碳酸司维拉姆片原料粒度对产品质量的影响研究

Study on the Effect of Raw Material Particle Size of Sevelamer Carbonate Tablets on Product Quality

目的研究碳酸司维拉姆片原料粒度对产品质量的影响。方法于2019年6月—2020年11月展开该实验研究;采用不同粒度碳酸司维拉姆原料进行实验研究,对混合效果、压片可压性、崩解时间、崩解延迟、体外磷结合效果进行研究,考察碳酸司维拉姆片不同粒度原料对产品质量的影响。结果采用D90为41.5、62.4、81.6、101.6μm的原料药与辅料混合,混合效果良好。使用旋转压片机压片,可以轻松压制到适当硬度,可压性良好。试验显示碳酸司维拉姆原料粒径越小,碳酸司维拉姆片的崩解时间越长,影响因素放置一定时间后崩解延迟越显著。原料体外磷结合试验显示,随着原料粒度变小,碳酸司维拉姆的磷结合力提高,磷酸盐去除速率较快。结论原料粒度对碳酸司维拉姆片崩解时间和磷结合能力存在一定程度的影响,合理控制原料药粒径可确保仿制制剂与参比制剂溶出一致,达到磷结合的理想效果。

Objective To study the effect of raw material particle size of sevelamer carbonate tablets on product quality.Methods The research work was carried out in June 2019,and the experimental study was completed in November 2020;the experimental research was carried out with different particle size sevelamer carbonate raw materials,and the mixing effect,compressibility,disintegration time,and disintegration delay,in vitro phosphorus binding effect to study the effect of different particle size raw materials of sevelamer carbonate tablets on product quality.Results The raw materials with D90 of 41.5μm,62.4μm,81.6μm,101.6μm were mixed with excipients,and the mixing effect was good.Using a rotary tablet press to compress tablets,it can be easily compressed to an appropriate hardness with good compressibility.Tests have shown that the smaller the particle size of the sevelamer carbonate raw material,the longer the disintegration time of the sevelamer carbonate tablet,and the more significant the disintegration delay after the influencing factors are placed for a certain period of time.The in vitro phosphorus binding test of the raw material showed that as the particle size of the raw material becomes smaller,the phosphorus binding force of sevelamer carbonate increases,and the phosphate removal rate was faster.Conclusion The particle size of the raw material has a certain degree of influence on the disintegration time and phosphorus binding capacity of sevelamer carbonate tablets.A reasonable control of the particle size of the raw material drug can ensure that the dissolution of the imitation preparation and the reference preparation are consistent,and achieve the desired effect of phosphorus binding.