依托泊苷固体分散体的制备及体外研究

目的 制备依托泊苷固体分散体，改善依托泊苷的溶出度。方法 应用聚乙烯吡咯烷酮（PVPK30）和聚乙二醇（PEG6000）为载体，以溶剂法制备固体分散体。采用正交实验设计考察制备固体分散体的最佳工艺条件，并对所得样品进行体外溶出度研究，以X线衍射、DSC-量热分析进行物相鉴定。结果 依托泊苷在载体PVPK30和PEG6000中结晶消失。药物的溶出速度随载体比例增加而增加。结论 采用PVPK30和PEG6000所制依托泊苷固体分散体能显著提高药物的体外溶出度，药物以无定形状态或分子态存在于载体中。

Preparation and evaluation of etoposide solid dispersions in vitro

OBJECTIVE To prepare etoposide solid dispersion to enhance the dissolution rate. METHODS Etoposide solid dispersion was prepared by solvent evaporation method with PVPK30 and PEG6000 as carriers. The dissolution rate was tested. X-ray powder diffractometry and differential scanning calorimetry were applied to determine the status of etoposide in the carriers. RESULTS The crystal form of etoposide disappeared in the dispersion, and the higher the carrier-etoposide ratio, the faster the drug dissolution. CONCLUSIONS The dissolution rate of etoposide has been greatly improved and the drug exists as amorphous or molecular in the carriers.