响应面法优化盐酸多西环素缓释片处方工艺  

Optimizing the preparation of doxycycline hydrochloride sustained release tablet using response surface methodology

作　　者：喻佰启[1,2] 王永禄[1] 殷海翔[1] 王栋[1] 吕贝贝[1] 李学明[1] 

机构地区：[1]南京工业大学药学院,江苏南京211816 [2]马鞍山市临床检验中心,安徽马鞍山243000

出　　处：《中国生化药物杂志》2014年第3期165-168,共4页Chinese Journal of Biochemical Pharmaceutics

基　　金：江苏省博士后科研资助计划(1301012A);江苏政府留学奖学金(2013);国家自然科学基金资助项目(81170492)

摘　　要：目的利用响应面分析法优化盐酸多西环素缓释片处方。方法通过单因素考察确定对释放度影响最大的3个因素:羟丙基甲基纤维素(hydroxypropyl methyl cellulose,HPMC)的用量、粘合剂聚乙烯吡咯烷酮-K30(polyvinylpyrrolidone-K30,PVPK30)的浓度、乳糖与微晶纤维素(microcrystalline cellulose,MCC)的比例,以2 h、4 h、8 h的释放度综合评分作为响应值,利用BoxBenhnken中心组合实验设计原理,采用三因素三水平的响应面分析法,确定各处方的用量。结果筛选得到优化的处方为:HPMC K15质量分数为片重的30%、粘合剂PVP-K30浓度为10%、乳糖与MCC比例为1:3,其体外释药行为较理想。结论筛选所得的盐酸多西环素缓释片处方工艺稳定可行。Objective In this article Response Surface Analysis(RSA)was applied to optimize the formulation of doxycycline hydrochloride sustained release tablet.Methods Single factor exploration was used to determine the three factors which have the greatest impact on the release rate.The three factors were the dosage of the HPMC in the total weight of the tablet,the concentration of PVP-K30,and the ratio of lactose to microcrystalline cellulose,respectively.The composite score of the release behaviour was taken as the response value.The dosage of the ingredients were determined by Box-Benhnke design principles and 3 factors and 3 levels.Results The optimized formulation and process are as follows:the dosage of the HPMC in the total weight of the tablet was 30%;the concentration of PVP-K30 was 10%,and the ratio of lactose to microcrystalline cellulose was 13.The release behavior in vitro is ideal.Conclusion The optimized preparation process of doxycycline hydrochloride sustained release tablet is stable,highly efficient and suitable for industrial production.

关 键 词：盐酸多西环素 缓释片 响应面法 体外释放度 

分 类 号：R943[医药卫生—药剂学]