伊曲康唑纳米晶体的制备与表征

发布时间：2018-03-29 21:36

本文选题：伊曲康唑　切入点：纳米晶体　出处：《中国医院药学杂志》2017年10期

【摘要】：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。
[Abstract]:Objective: to prepare itraconazole nanocrystals and characterize their pharmacological properties. Methods: itraconazole nanocrystals were prepared by wet medium grinding and freeze-drying. The particle size and polydispersity coefficient of itraconazole nanocrystals were measured by Ma Erwen laser particle size analyzer, the morphology of itraconazole particles was observed by scanning electron microscope, the morphology of itraconazole particles was observed by differential scanning calorimetry, The changes of crystal structure and chemical structure of itraconazole before and after nano-itraconazole were studied by X-ray powder diffraction (XRD). The dissolution behavior of itraconazole nanocrystals before and after itraconazole nanocrystalline was compared with that of marketable capsules in four kinds of dissolution media, such as pH 1.2 ~ (2 +), pH 4.0 ~ (-1), pH 6.8, and water. Results: the average particle size of the prepared itraconazole nanocrystals was 317 nm 路m ~ (-1) PDI 0.29, and before and after nanocrystallization. The crystal form and chemical structure of itraconazole did not change obviously. In the solution of pH 1.2, pH 4.0, pH 6.8, and in four kinds of dissolution media, such as water, water, and so on, The order of drug dissolution rate is itraconazole nanocrystalline marketed itraconazole capsule physical mixture and itraconazole raw material. Conclusion: wet medium grinding and freeze-drying process are used. Itraconazole nanocrystals with small average diameter and uniform size can be prepared, and itraconazole is still crystalline after nanocrystalline. The preparation of nanocrystalline itraconazole can obviously improve the dissolution performance of itraconazole and improve the oral absorption of the drug.
【作者单位】：河北科技大学化学与制药工程学院;河北省药物化工工程技术研究中心;
【基金】：河北省自然科学基金资助项目(编号:H2014208151) 河北省高等学校科学技术研究项目(编号:ZD2014079)
【分类号】：R943

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