药对共确定16个共有峰，指认苦参碱、槐定碱、氧化苦参碱、木兰花碱、非洲防己碱、表小檗碱、药根碱、黄连碱、巴马汀、小檗碱共10个共有峰。含量测定结果显示，黄连-苦参配对后相比黄连药材及苦参药材，特征性成分均有显著性差异。黄连-苦参（5∶1）时苦参碱、槐定碱、木兰花碱含量为各比例最高，相比单药材提取具有显著性差异；黄连-苦参（4∶1）时，非洲防己碱、表小檗碱、黄连碱、巴马汀、小檗碱含量为各比例最高，相比单药材提取具有显著性差异，且黄连总生物碱溶出最高；黄连-苦参（1∶1）时苦参总生物碱含量最高，且药根碱含量为各比例最高；黄连-苦参（1∶3）时氧化苦参碱含量为各比例最高。结论 黄连-苦参不同配比时，以特征性成分个数与含量为标示的“质”与配伍用“量”之间的相关差异性较明显，显示出一定的成分相互促溶作用。苦参中3种成分的溶出量随黄连比例的降低呈现“U”型分布，而黄连中7种成分溶出量随黄连比例的降低整体呈现降低趋势。与黄连、苦参各药材单提相比，各比例下苦参中总生物碱类成分的溶出均有不同程度的提升，黄连中总生物碱类成分在黄连-苦参（5∶1）及（4∶1）比例下溶出表现为提升，其他比例表现为降低。药对中生物碱类成分的溶出规律与临床验方中药对的使用配比成正相关。为进一步开展该药对的量-效关联性分析确定了物质基础，也为临床潜方时确定适宜用量提供参考。

Objective Based on the classic prescriptions and the commonly used Huanglian (Coptidis Rhizoma, CR)-Kushen (Sophprae Flavescentis Radix, SFR) herb pair in the clinical prescriptions of masters of traditional Chinese medicine (TCM), the quantity-quality change correlation of the characteristic components of the herb pair with different ratios was analyzed, and the quantity-effect correlation of the herb pair was analyzed. and clinical application to provide a reasonable dosage ratio reference. Methods HPLC method was used to establish nine batches of CR-SFR herb pairs with different ratios (5:1, 4:1, 3:1, 2:1, 1:1, 1:2, 1:3, 1:4, 1:5), establish the HPLC characteristic fingerprint of the herb pair and the content determination method of its characteristic components, and analyze the differences and correlations of the components of the nine groups of samples. Results A total of 16 common peaks were determined in the CR-SFR herb pair of nine ratios, and ten common peaks were identified for matrine, sophoridine, oxymatrine, magnoflorine, columbamine, epberberine, jatrorrhizine, coptisine, palmatine and berberine. The content measurement results showed that after the pairing of CR and SFR, there were significant differences in the characteristic components compared with CR and SFR. CR-SFR (5:1) has the highest content of matrine, sophoridine and magnolinine in each ratio, and there is a significant difference compared with the extraction of single medicinal materials; CR-SFR (4:1). At that time, the contents of African fanghepine, epiberberine, coptisine, palmatine, and berberine were the highest in each ratio. Compared with the extraction of single medicinal materials, there was a significant difference, and the total alkaloids of CR had the highest dissolution; CR-SFR (1:1), the total alkaloid content of SFR is the highest, and the content of jatrorrhizine is the highest among all ratios; the CR-SFR (1:3) condition is the highest oxymatrine content among all ratios. Conclusion When CR-SFR is mixed in different proportions, the correlation between the quality indicated by the number and content of characteristic ingredients and the quantity used for compatibility is more obvious, showing a certain mutual solubility-promoting effect of the ingredients. The dissolution amounts of the three components in SFR showed a “U”-shaped distribution as the proportion of CR decreased, while the dissolution amounts of the seven components in CR showed an overall decreasing trend as the proportion of CR decreased. Compared with CR and SFR alone, the dissolution of total alkaloids in SFR was improved to varying degrees at each ratio. The total alkaloids in CR were in CR-SFR (5:1) and (4:1) ratio showed an increase in dissolution, while other ratios showed a decrease. The dissolution pattern of alkaloid components in the drug pair is positively correlated with the ratio of the herb pair used in clinical prescriptions. This study determines the material basis for further carrying out the “dose-effect” correlation analysis of this drug pair, and also provides a reference for determining the appropriate dosage when preparing clinical prescriptions.

R283.6

国家重点研发计划（2017YFC1700602）