苯甲酸阿格列汀片处方工艺的研究及其溶出度评价

摘要

为了筛选出苯甲酸阿格列汀片的处方工艺,采用L34)正交表进行设计,对处方中甘露醇与微晶(9纤维素量的比例、质量分数3%羟丙基甲基纤维素水溶液的用量、交联羧甲基纤维素钠的用量以及其内加外加的比例进行优化及筛选,检测该处方工艺下所制片剂的脆碎度、硬度、溶出度和主药含量,比较自制片剂与原研片剂在进口标准条件下所测溶出曲线的相似性.研究结果表明:确定处方工艺为苯甲酸阿格列汀34 g、甘露醇50 g、微晶纤维素50 g、质量分数3%羟丙基甲基纤维素水溶液62 g、交联羧甲基纤维素内加20 g外加10 g、硬脂酸镁1.6 g(制备1000片).按该工艺制得苯甲酸阿格列汀片的脆碎度为0.17%~0.21%、硬度为9.9 kgf~10.3 kgf、崩解时间为230 s~240 s、主药质量分数为99.9%.在按进口标准要求测量下,自制片剂与原研片剂溶出曲线的相似因子(f2)均大—80.所以,由本研究可知自制片剂与原研片剂体外溶出行为相似,处方合理.%To screen the optimal prescription formulation process of the alogliptin benzoate tablets,the ratio of mannitol to microcrystalline cellulose,the amount of 3% HPMC solution,the amount of croscarmellose sodium and its ratio of inside addition to outside addition were optimized with the L9(34)orthogonal test.The friability, hardness,dissolution rate and main component of these self-prepared alogliptin benzoate tablets were also detected. And the dissolution curves of the self-prepared tablets were compared with those of the commercial tablets under the import standard. The optimized formulation of alogliptin benzoate tablet(1 000 pieces)was found to be comprised of 34 g of alogliptin benzoate,50 g of mannitol,50 g of microcrystalline cellulose,62 g of 3% HPMC solution,20 g of microcrystalline cellulose inner-added,10 g of microcrystalline cellulose external-added,1.6 g of magnesium stearate.The friability,hardness,disintegration time and main component of three batches of alogliptin benzoate tablets prepared by optimized prescription were 0.17%-0.21%, 9.9 kgf-10.3 kgf,230 s-240 s and 99.9%,respectively. Similar factors f2of dissolution curves for prepared tables and commercial tablets were above 80 under the import standard. The dissolution behavior of prepared tablets is similar to that of commercial tables.The optimized formulation is rational.