格列喹酮缓释片的处方设计

Formulation Design of Gliquidone Sustained-release Tablets

目的:对格列喹酮缓释片进行处方研究。方法:以药物的累积释放度为标准,同时结合相似因子,首先进行单因素试验,确定影响药物释放的主要因素,在此基础上,以HPMC(K4M)及乳糖的含量为变量,进行比较试验,采用综合评分法确定最优处方。并且对最优处方进行验证。结果:最优处方为格列喹酮、HPMC(K4M)、乳糖用量分别为60mg、30mg、55mg,70%乙醇为粘合剂,所制得的格列喹酮缓释片在2,6,12h的体外累积释放度分别为(19.82±0.92)%,(51.07±0.95)%和(83.48±0.71)%。结论:格列喹酮缓释片体外显示出缓释行为,释放度符合规定,可进一步研究开发。

Objective： To optimize the formulation of gliquidone sustained-release tablets. Method： Combined with similarity factor, the single factor testing was made to determine the controlling factors with the accumulation percent of drug release as criteria. On the basis of the testing, comparative method was used to optimize pharmaceutical formulation by grading methods with HPMC （K4M） and lactose as variables. Result： the optimum formulation was as follows： the amounts of gliquidone,HPMC,lactose were 60mg,30mg, 55mg respectivly and 70% Alcohol was adhesive. The in vitro release rates at 2,6,12h were （ 19.82 ±0.92）% ,（51.07 ＋0.95）% , （83.48 ±0.71 ）%, respectively. Conclusion： Gliquidone sustained-release tablets present sustained release behaviors in vitro and the in vitro accumulated drug release is in conformity with the requirements. It is worth further research.