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水溶胶冻干法制备微粉化辛伐他汀

期刊名称：高效化学工程学报，2006，20(5): 814-819
时间：0
分类：TQ028.63[化学工程] R972.6[医药卫生—药品;医药卫生—药学]
作者机构：[1]北京化工大学纳米材料先进制备技术与应用科学教育部重点实验室,北京100029
相关基金：国家“863”计划工作（2004AA218042）：国家杰出青年科学基金（20325621）.
相关项目：流态化技术和多相流反应工程

关键词：辛伐他汀, 水溶胶, 冷冻干燥, 微粉化, Simvastatin, hydrosol, freeze-drying, micronization

中文摘要：

利用反溶剂沉淀法，以甲醇为溶剂，水为反溶剂，将辛伐他汀的甲醇溶液与水混合，形成水溶胶，用液氮速冻，经冷冻干燥，得到微粉化的辛伐他汀。并利用扫描电镜（SEM）、X射线衍射（XRD）、红外光谱分析（FT-IR）、差热分析（DSC）、比表面分析（BET）等分析方法对产品的特性进行了表征，此外还测定了微粉化后产品的溶解速率，并和原料进行了对比。结果表明，辛伐他汀粉体粒度随水与甲醇的混合体积比的增加和辛伐他汀的甲醇溶液浓度的减小而减小，同时团聚减小。而混合温度与转速对产品粒径影响不大。当水与甲醇溶液的混合体积比为10：1，辛伐他汀的甲醇溶液浓度为0．1mol·L^-1时，所得药物颗粒为纤维状，短径在500nm左右，比表面可达10m^2·g^-1以上，同时溶解速率比原粉提高近10倍。

英文摘要：

The micronized Simvastatin was prepared by freeze-drying its hydrosol which was prepared by the antisolvent precipitation method. In the preparation of the hydrosol, the water and methanol were used as antisolvent and solvent, respectively. When the water and methanol solution of Simvastatin were quickly mixed, the hydrosol was obtained. The freeze-dried powder samples were characterized by scanning electron microscopy （SEM）, powder X-ray diffraction （XRD）, Fourier transform infrared spectrometry （FT-IR）, differential scanning calorimetry （DSC）, surface area analysis and dissolution test. The results indicate that the drug particle size decreases with the increase of the volumetric ratio of water/methanol solution of Simvastatin and the decrease of the Simvastatin concentration in methanol. The agglomeration is also reduced with higher volumetric ratio of water/methanol solution and lower Simvastatin concentration. However, the stirring speed and mixing temperature have little effect on the drug particle size. It is found that when the Simvastatin concentration in methanol is 0.1 mol.Lq and the volumetric ratio of water/methanol solution is 10：1, the shape of the micronized Simvastatin prepared by freeze-drying is fibriform with a diameter of about 500 nm. The specific surface area of the micronized Simvastatin is about ｜0 m2.g-l, which is about 2.4 times larger than that of the unmicronized Simvastatin. Furthermore, compared with the unmicronized Simvastatin, the velocity of dissolution of the micronized Simvastatin is enhanced about 10 times. These improvements enhance the bioavailability of the micronized Simvastatin.

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