生血宝的液-固制剂质量属性传递规律分析

Anlysis on Quality Attribute Transfer Law of Liquid-solid Preparation of Shengxuebao

目的:以生血宝为模型中药,探索中药复方制剂从液体到固体剂型的成分变化研究方法与传递规律。方法:基于前期所建立的生血宝超高效液相色谱法(UPLC)定性、定量方法,建立生血宝自制汤剂、市售颗粒剂与合剂3种制剂的指纹图谱,并对其中19种成分进行定量分析;分别采用“中药色谱指纹图谱相似度评价系统”(2012版)与总量统计矩相似度法评价3种制剂的指纹图谱相似度;计算3种制剂化学成分分子连接性指数(MCI)及平均摩尔MCI,计算各成分0~8阶、8亚类共计72个MCI值,选用0~3阶平均摩尔MCI研究其中药成分群“印迹模板”结构特征及传递规律。结果:汤剂指纹图谱与对照指纹图谱、颗粒剂和合剂指纹图谱的相似度分别为0.971、0.888和0.799,表明颗粒剂和合剂2种剂型的化学组成与汤剂存在差异,且19种成分能够基本反应生血宝汤剂成分群整体情况;测得生血宝汤剂、颗粒剂与合剂3种制剂中可检出主要成分的质量分数总和分别5.4986、2.2820、1.4166 mg·g^(-1);3种制剂0~3阶的平均摩尔MCI整体上逐渐减小,且在同一类别的平均摩尔MCI里3种制剂也呈汤剂>颗粒剂>合剂的递减趋势,表明3种制剂所得样品化学成分的整体结构特征发生了细微变化。结论:生血宝3种制剂中传统汤剂中所含成分种类及含量最高、所携带成分信息量最大,颗粒剂与合剂依次递减。该研究进一步印证了传统汤剂是基础可靠的剂型,为中药现代剂型改革与复方制剂的质量一致性评价提供参考。

Objective:Taking Shengxuebao as the model traditional Chinese medicine(TCM),this study aims to explore the methodologies and transfer patterns in the composition changes of TCM compound preparations from liquid to solid dosage forms.Method:Based on the previously established ultra-high performance liquid chromatography(UPLC)qualitative and quantitative methods for Shengxuebao,the fingerprint profiles of three preparations of Shengxuebao(homemade decoction,commercially available granules and mixtures)were established,and nineteen components were quantitatively analyzed.The similarities of fingerprint profiles among these three preparations were assessed using the Similarity Evaluation System for Chromatographic Fingerprint of TCM(2012 edition)and the total quantum statistical moment similarity method,respectively.The molecular connectivity index(MCI)and the average molar MCI of the chemical components in the three preparations were calculated.Seventy-two MCI values across 0-8 orders,including 8 subclasses,were calculated.The average molar MCI of 0-3 orders was used to study the"imprint template"structural characteristics and transfer patterns of the medicinal component groups.Result:The similarities of the fingerprint profile of the decoction with those of the control,granules,and mixtures were 0.971,0.888 and 0.799,respectively,indicating that the chemical composition of the granules and mixtures differed from that of the decoction,and that the 19 components were able to basically respond to the overall situation of the component group of Shengxuebao decoction.The total mass fractions of the detectable major components in Shengxuebao decoction,granules and mixtures was measured to be 5.4986,2.2820,1.4166 mg·g^(-1),respectively.The average molar MCI of 0-3 orders showed a gradual decrease across the three preparations,with the trend of decoction>granules>mixtures,indicating subtle changes in the overall structural characteristics of the chemical components in the samples of the three preparations.Conclusion:Among the three formulations of Shengxuebao,the traditional decoction contained the highest variety and quantity of components and carried the most substantial amount of component information,with a decreasing order observed in the granules and mixtures.This study further validates that traditional decoction is a reliable and fundamental dosage form,providing a reference for the modernization of TCM dosage forms and the quality consistency evaluation of compound preparations.