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目的:探讨基于解痉效应表征的香连丸多成分整合溶出度评价的可行性。方法:采用小杯法和家兔离体肠肌实验,考察不同时间点的香连丸溶出液对乙酰胆碱、氯化钡引起肠肌收缩的解痉作用,测定药物对肠肌收缩张力与频率的抑制率,并计算基于肠肌收缩抑制率的生物效应溶出度,并以f2相似因子法,与高效液相色谱法测定木香烃内酯、去氢木香内酯及两者加权整合后的溶出曲线进行相关性评价。结果:整合溶出曲线与木香烃内酯、去氢木香内酯、生物效应溶出曲线的f2值分别为77.7、94.8、55.2,均大于50,表明整合溶出曲线与生物效应及单体成分的溶出曲线均相似。结论:多成分加权整合的溶出度能反映香连丸拮抗肠肌痉挛性收缩的生物效应,建立基于生物效应为导向的中药制剂多成分整合溶出度评价方法具有可行性。
OBJECTIVE: To investigate the feasibility of multi-component integrated dissolution evaluation of XiangLian pill based on the characterization of antispasmodic effect. Methods: Small cup method and intestinal muscle in vitro experiments to investigate the different time points Xianglian pill dissolution of acetylcholine, barium chloride induced contraction of the spasm of the spasm, measured the effect of drugs on the contraction of muscle tension and frequency Inhibition rate, and calculate the effect of dissolution of biological effects based on inhibition rate of intestinal muscle contraction, and f2 similar factor method, and high performance liquid chromatography determination of wood ketone lactone, dehydrocostus lactone and the weighted integration of the two Dissolution curve correlation evaluation. Results: The f2 values of dissolution dissolution curve, lignocellulose lactone, dehydrocostus lactone and bio-effect dissolution curve were 77.7, 94.8 and 55.2 respectively, both of which were greater than 50, indicating that the dissolution curves and bioeffects of monomer and Dissolution curves are similar. CONCLUSION: The dissolution of multi-component weighted integration can reflect the biological effect of Xiang-Lian-Pill in antagonizing the spastic contraction of intestinal muscles. It is feasible to establish a multi-component integrated dissolution evaluation method based on biological effects.