复方阿魏酸钠/天麻素缓速释双层片的处方优化

Preparation of Compound Sodium Ferulate-gastrodin Quick-release Double-layer Tablets

目的:优化复方阿魏酸钠/天麻素缓速释双层片的处方。方法:以累积释放度为指标,以填充剂用量、崩解剂用量和片剂硬度为考察因素,采用正交试验优化速释层处方;以阿魏酸和天麻素在1、4、8、12h的累积释放度为指标,以羟丙基甲基纤维素(HPMC K15M)和羧甲基纤维素钠(CMC-Na)的用量为考察因素,采用星点设计-效应面法优化缓释层处方。结果:速释层处方为填充剂40mg(微晶纤维素∶预胶化淀粉=1∶1,m/m),崩解剂(交联聚维酮)10mg,阿魏酸钠25mg,天麻素25mg,硬脂酸镁1mg,压片硬度为5kg/cm2;缓释层处方为阿魏酸钠50mg,天麻素50mg,HPMC K15M 47mg,CMC-Na13.8mg,微晶纤维素38.2mg,微粉硅胶1mg,硬脂酸镁1mg。结论:所选处方合理、可行,可制备出合格的复方阿魏酸钠/天麻素缓速释双层片。

OBJECTIVE： To optimize Compound sodium ferulate/gastrodin quick-release double-layer tablets. METHODS： The formulation of quick-release layer was optimized by orthogonal design with accumulatire release rate as index using the amount and solidity of filler and disintegrating agent as factors; the formulation of sustained-release layer was optimized by central composite design-response surface methodology with accumulative release rate of ferulaic acid and gastrodin within 1, 4, 8 and 12 h as index using the amounts of HPMC K15M and CMC-Na as factors. RESULTS： The formulation of quick-release layer was as follows： fill-er 40 mg as （MCC： pregelatinized starch=1： 1,m/m）, PVPP 10 mg as disintegrating agent, sodium ferulate 25 mg, gastrodin 25 mg, magnesium stearate 1 mg; solidity of tabletting 5 kg/cm^2; that of sustained-release layer was as follows： Sodium ferulate 50 mg, gastrodin 50 mg, HPMC K15M 47 mg, CMC-Na 13.8 mg, MCC 38.2 mg, silica gel 1 mg, magnesium stearate 1 mg. CON-CLUSIONS：Optimized formulation is reasonable and feasible, and Compound sodium femlate/gastrodin quick-release double-layer tablets can be prepared.