共无定型瑞格列奈-糖精的理化性质表征

Physicochemical characterization of co-amorphous repaglinide-saccharin

摘要: 采用真空减压旋转蒸发溶剂法制备得到了物质的量比为1∶1和2∶1的共无定型瑞格列奈-糖精。通过差示扫描量热分析法(DSC)、红外光谱法(FTIR)和粉末X线衍射法(PXRD)对共无定型瑞格列奈-糖精进行了表征。考察了其溶解度和溶出度，并与瑞格列奈晶体及无定型进行比较。结果表明，共无定型瑞格列奈-糖精在水及各种pH缓冲液中瑞格列奈的溶解度和溶出度均得到了显著的提高。在长期试验中，90 d内共无定型瑞格列奈-糖精能维持良好的无定型状态和化学稳定性。

Abstract: The rotary solvent-evaporation method was successfully used to prepare the co-amorphous repaglinide-saccharin(REP-SAC)with molar ratios of 1 ∶1 and 2 ∶1, respectively. The co-amorphous solids were characte-rized by differential scanning calorimetry(DSC), infrared spectroscopy(FTIR)and powder X-ray diffraction(PXRD). The solubility and dissolution of co-amorphous REP-SAC in various buffers were tested and compared with crystalline REP, physical mixtures of REP and SAC with molar ratios of 1 ∶1 and 2 ∶1, and amorphous REP. It was observed that co-amorphous REP-SAC had significantly enhanced solubility and dissolution. Also, co-amorphous REP-SAC was proved to be maintained in amorphous state with similar chemical stability to crystalline REP.