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目的采用固体分散技术提高难溶性药物托伐普坦的体外溶出度。方法选用聚维酮K29/32为载体材料,以溶剂蒸发法制备托伐普坦固体分散体。采用差示扫描量热法(DSC)、X-射线粉末衍射法(XRPD)对所得固体分散体进行鉴定,并进行溶解度、体外溶出实验。结果固体分散体的DSC图谱及XRPD确定了托伐普坦以无定形态分散在载体中,体外溶解实验表明其溶出较原料药、物理混合物均有明显提高。结论将托伐普坦与聚维酮K29/32制成固体分散体,其分散状态发生了改变,溶出性能明显提高。
Objective To improve the dissolution rate of soluble drug tolvaptan in vitro by solid dispersion technique. Methods Povidone K29 / 32 was used as carrier material, and the solid solution of tolvaptan was prepared by solvent evaporation method. The obtained solid dispersions were identified by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD), and their solubility and in vitro dissolution were tested. Results The DSC and XRPD of solid dispersions confirmed that tolvaptan was dispersed in the carrier in an amorphous state. The in vitro dissolution experiments showed that the dissolution of tolvaptan was significantly higher than that of the bulk drug and the physical mixture. Conclusion The solid dispersion of tolvaptan and povidone K29 / 32 has been prepared, and its dispersion state has been changed, and the dissolution performance has been obviously improved.