联苯双酯固体分散体的制备及表征

Preparation and characterization of bifendate solid dispersions

目的制备联苯双酯固体分散体,以提高联苯双酯的体外溶出度。方法以聚乙二醇6000(Polyethylene glycol 6000,PEG6000)、聚维酮K30(Povidone K30,PVP K30)和泊洛沙姆188(Poloxamer188,P188)为载体,采用溶剂挥发法制备联苯双酯固体分散体。同时,采用差示扫描量热法(Differential scanning calorimetry,DSC)、X射线粉末衍射法(X-ray powder diffraction,XRPD)和红外光谱法(Infrared Spectroscopy,IR)等技术对固体分散体进行表征。结果在三种载体制备的固体分散体中,联苯双酯的体外溶出度明显提高,且三种载体对联苯双酯的增溶效果依次为:P188>PVP K30>PEG6000。DSC、XRPD和IR结果表明,联苯双酯以分子形式或无定型存在于固体分散体中。结论采用溶剂挥发法制备联苯双酯固体分散体,能明显提高联苯双酯体外溶出度。

Objective A solid dispersion of bifendate was prepared to improve the in vitro dissolution of bifendate.Methods Bifendate solid dispersions were prepared by solvent evaporation method using PEG6000,PVP K30 and P188 as carriers.Meanwhile,the solid dispersions were characterized by DSC,XRPD and IR.Results The in vitro dissolution of bifendate was significantly improved in the solid dispersion prepared by three carriers,and the solubilization effect of the three carriers on bifendate was in the order of P188>PVP K30>PEG6000.DSC,XRPD and IR results showed that bifendate was in an amorphous or molecular form in the solid dispersions.Conclusions The in vitro dissolution of bifendate can significantly improve after it was loaded in the solid dispersions by solvent evaporation method.