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目的:制备伊曲康唑纳米晶体并进行药剂学性质表征。方法:采用湿法介质研磨结合冷冻干燥工艺制备伊曲康唑纳米晶体;采用马尔文激光粒度测定仪测定伊曲康唑纳米晶体的粒径和多分散系数(PDI);采用扫描电镜观察伊曲康唑粒子的形态;采用差示扫描量热法、红外光谱法、X-射线粉末衍射法研究伊曲康唑纳米化前后晶型和化学结构变化情况;采用浆法比较伊曲康唑纳米化前后及市售胶囊在pH1.2、pH4.0、pH6.8的溶液以及水等4种溶出介质中的溶出行为。结果:制备的伊曲康唑纳米晶体平均粒径为317 nm,PDI值0.29;纳米化前后伊曲康唑晶型和化学结构没有发生明显改变;在pH1.2、pH4.0、pH6.8的溶液以及水等4种溶出介质中,药物溶出速率快慢顺序为伊曲康唑纳米晶体>市售伊曲康唑胶囊>物理混合物及伊曲康唑原料药。结论:采用湿法介质研磨结合冷冻干燥工艺,可以制备平均粒径小且较为均匀的伊曲康唑纳米晶体;纳米化后伊曲康唑仍为结晶态;制成纳米晶体可以明显改善伊曲康唑的溶出性能,利于改善药物的口服吸收。
Objective: To prepare itraconazole nanocrystals and characterize their pharmacology. Methods: Itraconazole nanocrystals were prepared by wet media grinding and freeze-drying process. The particle size and polydispersity (PDI) of itraconazole nanocrystals were measured by Malvern laser particle size analyzer. The morphology and the chemical structure of itraconazole nanoparticles were investigated by differential scanning calorimetry, infrared spectroscopy and X-ray powder diffractometry. Compared with itraconazole nanocrystallization Before and after and the commercial capsules in pH1.2, pH4.0, pH6.8 solution and water dissolution of four dissolution behavior. Results: The average particle size of itraconazole nanocrystals was 317 nm with a PDI value of 0.29. The crystal forms and chemical structures of itraconazole did not change significantly before and after nanodization. At pH 1.2, pH 4.0, pH 6.8 Solution and water four dissolution medium, the dissolution rate of the drug in the order of itraconazole nanocrystals> itraconazole capsules commercially available> physical mixture and itraconazole API. Conclusion: Itraconazole nanocrystals with small average particle size and uniform distribution can be prepared by wet media grinding combined with freeze-drying process. Itraconazole is still in crystalline state after nanocrystallization. Conazole dissolution properties, which will help improve the oral absorption of drugs.