托伐普坦固体分散体的制备及体外溶出特性考察

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K_29/32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X-射线粉末衍射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PVP K_29/32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。

Preparation and in Vitro Dissolution of Tolvaptan Solid Dispersion

OBJECTIVE To enhance the dissolution rate of tolvaptan which is a poorly water-soluble drug by solid dispersion.METHODS Solid dispersions of tolvaptan were prepared by solution evaporation method,with polyvinylpyrrolidone(PVP) as a carrier.The physical states of tolvaptan were investigated by differential scanning calorimetry(DSC) and X-ray powder diffraction analysis(XRPD).The solubility and dissolution rate of tolvaptan,solid dispersions and physical mixtures were also compared. RESULTS The DSC and XRPD spectrum of the solid dispersion showed that tolvaptan existed in amorphous form in the carrier.The dissolution of tolvaptan solid dispersions was much faster than that of tolvaptan and the physical mixtures. CONCLUSION Our prepared PVP k29/32 solid dissolution containing tolvaptan has changed its dispersion with higher dissolution