关键词: 尼美舒利, 双层片, 正交设计, 星点设计-效应面法, 缓释, 速释

Abstract:

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.

Key words: Nimesulide, Bilayer tablets, Orthogonal design, Central composite design-response surface methodology, Sustained release, Fast release