复方缬沙坦/苯磺酸氨氯地平片的制备和体外溶出测定

目的:研制与上市品具有相似体外溶出的复方缬沙坦/苯磺酸氨氯地平片。方法:采用湿法制粒压片工艺制备自制品,通过单因素试验初步筛选处方,中心复合设计优化处方。比较不同pH溶出介质(pH 1.2盐酸、pH 4.5乙酸缓冲液和0.1%聚山梨酯80-pH 6.8磷酸缓冲液)中自制品与市售复方片的溶出行为,通过相似因子f2计算,评价2种药物体外溶出的相似性。结果:与市售片比较,以优化处方制备的复方片中缬沙坦和苯磺酸氨氯地平在不同pH值溶出介质中的溶出度相似因子f 2均>50。结论:自制的复方片与市售片体外溶出行为相似。

Preparation and dissolution of compound valsartan and amlodipine besylate tablets

Objective: To prepare compound valsartan and amlodipine besylate tablets with similar dissolution to marketed products.Methods: The compound tablets were prepared with wet granulation followed by compression.The formulations were screened by the single factor test,and then optimized through the center composite design.By evaluating the dissolution behavior in different dissolution media hydrochloric acid(pH 1.2),acetic acid buffer solution(pH 4.5),phosphate buffer solution(pH 6.8) containing 0.1% Tween 80],the similarity between marketed products and test tablets was evaluated by similarity factors(f 2).Results: All the dissolution similarity factors(f 2) of amlodipine besylate and valsartan were larger than 50 between the optimized compound tablet and marketed products in different dissolution media.Conclusion: The dissolution characteristics of self-made tablets are similar with that of marketed products in vitro.