壬苯醇醚阴道用缓释凝胶的研制

目的制备壬苯醇醚阴道用缓释凝胶并优化其处方与工艺。方法采用正交试验设计 ,考察了聚卡波菲用量、卡波沫用量、pH值、甘油用量、液体石蜡用量、山嵛酸甘油酯用量及不同工艺对释放度的影响 ,与国外产品进行残差平方和、拟合度、区分因子和相似因子比较 ,确定壬苯醇醚阴道用缓释凝胶的处方工艺 ,并考察了其初步稳定性。结果优化所得处方工艺为 :聚卡波菲用量0 5 % (w) ,卡波沫用量 1% (w) ,甘油用量为 5 % (w) ,液体石蜡用量为 5 % (w) ,山嵛酸甘油酯用量为 1% (w) ,pH值为 4 5 ,选用工艺 1。 结论按优化处方工艺制得的壬苯醇醚阴道用缓释凝胶稳定 ,与国外产品比较具有相似的释放度 ,且以复合模式释放。

Preparation and in vitro drug release characterization of nonoxynol-9 sustained-release gel for vagina

Objective To optimize the preparation and formulation of nonoxynol-9 suatained-release gel for vagina.Method The orthogonal design was used to screen the preparation and formulation of nonoxynol-9 sustained-release gel for vagina which took SUM,r2,difference factor and similarity factor compared with a similar product as index on the base of the influence of pH,preparation and the amount of Polycarbophil,Carbopol,glycerol,liquid paraffin and Compritol 888 ATO on drug release.Result The optimal combination of preparation and formulation is 0.5%(w) polycarbophil,1.0%(w) carbopol,5%(w) glycerol,10%(w) liquid paraffin and 1%(w) Compritol 888 ATO,pH 4.5 and preparation method 1.Conclusions The optimized preparation and formulation of nonoxynol-9 sustained-release gel for vagina has the properties of preliminarily steady and similar release with a foreign product.