尼美舒利亲水凝胶骨架片的研制

Study and preparation of hydrophilic gel matrix tablet of nimesulide

目的优化尼美舒利亲水凝胶骨架片的制备方法,并进行体外释放研究。方法采用正交试验设计,以体外累积释药百分率为指标,以羟丙基甲基纤维素(HPMC)K100-LV CR、乳糖、50 g.L-1聚乙烯比咯烷酮(PVP)的处方用量作为影响因素筛选缓释片的最佳处方,并测定3批优化处方的体外释放度。结果优化处方为HPMC K100-LV CR 100 mg,乳糖50 mg,50 g.L-1PVP 3 mL;尼美舒利亲水凝胶骨架片在12 h释放量达97%以上,无时滞、突释等现象;其体外释药动力学符合零级方程。结论尼美舒利亲水凝胶骨架片处方合理,制备工艺可靠,体外释药效果良好。

Objective To optimize the preparative method of nimesulide hydrophilic gel matrix tablet,and to perform the release study in vitro.Methods The optimal formulation of nimesulide hydrophilic gel matrix tablet was obtained by orthogonal design,with the rate of drug accumulative release in vitro as index,and the amount of hydroxypropyl methyl cellucose（HPMC,K100-LV CR）,lactose and 50 g·L^-1 polyvinylpyrrolidone（PVP） were choosed as three influential factors.Results The orthogonal design results as flows：HPMC K100-LV CR 100 mg,lactose 50 mg,50 g·L^-1 PVP 3 mL.The rate of drug accumulative release in vitro was more than 97% within 12 h,and there was no time-lag and sudden release phenomenon.The drug release in vitro could be well fitted with the zero-order equation.Conclusion The formulation and the technics are feasible and steady-going,the hydrophilic gel matrix tablets prepared show well effect in vitro.