Box-Behnken效应面法优化盐酸坦洛新缓释微丸包衣处方  

Optimization of coating film formulation of tamsulosin hydrochloride extended-release pellets by Box-Behnken response surface methodology

作　　者：谢向阳[1] 陈晨[1] 林雯[2] 韩亮[1] 汪涛[3] 

机构地区：[1]广州军区武汉总医院,湖北武汉430070 [2]黄石市爱康医院检验科,湖北黄石435000 [3]中国人民解放军武汉疗养院,湖北武汉430074

出　　处：《中国医院药学杂志》2014年第20期1743-1747,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:通过Box-Behnken效应面法优化盐酸坦洛新缓释微丸包衣处方。方法:以缓释包衣液聚合物比例(X1,Eudragit RS 30D:Eudrgit RL 30D)和包衣增重(X2,%)为考察因素,以2,6,10 h的累积释放度Y2 h,Y6 h,Y10 h为考察指标,利用二因素三水平Box-Behnken效应面法优化缓释微丸包衣处方,并采用f2相似因子对自制制剂和市售制剂的体外释放度进行比较。结果:聚合物比例(Eudragit RS30D∶Eudrgit RL30D)为30∶70,包衣增重为时25%,所得缓释微丸各时间点释放度符合标准;自制制剂和市售制剂在释放介质中的释放度相似因子f2为69.6。结论:采用Box-Behnken效应面法优化盐酸坦洛新缓释微丸包衣处方的预测性良好,制得的盐酸坦洛新缓释微丸体外释放符合要求。OBJECTIVE To optimize the coating film formulation of tamsulosin hydrochloride extended-release pellets by Box-Behnken response surface methodology.METHODS In the Box-Behnken response surface methodology,the ratio of Eudragit RS 30 D to Eudrgit RL 30D（X1） and coat weight gain（X2） were selected as the independent variables,and in vitro accumulated releases from the pellets at 2,6,and 10 h were chosen as dependent variables.The release rate of the extended-release pellets and the reference pellets were compared by calculating the similarity factor f2 value.RESULTS When the ratio of Eudragit RS 30 D to Eudrgit RL 30D（X1） was 30∶70 and coat weight gain（X2） was25%,the accumulative release percentages at 2,6,10 h were consistent with the criterion of USP,The f2 for the extended-release pellets and the reference pellets in dissolution mediums was 69.6.CONCLUSION The Box-Behnken response surface methodology was successfully used to optimize the coating film formulation of tamsulosin hydrochloride extended-release pellets.The release profiles of the pellets complied with requirements of the USP.

关 键 词：BOX-BEHNKEN效应面法 盐酸坦洛新 缓释微丸 包衣处方 

分 类 号：R944[医药卫生—药剂学]