基于药物体系的连翘饮药物制备物质量表征分析研究

Quality-representation of medicinal-preparation of Lianqiao Yin based on medicinal system

目的基于药物体系建立连翘饮制备物有效指标性成分的含量测定方法,进行药物制备物质量表征关联分析研究,并确定影响质量的关键因素,为创制连翘饮优质抗菌药物奠定基础。方法采用所建立的HPLC-DAD分析法测定连翘饮制备物有效指标性成分的含量。体外抗菌作用强度考察采用纸片扩散法,观察抑菌圈直径大小的变化;体内抗菌作用考察,采用金黄色葡萄球菌的5%干酵母悬液,腹腔感染给药小鼠,观察小鼠在染菌后7 d内的死亡率和平均存活时间。结果连翘饮药物制备物有效指标性成分即栀子苷、升麻素苷、升麻素、甘草苷、连翘酯苷A、5-O-甲基维斯阿米醇苷、连翘苷、甘草酸的线性关系良好,加样回收率合格。3种药物制备物体内、外均表现出抗菌作用,抗菌作用大小为:富集物>稀醇提取物>水提取物。连翘饮药物制备物药学-药效质量表征关联分析可知,在3种制备物中,尤以富集物中有效指标性成分的含量较高、比例独特、出膏率较低,药物用量较小,抗菌作用较强。结论基于药物体系建立的连翘饮有效指标性成分的含量测定方法操作简便、准确灵敏、重复性好,可用于连翘饮药物制备物质量表征研究。基于药物体系的基本组成及其制备得率,提高关键有效成分的含量,优化组成比例,是提升药物药效的关键要素。

Objective To establish the method of quantitative determination for effective index components of medicinal-preparation of Lianqiao Yin based on medicinal system, analyze quality-representation correlation, insure key factors influencing quality and prepare antimicrobial agents with high quality from Lianqiao Yin. Methods The content of effective index components of medicinal-preparation of Lianqiao Yin was detected by using HPLC-DAD. According to the size of the antibacterial annulus, use paper disk method to determine the antibacterial effect of drug-preparation in vitro. In vivo, Staphylococcus aureus was cultured for 18 hours and 5 % yeast liquor was inoculated into the abdominal cavity of mice who had given medicine. Death rate and average survival time were observed and analyzed within 7days after being infected. Results The effective index components gardenosid （GD）; prim-O-glucosylcimifugin （PGCN） ; cimifugin （ CN ） ; liquiritin （ LQR ） ; forsythoside A （ FTA ） ; 4 ＇-O-D-glucosyl-5-O- methylvisamminol （ GMV ） ; phillyrin （ Phil ） ; glycyrrhizic acid （ GZA ）, of medicinal-preparation of Lianqiao Yin showed a good linear relationship, and qualified average recovery. All 3 kinds of medicinal- preparation had antibacterial effects in vivo and in vitro, and their descending order was as follows： enrichment 〉 alcohol extract 〉 water extract. According to the medicine-efficacy correlation analysis, among 3 medicinal-preparation, the content of effective index components is higher in enrichment with unique proportion, lower extraction rate, lower dosage and higher antibacterial effect, which is the best medicinal-preparation application form of Lianqiao Yin. Conclusion The method is simple, accurate and sensitive with good repetition, which can be used in the study on quality-representation of medicinal- preparation of Lianqiao Yin. Based on the basic composition and extraction rate of medicinal system, the key factor for increasing medicinal efficacy is to promoting relative effective components and optimizing their proportion.