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目的制备难溶性药物依折麦布固体分散体,改善其溶出性质,为固体分散体技术提高难溶性药物溶出及生物利用度提供新的参考。方法以共聚维酮(polyvinyl pyrrolidone-vinyl acetate copolymer,PVP VA64)作为亲水性载体材料,采用溶剂挥发法制备不同处方的依折麦布固体分散体,并进行溶出度考察;通过红外光谱法、差式扫描量热法及X射线衍射法对依折麦布固体分散体进行表征与评价。结果依折麦布与PVP VA64的质量比为1∶10时,依折麦布在质量分数0.1%十二烷基硫酸钠醋酸盐缓冲液中30 min累积溶出接近100%,与物理混合物相比,显著提高了依折麦布固体分散体的体外溶出度,物态鉴别表明依折麦布以无定型状态存在于载体中。结论制备依折麦布PVP VA64固体分散体,可显著提高其体外溶出度。
OBJECTIVE To prepare insoluble ezetimibe solid dispersions and improve their dissolution properties, and to provide a new reference for solid dispersion technology to improve the dissolution and bioavailability of poorly soluble drugs. Methods The polyvinylpyrrolidone-vinyl acetate copolymer (PVP VA64) was used as the hydrophilic carrier material, and the ezetimibe dispersions of different prescriptions were prepared by solvent evaporation method. The dissolution rate was investigated. Differential scanning calorimetry and X-ray diffraction were used to characterize and evaluate the ezetimibe dispersion. Results When the mass ratio of ebemarin to PVP VA64 was 1:10, the cumulative elution of ezetimibe in 0.1% sodium lauryl sulfate acetate buffer solution for 30 min was nearly 100% Ratio, significantly increased the dissolution of ezetimibe solid dispersion in vitro, physical identification showed that ezetimibe amorphous state exists in the carrier. Conclusion The preparation of ezetimibe PVP VA64 solid dispersion can significantly improve its in vitro dissolution.