Optimization and characterization of nimesulide bilayer tablets by response surface methodology  

效应面法优化尼美舒利双层缓释片处方(英文)

作　　者：单利[1] 范云周[2] 王玉丽[1] 陈红鸽[1,3] 高春生[1] 杨美燕[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850 [2]北京大学医学部药学院,北京100191 [3]解放军302医院,北京100039

出　　处：《Journal of Chinese Pharmaceutical Sciences》2014年第2期89-93,共5页中国药学（英文版）

基　　金：Important National Science & Technology Specific Projects of China(Grant No.2012ZX09301003-001-009)

摘　　要：The objectives of this present investigation were to develop and formulate nimesulide bilayer tablets by using different polymer combinations and fillers, to optimize the formulations for different drug release variables by orthogonal design and central composite design-surface methodology and to evaluate drug release pattern of the optimized product. The bilayer tablet containing a fast release layer（FRL） and a sustained release layer（SRL） provided an initial burst release of nimesulide, followed by the sustained release for a period of time. The optimal formulation obtained was as follows：（I） the formulation of FRL： nimesulide, 50 mg; lactose, 92 mg; starch, 22 mg; CCMC-Na, 14 mg; PVP K30, 1 mg; micronized silica gel, 1 mg; magnesium stearate, 0.9 mg; and iron oxide red, 0.1 mg; and（II） the formulation of SRL： nimesulide, 150 mg; HPMC K100LV, 26 mg; HPMC K4M, 33 mg; lactose, 54 mg; PVP K30, 1 mg; micronized silica gel, 1 mg; and magnesium stearate, 0.9 mg. According to the optimal formulation, the biphasic type of release was identified. The in vitro drug dissolution from the bilayer tablets was sustained for about 16 h after releasing 15% of drug in the first 10 min. The developed nimesulide bilayer tablets with improved efficacy can perform therapeutically better than the conventional tablets.采用正交设计及星点设计-效应面法对尼美舒利双层缓释片处方进行优化。优化后的处方如下:(I)速释层:尼美舒利,50 mg;乳糖,92 mg;淀粉,22 mg;CCMC-Na,14 mg;PVP K30,1 mg;微粉硅胶,1 mg;硬脂酸镁,0.9 mg;氧化铁红,0.1 mg;(II)缓释层:尼美舒利,150 mg;HPMC K100LV,26 mg;HPMC K4M,33 mg;乳糖,54 mg;PVP K30,1 mg;微粉硅胶,1 mg;硬脂酸镁,0.9 mg。优化后的处方在初期药物快速释放(10 min释放15%),后期缓慢释放持续一段时间(16 h),具有双相释放特征,且放置6个月后无明显变化。

关 键 词：NIMESULIDE Bilayer tablets Orthogonal design Central composite design-response surface methodology Sustainedrelease Fast release 

分 类 号：R944[医药卫生—药剂学]