星点设计-响应面法优化布地奈德缓释片处方  

Formulation Optimization of Budesonide Sustained-release Tablet by Central Composite Design-response Surface Method

作　　者：任远志 张涛 黄华[1] 刘秀洁 周劲松 

机构地区：[1]重庆医科大学药剂学研究室,重庆400016 [2]福安药业集团重庆礼邦药物开发有限公司,重庆401121

出　　处：《中国药房》2017年第10期1395-1398,共4页China Pharmacy

摘　　要：目的:优化布地奈德缓释片处方。方法:以2、4、8 h的累积释放度为考察指标,采用星点设计-响应面法优化布地奈德缓释片处方中羟丙基纤维素L(HPC-L)用量、大豆磷脂用量、填充剂(固定总量200 mg)乳糖-微晶纤维素质量比,并进行验证。比较所制缓释片与原研制剂在p H 7.2、7.0、6.8的磷酸盐缓冲液中的释药行为。结果:最优处方为布地奈德9 mg、HPC-L 46.49 mg、大豆磷脂9.23 mg、填充剂乳糖-微晶纤维素质量比为1∶2.9;所制缓释片在2、4、8 h的累积释放度分别为21.9%、50.1%、99.5%,与预测值(22.0%、50.0%、98.5%)的相对误差分别为0.45%、0.20%、1.02%(n=3),与原研制剂的累积释放度比较相似因子f2均大于50。结论:成功制得布地奈德缓释片,其释药行为与原研制剂相似。OBJECTIVE：To optimize the formulation of Budesonide sustained-release tablet. METHODS：Using the cumulative releases in 2,4,8 h as investigation indexes,central composite design-response surface method was used to optimize the amount of hydroxypropylcellulose L（HPC-L）,amount of soybean phosphatides,and filler（fixed total 200 mg）lactose-microcrystalline cellulose mass ratio in the formulation of Budesonide sustained-release tablet,and the verification test was conducted.The release behaviors of prepared sustained-release tablet and original preparation in p H 7.2,7.0,6.8 phosphate buffer were com-pared. RESULTS：The optimal formulation was as follow as budesonide of 9 mg,HPC-L of 46.49 mg,soybean phosphatides of9.23 mg,filler lactose-microcrystalline cellulose mass ratio of 1 ∶ 2.9;the cumulative releases in 2,4,8 h were 21.9%,50.1%,99.5%,the relative errors with predicted values（22.0%,50.0%,98.5%）were 0.45%,0.20%,1.02%（n=3）,respectively.Compared with cumulative release of original preparation,the f2 was higher than 50. CONCLUSIONS：Budesonide sustained-release tablet is successfully prepared,which shows similar release behavior to original preparations.

关 键 词：布地奈德 缓释片 星点设计-响应面法 处方筛选 

分 类 号：R944.4[医药卫生—药剂学] Q577[医药卫生—药学]