基于解痉效应表征的香连丸多成分整合溶出度研究

Study on multi-component integration dissolution of Xianglian pills based on spasmolytic effect

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 practicability of multi-component integration dissolution of Xianglian pills based on the spasmolytic effect.METHODS Small glass method and isolated rabbit intestinal muscle tests were adopted to estimate the spasmolytic effect of the dissolution liquid of Xianglian pills on myenteric motion stimulated by acetylcholine and barium chloride at different time points,determine the inhibition rate of amplitude and frequency of intestinal muscle contraction,calculate the biological activity dissolution based the inhibition rate of intestinal muscle contraction.With f2 as the similarity factor,high performance liquid chromatography was used to determine costunolide and dehydrocostuslactone,establish the integration dissolution curve and perform correlation analysis.RESULTS The values of f2 between the integration dissolution curves and costunolide,dehydrocostuslactone,biological activity curves in sequence were 77.7,94.8,55.2,all more than50,indicating that integration dissolution curve was similar with biological activity curve and two component curves.CONCLUSION Multi-component integration dissolution can express the biological effect of Xianglian pills to inhibit intestinal muscle contraction,which is feasible to evaluate the dissolution of traditional Chinese medicine preparation guided by biological effect.