尼美舒利巴布剂基质处方的优选

目的对尼美舒利巴布剂的基质处方进行优化。方法采用正交试验,以卡波姆及聚丙烯酸钠为骨架材料,聚乙烯吡咯烷酮K30及羧甲基纤维素钠为增黏剂,聚乙烯醇为成膜剂,以内聚力、剥离强度为评价指标优选尼美舒利巴布剂的基质处方,并对制剂体外释药特性进行考察。结果基质中各成分对内聚力的作用大小依次为卡波姆>羧甲基纤维素钠>聚乙烯醇,对剥离强度的作用大小依次为卡波姆>聚乙烯吡咯烷酮K30>聚丙烯酸钠,优选得到最优配方为卡波姆∶聚丙烯酸钠∶聚乙烯吡咯烷酮K30∶羧甲基纤维素钠∶聚乙烯醇=3.0∶4.0∶0.5∶0.2∶0.5(质量比)。巴布剂的体外释药特性与凝胶剂相似,但释药速度更快(P<0.05)。结论通过优化处方配比,可制得黏附性能良好的尼美舒利巴布剂。

Optimization of the matrix formulation of nimesulide cataplasms

Objective To optimize the matrix formulation of nimesulide cataplasms.Methods The matrix of nimesulide cataplasms was optimized by orthogonal design with carbomer and sodium polyacrylate as the matrix,PVP K30 and CMC-Na as the viscosity-increasing agents,PVA as the film material and cohesive strength and adhesion strength as the evaluation indices.The transdermal penetration in vitro was studied as well.Results The order of cohesive strength effect was carbomer>CMC-Na>PVA while the order of adhesion strength effect was carbomer> PVP K30 > sodium polyacrylate.The matrix formulation of nimesulide cataplasms was made with carbomer∶sodium polyacrylate∶PVP K30∶CMC-Na∶PVA of 3.0∶4.0∶0.5∶0.2∶0.5.The drug release in vitro of the cataplasms was similar with that of the gels with the quicker rate(P<0.05).Conclusion Nimesulide cataplasms with good viscoelasticity can be prepared by the optimal matrix formulation.