不同载体非诺贝特固体分散体的表征、溶出度和抑晶作用的对比研究

Comparisons of Characterization,Dissolution and Crystallization Inhibition Effect of Different Fenofibrate Solid Dispersions

分别以Soluplus？、聚乙二醇（PEG）6000和泊洛沙姆188为载体,采用熔融淬冷技术制备了药物-载体质量比为1∶3的非诺贝特固体分散体,并以扫描电镜（SEM）、粉末X-射线衍射（PXRD）和差示扫描量热（DSC）技术进行表征。PXRD和DSC数据表明,非诺贝特在3种固体分散体中均主要以无定形状态存在。以Soluplus？为载体时,水中固体分散体中非诺贝特的溶出率（60 min时）及溶解度（25℃）显著高于其他两种固体分散体及物理混合物（P〈0.05）。在非诺贝特超饱和的状态下,含有Soluplus？的水溶液中非诺贝特1 h时的溶解度为20.4μg/ml,显著高于含有另两种聚合物的水溶液（P〈0.05）,表现出更好的结晶抑制效应。

Fenofibrate solid dispersions with Soluplus, polyethylene glycol （PEG） 6000 or poloxamer 188 as the carrier in 1 ： 3 drug to carrier ratio were prepared by melt-quenching method and characterized by scanning electron microscopy （SEM）, powder X-ray diffraction （PXRD） and differential scanning calorimetry （DSC）. The results of PXRD and DSC indicated that fenofibrate existed in an amorphous form in three kinds of solid dispersions. The dissolution at 60 min and solubility at 25℃ of fenofibrate from the solid dispersions with Soluplus as the carrier in water were significantly higher than those from the other two solid dispersions and physical mixtures （P〈0.05）. When fenofibrate existed in a supersaturated state in the solution containing Soluplus, the solubility of fenofibrate at 1 h was 20.4 μg/ml, which was significantly higher than that in solutions containing the other two polymers （P〈0.05）. It indicated that the crystallization inhibition effect of Soluplus was the best among three polymers.