星点设计-响应面法优化盐酸罗沙替丁醋酸酯缓释片的处方  

Optimization of the Formulation of Roxatidine Acetate Hydrochloride Sustained-release Tablets by Central Composite Design-response Surface Methodology

作　　者：段颐珊 杜娟 孙璐 李雪怡 林宁 DUAN Yishan;DU Juan;SUN Lu;LI Xueyi;LIN Ning(School of Pharmacy,Hubei University of TCM,Wuhan 430065,China)

机构地区：[1]湖北中医药大学药学院,武汉430065

出　　处：《中国药房》2018年第7期927-929,共3页China Pharmacy

基　　金：湖北省科技计划项目(No.2012FFB03705);湖北省教育厅科研项目(No.D20101801)

摘　　要：目的:优化盐酸罗沙替丁醋酸酯(ROX)缓释片的处方。方法:采用粉末直接压片法制备ROX缓释片,以1、4、8 h的体外累积释放度的综合指标为指标,以乳糖/微晶纤维素(MCC)(m/m)、乙基纤维素(EC)用量、羟丙基甲基纤维素(HPMC)用量为因素,采用星点设计-响应面法优化制剂处方,并进行验证。结果:最优处方为ROX 75 mg、乳糖45 mg、MCC 91 mg、EC 65 mg、HPMC 124 mg、微粉硅胶2 mg。所制缓释片1、4、8 h的体外累积释放度分别为(30.7±0.5)%、(65.8±0.7)%、(89.4±0.6)%,与预测值的相对误差分别为0.6%、0.8%、1.2%。结论:成功制得达到预期缓释效果的ROX缓释片。OBJECTIVE:To optimize the formulation of Roxatidine acetate hydrochloride(ROX)sustained-release tablets.METHODS:ROX sustained-release tablets were prepared by direct powder compression method.Central composite design-response surface methodology was used to optimize the formulation with composite index of 1,4,8 h in vitro accumulative release rate as index,using mass ratio of lactose/microcrystalline cellulose(MCC)(m/m),ethyl cellulose(EC)amount and HPMC amount as factors.Validation test was also conducted.RESULTS:The optimal formulation was as follows as ROX 75 mg,lactose 45 mg,MCC 91 mg,EC 65 mg,HPMC 124 mg,micropowder silica gel 2 mg.1,4,8 h in vitro accumulative release rates of prepared sustained-release tablets were(30.7±0.5)%,(65.8±0.7)%,(89.4±0.6)%,respectively.Related errors of them to predicted value were 0.6%,0.8%,1.2%,respectively.CONCLUSIONS:ROX sustained-release tablets are prepared successfully,and sustained-release effect is consisted with the expected effect.

关 键 词：盐酸罗沙替丁醋酸酯 缓释片 星点设计-响应面法 制备 处方优化 

分 类 号：R943[医药卫生—药剂学]