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目的 :制备尼群地平固体分散体 ,增加其溶解度和溶出速度。方法 :以聚乙二醇 6 0 0 0 (PEG 6 0 0 0 )、聚乙二醇 4 0 0 0(PEG 4 0 0 0 )、聚乙烯吡咯烷酮 (PVPk 30 )为载体 ,以溶剂 熔融法和共沉淀法制备尼群地平固体分散体。应用差热分析鉴别药物在载体中的存在状态 ,同时进行溶解度测定和溶出度研究。结果 :尼群地平与载体形成了低共熔物 ,药物以微细结晶存在于载体中 ,载体比例越大 ,药物溶出越快 ,溶解度越大。结论 :尼群地平与 3种载体形成的固体分散体在水中的溶解度均有显著增加 (P <0 .0 5 )。当尼群地平 载体比例达 1∶4时 ,尼群地平从固体分散体中的溶出速度明显大于尼群地平纯药和尼群地平 载体 (1∶8)物理混合物 (P <0 .0 5 )。 3种载体中以PVPK30对尼群地平的溶解度及溶出速度增加最为显著
OBJECTIVE: To prepare a solid dispersion of nitrendipine to increase its solubility and dissolution rate. METHODS: Polyethylene glycol (PEG 6000), polyethylene glycol (PEG 400) and polyvinylpyrrolidone (PVPk 30) were used as carriers, Preparation of solid solution of nitrendipine by coprecipitation method. The application of differential thermal analysis to identify the presence of drugs in the carrier, while solubility determination and dissolution studies. Results: Nitrendipine forms a eutectic with the carrier. The drug is present in the carrier with fine crystals. The greater the carrier ratio, the faster the dissolution of the drug and the greater the solubility. CONCLUSION: The solubility of solid dispersions formed by nitrendipine and three carriers are significantly increased in water (P <0.05). The dissolution rate of nitrendipine from the solid dispersion was significantly greater than that of the combination of nitrendipine and nitrendipine (1: 8) when the ratio of nitrendipine was 1: 4 (P <0.05) . The solubility and dissolution rate of nitrendipine in PVPK30 were the most significant among the three kinds of carriers