星点设计-效应面法优化黄独素B分散片的制备工艺

Optimization of Preparation Technology of Diosbulbin B Dispersible Tablets by Central Composite Design-response Surface Methodology

目的:优化黄独素B分散片的制备工艺,提高黄独素B的溶出速率。方法:建立黄独素B分散片体外溶出度测定方法;采用星点设计-效应面法,以填充剂微晶纤维素(MCC)的用量、载药量、助流剂微粉硅胶用量及崩解剂交联羧甲基淀粉钠(c CMS-Na)用量作为考察因素,以体外溶出度和崩解时限为指标,对黄独素B分散片成型工艺进行优选。建立二次多项式模型描述考察指标和4个因素之间的数学关系,绘制效应面图,确定较优处方并进行验证试验。结果:优选的最佳处方比例为:黄独素B:3.13%,MCC:35%,纤维素乳糖:53.24%,c CMS-Na:7.5%,微粉硅胶:1.13%。结论:采用星点设计-效应面法优选的黄独素B分散片成型工艺简便、可行性高,且崩解时限短、体外溶出快。

Objective ： To optimize preparation process of diosbulbin B dispersible tablets, to improve the dissolution rate of diosbul- bin B. Methods ： The in vitro dissolution method for diosbulbin B dispersible tablets was established. With dissolution in vitro and disintegration time limited as indexes, the central composite design-response surface methodology was adopted to optimize formulation process, the amount of microcrystalline cellulose （MCC）, drug loading, amounts of aerosil and cross-linked carboxymethyl starch sodium（ eCMS- Na） were used as factors. Quadratic polynomial model was established to descript the mathematic relation of indexes and four fac- tors. Rendering effect surface, and the prescription was optimized and verified. Results ： The best prescription was as following, with the amount of diosbulbin B was 3. 13% ,the amount of MCC was 35% ,the amount of cellulose lactose was 53.24% ,the amount of cCMS-Na was 7. 5%, and the amount of aerosol was 1.13%. Conclusion：Preparation process of diosbulbin B dispersible tablets by central composite design-response surface methodoloy is simple with short disintegration time limited and fast dissolution in vitro, which is suitable for industrial production.