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目的研究山楂叶总黄酮组分中代表成分的平衡溶解度与油水分配系数,比较其相似性,为山楂叶总黄酮组分整体水溶性和脂溶性的表征奠定基础。方法以山楂叶总黄酮组分为模型药物,选择芦丁、槲皮素、金丝桃苷为代表性成分,用HPLC法同时测定各成分在不同pH值的缓冲液及水中的平衡溶解度和表观油水分配系数(P_(app)),运用向量余弦法(cosine)和格鲁布斯法(Grubbs)评价其相似性。色谱条件:色谱柱为Zorbax Eclipse Plus C_(18)柱(250 mm×4.6 mm,5μm),流动相为乙腈(A)-0.4%磷酸水溶液(B),梯度洗脱:0~10 min,20%乙腈;10~11 min,20%~40%乙腈;11~20 min,40%乙腈;20~21 min,40%~20%乙腈;21~25 min,20%乙腈;检测波长为360 nm;体积流量为0.8 mL/min;柱温为40℃。结果芦丁、槲皮素、金丝桃苷在不同pH值缓冲液及水中的平衡溶解度及P_(app)均相似,在不同pH值缓冲溶液中芦丁、槲皮素和金丝桃苷3个成分平衡溶解度的cosine值分别为0.998、0.988、0.987,P_(app)的cosine值分别为0.976、0.981、0.978,cosine值均大于0.9,芦丁、槲皮素和金丝桃苷平衡溶解度的Grubbs值分别为1.057、1.083、1.124、1.117、1.022、1.030、1.082、1.112,P_(app)的Grubbs值分别为1.125、1.107、1.079、1.034、1.041、1.037、1.129、1.128,Grubbs检验结果均小于G临界值1.153,相似性良好。结论相似性分析客观地反映了组分内各成分性质的离散程度,可增加组分性质评价的科学性,为中药组分的制剂设计提供依据。
Objective To study the equilibrium solubility, oil-water partition coefficient and the similarity of representative components in the total flavonoids of hawthorn leaves, and lay a foundation for the overall water-solubility and fat-soluble characterization of the total flavonoid components of hawthorn leaves. Methods The total flavonoids of hawthorn leaves were used as model drugs. Rutin, quercetin and hyperoside were selected as the representative components. The equilibrium solubility of each component in different pH buffers and water was determined by HPLC Oil and water distribution coefficient (P_ (app)) was evaluated by cosine and Grubbs. The chromatographic conditions were as follows: the column was Zorbax Eclipse Plus C 18 column (250 mm × 4.6 mm, 5 μm), the mobile phase consisted of acetonitrile-0.4% phosphoric acid solution (B), gradient elution: 0-10 min, % Acetonitrile; 10-11 min, 20-40% acetonitrile; 11-20 min, 40% acetonitrile; 20-21 min, 40% -20% acetonitrile; 21-25 min, 20% acetonitrile; ; Volume flow rate was 0.8 mL / min; column temperature was 40 ℃. Results The equilibrium solubility and P_ (app) of rutin, quercetin and hyperoside in different pH buffers and water were similar. Rutin, quercetin and hyperoside 3 in different pH buffer solutions The cosine values of the equilibrium solubility of the components were 0.998,0.988 and 0.987, respectively. The cosine values of P app were 0.976, 0.981 and 0.978, respectively. The cosine values were all higher than 0.9. The equilibrium solubility of rutin, quercetin and hyperoside Grubbs values were 1.057,1.083,1.124,1.117,1.022,1.030,1.082,1.112 respectively. The Grubbs values of P app were 1.125, 1.107, 1.079, 1.034, 1.041, 1.037, 1.129 and 1.128, respectively. The Grubbs test results were less than G critical value of 1.153, similarities. Conclusion Similarity analysis objectively reflects the discrete nature of the components in the components, which can increase the scientific nature of the component properties evaluation and provide the basis for the formulation design of the traditional Chinese medicine components.