阿齐沙坦自微乳化释药系统的制备与质量评价  

Preparation and quality evaluation of azilsartan self-microemulsifying drug delivery systems

作　　者：郝菲 姚晨 张燕 秦烨 HAO Fei;YAO Chen;ZHANG Yan;QIN Ye(Department of Pharmacy,No.161 Hospital of the Chinese People′s Liberation Army,Wuhan 430014,China)

机构地区：[1]解放军第一六一医院药剂科

出　　处：《西北药学杂志》2019年第5期647-651,共5页Northwest Pharmaceutical Journal

摘　　要：目的制备阿齐沙坦自微乳化释药系统(Azi-SMEDDSs)并评价其质量。方法通过初步溶解度实验考察阿齐沙坦(Azi)原料药在不同油相、表面活性剂和助表面活性剂中的溶解度,最终选择玉米油为油相,吐温20为表面活性剂,PEG400为助表面活性剂,以粒径分布和多分散性指数(PDI)作为考察指标,利用3因素3水平Box-Behankn实验设计优化Azi-SMEDDSs处方并得到最优处方的设计空间;采用透射电镜观察Azi-SMEDDSs形成微乳的微观形态,采用激光粒度仪测定粒径分布和PDI;比较了Azi原料药与Azi-SMEDDSs的体外溶出速率。结果在Azi-SMEDDSs最优处方设计空间内任取一点:玉米油质量分数为60.0%,吐温20质量分数为25.0%,PEG400质量分数为15.0%,得到微乳的平均粒径为83.7±4.6 nm,PDI为0.251±0.009,透射电镜下显示Azi-SMEDDSs微乳粒径分布较均匀;Azi-SMEDDSs中的药物体外溶出速率显著高于Azi原料药。结论制备的Azi-SMEDDSs体外溶出速率较快,有望改善口服生物利用度,提高治疗效果。Objective To prepare azilsartan self-microemulsifying drug delivery systems(Azi-SMEDDSs)and evaluate its quality.Methods The solubility of azilsartan(Azi)in different oil phases,surfactants and co-surfactants was investigated by preliminary solubility experiments.The corn oil as oil,Tween 20 as surfactant and PEG400 as co-surfactant were taken as independent variables.The dependent factors were particle size distribution and poly-dispersity index(PDI).Azi-SMEDDSs formulations were studied by using the 3-factor 3-level Box-Behankn experiment design system and the optimal formulation was obtained.The microscopic morphology of Azi-SMEDDSs was observed by transmission electron microscopy.The particle size distribution and PDI were determined with a laser particle size analyzer.The in vitro dissolution rates of drug substance and Azi-SMEDDSs were compared.Results The optimal formulation of Azi-SMEDDSs was 60.0%cornoil,25.0%surfactant and 15.0%PEG400,and the formulation showed average particle size of 83.7±4.6 nm,0.251±0.009 PDI.The particle size distribution of Azi-SMEDDSs was uniform under the transmission electron microscope.The in vitro dissolution rate of Azi-SMEDDSs was significantly higher than that of drug substance.Conclusion In this study,the in vitro dissolution rate of Azi-SMEDDSs is faster,which is expected to improve the oral bioavailability and improve the therapeutic effect.

关 键 词：阿齐沙坦 自微乳化释药系统 Box-Behankn实验设计 体外溶出度 

分 类 号：R94[医药卫生—药剂学]