缬沙坦片的制备工艺及质量一致性评价研究

Preparation of Valsartan Tablets and evaluation of quality consistency

目的开发缬沙坦仿制片,并对其进行体外质量一致性评价。方法以缬沙坦原研制剂(80 mg)为对照药品,单因素实验考察影响缬沙坦溶出度的处方因素及制备工艺参数,从而确定最佳处方和制备工艺,并测定自制片和原研药在4种溶出介质的溶出过程,采用相似因子(f_2)法对两者的溶解曲线进行相似性评价。结果 3批缬沙坦仿制药在磷酸盐缓冲液(pH6.8)中15 min内溶出85%,在水、pH1.2盐酸溶液、pH4.5醋酸盐溶液中的f_2均大于50。结论以溶出度为主要考察指标,通过单因素实验开发的缬沙坦片仿制药与原研药体外溶出具有一致性,质量符合要求。

Objective To develop a formulation of generic Valsartan Tablets and evaluate the quality consistency in vitro.Methods Diovan（R）~ HCT （80 mg） was used as the reference drug.In order to determine the best formulation and the best preparation processing,the single factor experiments were applied to determining the best formulation and the best preparation processing.And dissolution test was used as the evaluation index in the single factor experiments.Meanwhile the dissolubility of generic Valsartan Tablets and original preparation was investigated in four different media to evaluate the similarity of dissolution by calculating similar factor （f2）.Results The dissolution was above 85% of three batches of generic Valsartan Tablets in the phosphate buffer （pH 6.8）.The similar factors were all more than 50 in the water,hydrochloric acid solution （pH 1.2）,and acetate buffer solution （pH 4.5）.Conclusion The f2 similarity factor results indicate a similarity in the reference drug and generic Valsartan Tablets which were developed by single factor experiments,which means the quality of genetic Valsartan Tablets is qualified.