正交试验法优选染料木素固体分散体制备工艺

Optimization of Preparation Process for Genistein Solid Dispersions by Orthogonal Test

目的:优选染料木素固体分散体的制备工艺。方法:以45 min的累计溶出度和溶出50%所用的时间(t1/2)的综合评分为指标,通过单因素试验和正交试验考察药载比(m/m)、熔融温度、搅拌时间、表面活性剂及过筛目数对染料木素固体分散体制备工艺的影响,并进行验证试验。采用高效液相色谱法测定染料木素含量,色谱条件为Diamonsil C18色谱柱,流动相为甲醇-0.05%磷酸(70∶30),检测波长为262 nm,柱温为30℃,进样量为10μl。结果:固体分散体的最优制备工艺为药载比1∶9,熔融温度75℃,搅拌时间10 min,过40目筛,不加表面活性剂。按最优制备工艺所制的3批样品的t1/2分别为23.32、23.10、23.28 min,累计溶出度分别为91.90%、89.63%、90.08%。结论:优化的制备工艺可行,成功制得染料木素固体分散体。

OBJECTIVE：To optimize preparation process of Genistein solid dispersions. METHODS：With the cumulative dissolution for 45 min and the time of 50% dissolution（t_（1/2））as index,single factor test and orthogonal test were used to investigate the effects of drugs and carrier ratio（m/m）,melting temperature,mixing time,surfactants and mesh sieve on preparation process,and validated.The content of genistein was determined by HPLC. Chromatographic conditions were as follows as Diamonsil C18 column,mobile phase consisted of methanol-0.05% phosphoric acid（70 ∶ 30）,detection wavelength 262 nm,column temperature30 ℃,sample size 10 μl. RESULTS：Optimal preparation process was as follows as drugs and carrier ratio of 1 ∶ 9,melting temperature 75 ℃,mixing time 10 min,mesh sieve 40,no active agent. t_（1/2）of 3 batches of samples prepared by optimized preparation technology were 23.32,23.10 and 23.28 min,and cumulative dissolution of them were 91.90%,89.63% and 90.08%,respectively. CONCLUSIONS：Optimized preparation process is reliable,and Genistein solid dispersion is prepared successfully.