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目的将难溶性微管蛋白抑制剂SUD-35制备成固体分散体,以增加其溶解度及溶出速率。方法以聚乙二醇6000为载体,溶剂-熔融法制备SUD-35固体分散体。采用差示扫描量热分析与X-射线衍射观察药物在载体中的存在状态,并进行溶解度和体外溶出度研究。采用MTT法对SUD-35固体分散体对小鼠白血病L1210细胞药效进行测定。结果 SUD-35固体分散体中SUD-35的溶解度和溶出速率相对原料药和物理混合物均有明显提高,差示扫描量热分析与X-射线衍射结果显示SUD-35以无定型状态存在于固体分散体中,细胞药效结果显示SUD-35固体分散体对小鼠白血病L1210细胞增殖抑制率强于SUD-35纯药。结论聚乙二醇6000为载体制备SUD-35固体分散体,可显著提高SUD-35的溶解度及溶出速率。
Objective To prepare a solid dispersion of the sparingly soluble tubulin inhibitor SUD-35 to increase its solubility and dissolution rate. Methods The solid dispersion of SUD-35 was prepared by solvent-melt method using polyethylene glycol 6000 as a carrier. Differential scanning calorimetry and X-ray diffraction were used to observe the existence of drug in the carrier, and the solubility and in vitro dissolution were studied. The efficacy of SUD-35 solid dispersion on mouse leukemia L1210 cells was determined by MTT assay. Results The solubility and dissolution rate of SUD-35 in SUD-35 solid dispersions were significantly higher than that of API and physical mixtures. The results of differential scanning calorimetry and X-ray diffraction showed that SUD-35 existed in the amorphous state Dispersion, the cell efficacy results show that SUD-35 solid dispersion on mouse leukemia L1210 cell proliferation was stronger than the SUD-35 pure drug. Conclusion Polyethylene glycol 6000 as a carrier to prepare SUD-35 solid dispersion can significantly improve the solubility and dissolution rate of SUD-35.