以泻白散为例探讨经典名方复方制剂开发中粳米对汤剂理化性质的影响

Discussion on the Influence of Japonica Rice on the Physicochemical Properties of Famous Classical Formulas Compound Preparation with Xiebai San for Example

目的以泻白散为例,比较加减粳米所得汤剂的理化性质的异同点,为古代经典名方复方制剂开发中粳米的取舍提供依据。方法表征粳米对汤剂化学性质的影响:(1)测定泻白散和粳米阴性汤剂中主要化学成分含量;(2)比较二者的指纹图谱;(3)测定并比较二者主要活性成分的热稳定性。表征粳米对汤剂物理性质的影响:(1)测定汤剂的干膏率;(2)测定汤剂胶体的粒径、电位及电导率;(3)检查汤剂冻干粉的溶化性,以预测服用时粳米对制剂物理性质的影响。结果化学性质方面:泻白散汤剂中各主要化学成分含量显著低于粳米阴性汤剂;二者的液相色谱指纹图谱相似度高;泻白散汤剂共有峰面积均小于粳米阴性汤剂;加热导致泻白散汤剂中地骨皮乙素含量显著降低,而粳米对该成分的热稳定性无显著影响。物理性质方面:粳米阴性汤剂胶体粒径略小于较泻白散样品,二者电位、电导率无显著差异;泻白散干膏率显著高于粳米阴性汤剂;粳米阴性样品冻干粉溶化性较泻白散样品冻干粉更好,沉淀及不溶性杂质少。结论泻白散中粳米降低了活性成分的溶出,对汤剂加热过程中主要活性成分的热稳定性没有影响,增加了泻白散样品冻干粉复溶后不溶物的含量,建议古代经典名方复方制剂研制时可以去除粳米。

Objective This paper will take Xiebai San as an example to compare the similarities and differences of the physical and chemical properties of the decoction obtained by adding or reducing japonica rice,so as to provide a basis for the selection of japonica rice in the development of the ancient famous classical formulas prescription compound preparation.Methods Characterization of the effect of japonica rice on the chemical properties of the decoction:1.Determination of the contents of the main chemical components in Xiebai San and japonica rice negative decoction by the established ultra performance liquid chromatography(UPLC)method;2.The fingerprint profiles of the two were analyzed for similarity;3.Determine and compare the thermal stability of the main active ingredients of the two according to the established content determination method.Characterization of the effect of japonica rice on the physical properties of the decoction:1.Measuring the dry paste rate of decoction;2.The particle size,zeta potential and conductivity of colloidal phase were determined by laser particle size analyzer;3.Testing the solubility of the decoction lyophilized powder,in order to predict the effect of japonica on the physical properties of the preparation when taking medicine.Results Chemical Properties:The content of main chemical components of Xiebai San decoction was significantly lower than that of japonica rice negative decoction;the UPLC fingerprints of the two were highly similar;and the common peak area of Xiebai San decoction was smaller than that of japonica rice negative decoction;Heating results in a significant decrease in the content of kukoamine B in Xiebai San decoction,while japonica rice has no significant effect on its thermal stability.Physical Properties:The colloidal particle size of japonica rice negative decoction was slightly smaller than that of Xiebai San,and there was no significant difference in zeta potential and conductivity between them;The dry paste rate of Xiebai San was significantly higher than that of japonica rice negative decoction;and the lyophilized powder japonica rice negative sample had better solubility than that of the lyophilized powder of the Xiebai San powder sample,with less precipitation and insoluble impurities.Conclusion The japonica rice in Xiebai San reduced the dissolution of the main active ingredients,which had no effect on the thermal stability of the main active ingredients during the heating process of the decoction,and increased the content of insoluble matter in lyophilized powder of Xiebai San.It was suggested that the japonica rice could be removed during the development of famous classic formulas prescription compound,“japonica rice water to be taken”should be marked in the drug instructions.