国内外交联羧甲纤维素钠结构及功能性指标的质量研究

Quality Study on the Structure and Functionality-related Characteristics of CCS from Home and Abroad

考察国内外不同来源的交联羧甲纤维素钠(CCS)在结构及功能性指标上的差异,并对其吸湿行为进行表征,建立正交偏最小二乘(OPLS)模型分析CCS的质量对多潘立酮片崩解时间及溶出度的影响。结果表明,不同来源CCS的取代度、交联密度、粒子形态、粒径、膨胀度、沉降体积、粉体流动性和水吸收速率均存在差异,且粒子形态及粒径会影响流动性的大小,碱性取代基的比例会对吸水性能产生影响。不同来源CCS的膨胀度、沉降体积、酸性取代度、碱性取代度、颗粒间孔隙率、交联密度、d(0.5)和水分对多潘立酮片的崩解时间和溶出度有较大影响。因此,对不同来源CCS的结构及功能性指标进行分析将有助于为制剂处方选择适宜的辅料提供一定的依据。

The differences in structure and functionality-related characteristics of croscarmellose sodium(CCS)from different sources at home and abroad were investigated,and their moisture absorption behaviors were characterized.Then,the orthogonal partial least squares(OPLS)model was established to analyze the impacts of the quality of CCS on the disintegration time and dissolution of domperidone tablets.The results showed that the degree of substitution,crosslink density,particle morphology,particle size,swelling,settling volume,powder fluidity and water uptake rate of CCS from different sources were different.The particle morphology and particle size would affect the powder fluidity.The proportion of basic substituents would affect the water absorption of CCS.Swelling,settling volume,degree of acidic substitutions,degree of basic substitutions,inter-particle porosity,crosslink density,d(0.5)and moisture content of CCS from different sources had a large effect on the disintegration time and dissolution of domperidone tablets.Therefore,the analysis of structural and functionality-related characteristics of CCS from different sources will help to provide a basis on selecting the appropriate excipients for formulation design.