Formulation optimization of metoprolol succinate sustained release pellets using central composite design-response surface methodology
10.7644/j.issn.1674-9960.2014.05.007
- VernacularTitle:星点设计-效应面法优化琥珀酸美托洛尔缓释微丸处方
- Author:
Jingjing DAI
;
Yong QIAN
;
Yinghui ZHANG
;
Yuli WANG
;
Xinyi CHANG
;
Meiyan YANG
;
Li SHAN
;
Chunsheng GAO
- Publication Type:Journal Article
- Keywords:
metoprolol succinate;
coated pellets;
sustained release;
central composite design;
response surface methodology
- From:
Military Medical Sciences
2014;(5):351-354
- CountryChina
- Language:Chinese
-
Abstract:
Objective To optimize the formulation of metoprolol succinate ( MS) controlled release pellets by central composite design-response surface methodology .Methods MS sustained-release pellets were prepared using sugar pellet cores as starter beads , ethyl cellulose as coating materials and MS itself as a pore former .The formulation of MS sustained-release pellets was optimized by a central composite design with two factors at five levels .These two factors ( two independ-ent variables) were the pore former level and coating level , and the evaluated indexes ( namely dependent variables ) included the in vitro cumulative release percentages of MS at 1, 4, 8, 12 and 16 h, respectively.Results and Conclusion The results of mathematical equation fitting suggested that the second-order quadratic model was the optimal fitting equa-tion.According to the response surfaces , the optimum values at the pore former level and coating level weve ranged from 16%to 18%and 20% to 25%, respectively .The in vitro cumulative release percentage of MS from the pellets at 1 h reached 9.15%,which consequently eliminated the lag phase in the initial release period and exhibited a good sustained-release effect.Central composite design-response surface methodology can be applied to optimizing the coating formulation for MS sustained release pellets .
