Study On The Correlation Between The Quality Of Medicinal MCC And The Application Performance Of Its Tablet

Microcrystalline Cellulose(MCC)has the quality of good flowability,formability,disintegrative,non-toxicity,harmlessness,good biocompatibility,and does not react with other ingredients in drug.Therefore,it is currently one of the most widely used pharmaceutical excipients in the pharmaceutical industry,and is widely used in the pharmaceutical field as fillers,disintegrants,diluents,and adhesives.However,due to the late start of MCC industry in China,the current domestic MCC production can only have certain safety instruction according to the Pharmacopoeia,but don't have specific application instruction.And because of the unclear demand for MCC selection,it is impossible to provide drug performance references for MCC production.As a result,the production and application of MCC are disconnected,which has become one of the important factors restricting the improvement of MCC industry in China.Therefore,this subject explored the quantitative relationship between the quality of MCC and the application performance of its tablet from different perspectives.During the process,the quality of MCC was characterized by quality indicator(particle size,crystallinity,comprehensive characteristics of powders)and particle morphology.The application properties of tablet mainly include hardness,disintegration and dissolution.The specific research content is as follows:Firstly,by comparing the quality of MCCs prepared under different acid concentration and the application performance of the tablets,the MCC made at 4.5 mol/L acid concentration was selected as a sample.Then it was compared with other domestic and imported MCC samples,the differences between the quality of MCC and the application performances of tablet were investigated.The results showed that there was not much difference between the quality of the same model of MCC and the application performance of the tablet,while the quality of different models of MCC and the application performances of tablets were greatly different.That is,the quality of the MCC will affect the performances of the tablet.Secondly,different models of MCC with different quality and application performance were used as samples.Multivariate stepwise regression analysis was used to study the correlation between the quality indicator of MCC and the application performance of tablet.The results showed that a significant linear regression equation was established between crystallinity and hardness.The equation showed that the greater the crystallinity of MCC particles,the greater the hardness of the tablet,but there was no significant functional relationship between particle size and tablet hardness.Besides,the particle size and crystallinity have a certain effect on the disintegration and dissolution of tablets,but there is no multivariate function relationship.In addition,the linear regression equation can be established between the comprehensive properties of each model of MCC and application performances of tablets.The order of importance of the comprehensive properties of the powders to the application performances was as follows:compression degree>angle of repose>bulk density=swelling ratio.Finally,two models of MCC with large differences in morphology were selected as samples,and the fractal dimension and shape factors of them were used to characterize morphology of MCC s.The functional relationship between morphology of the MCCs and application performance of tablets were established.Furthermore,the effect of particle morphology on tablet disintegration behavior was explored.The results showed that the circularity was the most important shape factor after the analysis of the MCC shape factors by box plot.Moreover,the fractal dimensions and circularity of the two models of MCC were established functional relationships with hardness,disintegration,and dissolution of tablet,respectively.The functional relationships showed that the larger the fractal dimension of the MCC,the rougher the morphology of the particles,resulting in a longer disintegration time and less dissolution of the tablet.In addition,the functional relationship between circularity and application performance indicated that the greater the circularity of MCC can result in a shorter disintegration time and greater dissolution of the tablet.The preliminary exploration result of the morphology of MCCs on the disintegration behavior of tablets showed that the disintegration forms of tablets made by two models of MCC belong to the "laminating type ".For the same model of MCC,when the circularity was smaller and the fractal dimension was larger,the produced tablet had the larger diameter growth rate and smaller thickness growth rate after swelling.In summary,this paper established a certain quantitative correlation between the quality of MCC and the application performance of tablet.For the first time,a preliminary quantitative relationship was established between the particle morphology and the application performance of tablet by quantify the tablet morphology.The research on the correlation between the quality of MCC and the application performance of tablet can provide important references for the preparation of MCC,the evaluation of products and the selection of MCC by pharmaceutical companies.Moreover,it has a positive significance for the quality improvement of MCC and pharmaceutical tablet.