西格列汀二甲双胍片的制备及其体外溶出度评价

摘要

目的:研究西格列汀二甲双胍片的最优处方,以期得到与原研捷诺达@相似的溶出曲线.方法:以溶出度、外观、硬度和偏重差异为考察指标,通过单因素实验,筛选出最优处方,比较自制制剂和参比制剂在4种介质中的溶出曲线.结果:选用MCC为稀释剂,PVP K30为黏合剂,SDS为增溶剂,硬脂富马酸钠为乳化剂.MCC采用外加的方法,PVP K30为27 mg.片-1,SDS为14 mg.片-1,硬脂富马酸钠为7 mg·片-1.15 min之内,自制制剂和参比制剂在4种溶出介质中的溶出度均大于85％,两者的溶出曲线相似.结论:西格列汀二甲双胍片的制备方法简单可行,满足大生产的需要.%Objective:To optimize the formulation of sitagliptin phosphate/metformin hydrochloride tablets to obtain similar dissolution profiles with RLD (reference listed drug,JANUMAT(R)).Methods:The formulation of sitagliptin phosphate/metformin hydrochloride tablets was optimized in terms of dissolution,appearance,hardness and tablet weight difference by single factor test,and the dissolution profiles were compared with RLD in four kind of dissolution media.Results:MCC,PVP K30,SDS and sodium stearyl fumarate were selected as diluent,adhesive,solubilizer and lubricant,respectively.MCC was added after granulation and the amounts of PVP K30,SDS and sodium stearyl fumarate in one tablet were 35 mg,7 mg and 3.5 mg,respectively.The dissolution was above 85％ for both self-prepared preparations and RLD in 15 min,and the dissolution profiles were similar.Conclusion:The method of preparing sitagliptin phosphate/metformin hydrochloride tablets is simple and can meet the requirements of large-scale production.