热熔挤出法制备联苯双酯固体分散体的工艺

目的应用热熔挤出技术制备难溶性药物联苯双酯(bifendate,DDB)的固体分散体,提高DDB的溶出度。方法以共聚维酮(S630)(PVP,N-乙烯基-2-吡咯烷酮和醋酸乙烯酯以质量比为60∶40的比例合成的水溶性共聚物)、PEG6000、丙烯酸树脂Ⅳ为亲水性载体辅料,采用同向双螺杆热熔挤出技术制备DDB固体分散体。比较不同载体挤出物的差示扫描量热图谱和累积溶出曲线,从而判断热熔挤出法对提高DDB溶出度方面的作用。结果采用热熔挤出技术制备的固体分散体可以显著的提高DDB的溶出度。结论采用HME方法制备DDB固体分散体可以显著提高药物的溶出度。

The investigation of hot melt extrusion technology in the preparation of the solid dispersion of bifendate

Objective To prepare the solid dispersion of bifendate(DDB) by applying the hot melt extrusion (HME) technique. Methods Using S-630, PEG6000 and acrylic resins Ⅳ as hydrophilic carrier, solid dispersion was prepared by deploying hot melt extrusion method. Differential scanning calorimetry (DSC) and dissolution measurements were employed to explain the differences in drug release rates of bifendate from powders produced by the HME techniques. Results The hot melt extrusion technology can greatly enhance the dissolution rate with an argument of 3 times more than that of the dropping pill. Conclusion The hot-melt extrusion technology can greatly enhance the dissolution.