黄芩制剂制备过程成分含量变化及其药效相关性研究

Correlation between chemical composition and pharmacological activity of Scutellaria baicalensis during its preparation process

目的探讨黄芩制剂制备过程中主要指标性成分含量变化与其药效活性间的相关性,阐明黄芩制剂制备过程的关键影响环节,质量源于设计角度整体评价制剂质量疗效短板。方法模拟黄芩制剂制备过程(提取-浓缩-干燥-制粒),HPLC法测定各阶段化学成分的含量变化;以脂多糖(LPS)诱导小鼠腹腔巨噬细胞为炎症模型,测定各阶段中间体溶液的抗炎活性;聚类分析法和线性回归法对指标性成分-药效活性数据进行相关分析。结果提取-浓缩-干燥-制粒等过程中黄芩化学成分含量与其抗炎活性整体呈下降趋势,其中长时间热处理(浓缩、干燥)损失较大。结论黄芩制剂制备过程中的各阶段操作水平对其指标成分含量及药效活性影响显著,其中浓缩、干燥环节为影响其制剂质量的关键环节。

Objective Process design grants the quality connotation to products. To study the changes of main chemical ingredient of Scutellaria baicalensis preparation in the preparation process and the correlation with its pharmacological activity. To clarify the key step of S. baicalensis preparation process, and overall evaluate the short plate of the quality of preparation from the perspective of the design. Methods The preparation process（extracting-concentrating-drying-granulation） was simulated. HPLC analysis was employed to determine the contents of the chemical ingredients in each step of preparation process. Induction by LPS in mouse peritoneal macrophages of each intermediate was used as the model to determinate the anti-inflammatory activity. Cluster analysis and linear regression were used to analyze the correlation between its chromatogram and pharmacological activity. Results The content of chemical ingredients and anti-inflammatory activity of S. baicalensis were generally decreased on the whole, and the highest loss occurred in the concentrating-drying process. Conclusion Each step of the preparation process of S. baicalensis preparation has significant effect on the chemical ingredients and pharmacological activity. The concentrating and drying process may be the key process which could finally influence the quality of preparation.