羧甲淀粉钠工艺对片剂崩解性能的影响

Effect of Sodium Starch Glycolate Process on Tablet Disintegration Performance

目的:采用一种经交联工艺的羧甲淀粉钠作为崩解剂,改善难溶性药物的片剂在高湿条件下崩解不佳的现象。方法:以难溶性药物瑞卢戈利和培唑帕尼为模型药物,采用湿法制粒工艺制备瑞卢戈利片和培唑帕尼片,以羧甲淀粉钠的膨胀体积、溶胀后显微照片、片剂高湿条件下的崩解时间、溶出度及崩解照片为评价指标,评价不同工艺的羧甲淀粉钠对片剂在高湿条件下崩解性能的影响。结果:羧甲淀粉钠是否交联对片剂0天的崩解性能无显著影响,但使用无交联工艺的羧甲淀粉钠的片剂在高湿条件(92.5%RH)出现崩解不佳或不崩解现象,使用经交联工艺的羧甲淀粉钠的片剂在高湿条件(92.5%RH)下崩解良好。结论:经交联化的羧甲淀粉钠空间结构更强,在高湿条件下的凝胶化反应较弱,吸湿溶胀后仍有一定的空间间隙供水分进入片芯,可使难溶性药物在高湿条件下保持良好的崩解性能。

Objective:To use a cross-linked sodium starch glycolate as a disintegrant to improve the poor disintegration of poorly soluble tablets under high humidity conditions.Methods:Using insoluble drugs reslugolix and pazopanib as model drugs,relugolix tablets and pazopanib tablets were prepared by wet granulation process.The swelling volume and swelling micrographs of sodium starch glycolate,the disintegration time,dissolution rate and disintegration photos of tablets under high humidity conditions were used as evaluation indicators to evaluate the influence of sodium starch glycolate with different processes on the disintegration performance of tablets under high humidity conditions.Results:Whether the sodium starch glycolate was cross-linked or not had no significant effect on the disintegration performance of the tablet at 0 days,but the tablet using the sodium starch glycolate without cross-linking process had poor disintegration or no disintegration phenomenon under high humidity conditions(92.5%RH).The tablet using the cross-linked sodium starch glycolate disintegrates well under high humidity conditions(92.5%RH).Conclusion:The cross-linked sodium starch glycolate has stronger spatial structure and weaker gelation reaction under high humidity conditions.After moisture absorption and swelling,there is still a certain space gap for water to enter the tablet core,which can make insoluble drugs in the tablet core,maintains good disintegration properties under high humidity conditions.