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目的:考察二至丸水蜜丸和配方颗粒中5种药效活性成分的溶出情况,比较这些成分在2种剂型中的体外溶出特点。方法:参照《中国药典》2010年版二部附录X C溶出度测定法,采用第二法桨法,转速75 r·min-1,测试不同溶出介质(水,30%乙醇,0.1 mol·L-1盐酸和p H 4.5,6.8的磷酸盐缓冲液)。利用UPLC测定2种剂型中红景天苷、特女贞苷、女贞苷、木犀草素和齐墩果酸5种药效成分的体外溶出度,比较2种制剂的溶出行为。结果:在各个溶出介质中,二至丸2种不同制剂中各活性成分的溶出行为差别很大,配方颗粒中红景天苷、特女贞苷、女贞苷在各个介质里都能快速溶出且溶出量高(>85%);而水蜜丸中木犀草素和齐墩果酸只能在p H 6.8磷酸盐缓冲液中溶出很少的量(<30%)。从差异因子和相似因子分析,2种制剂中相同成分的溶出曲线无相似性。结论:和水蜜丸相比,配方颗粒中活性成分的累积溶出量更高,且在同一种溶出介质中,能溶出更多的药效成分。说明在体外溶出方面,配方颗粒这种新型的中药形式具有更大的优势。建立的溶出度方法可以应用于二至丸制剂的质量控制。
OBJECTIVE: To investigate the dissolution of five active ingredients from Erzhi Pill and prescription granules, and to compare the dissolution characteristics of these two ingredients in vitro. Methods: According to the XC dissolution assay of Appendix of Chinese Pharmacopoeia (2010 edition), the second method of paddle method was used to test the effect of different dissolution media (water, 30% ethanol, 0.1 mol·L-1 Hydrochloric acid and pH 4.5, 6.8 phosphate buffer). UPLC was used to determine the in vitro dissolution rates of salidroside, lentinum, virginia, luteolin and oleanolic acid in two different formulations. The dissolution profiles of the two formulations were compared. RESULTS: In each dissolution medium, the dissolution behavior of each active ingredient in two different preparations of Erzhi Pills varied greatly. Salidroside, Tetroside and Vasoflavin were rapidly dissolved in each medium (> 85%), whereas luteolin and oleanolic acid in Mifei Pill only eluted very little amount (<30%) in p H 6.8 phosphate buffer. From the difference factor and similarity factor analysis, the dissolution profiles of the same components in the two preparations showed no similarity. CONCLUSION: The cumulative dissolution of the active ingredient in the formula granule is higher than that of the water honey pill and more of the active ingredient elutes in the same dissolution medium. This shows that in vitro dissolution, formula particles of this new form of traditional Chinese medicine has a greater advantage. The established dissolution method can be applied to the quality control of Erzhi Pills.