重结晶微粉化提高布洛芬溶出度

A recrystallization method for improving ibuprofen dissolution

文中在 1L烧瓶实验装置中采用重结晶法以乙醇和丙酮为溶剂 ,水为沉淀剂进行了布洛芬的微粉化实验。通过优化重结晶过程的参数 ,例如体积比、温度、浓度、搅拌转速和连续相加料速度 ,确定了在温度低于 5℃ ,转速高于 80 0r/min ,以乙醇为溶剂 ,按 1∶2的体积比以 8mL/min以下的连续相加料速度将 0 6～ 0 8mol/L的布洛芬乙醇溶液加入水可以得到平均粒度小于 4 μm ,收率在 92 %以上的布洛芬产品。通过扫描电镜、X射线衍射对布洛芬粒度与结晶性进行了对比分析 ,以及通过溶出度测试比较了重结晶产品与原料药溶出的差异 ,显示出了重结晶产品在溶出方面的优越性。

The recrystallization method is an important method to produce micronized drugs. In an one liter flask device, with ethanol and acetone chosen as solvent candidates and distilled water chosen as precipitator, the main factors which might influence the mean particle size and recovery rate of recrystallized ibuprofen were studied in this article. Experimental results show that the optimum recrystallization conditions are as following: ethanol chosen as solvent, 5?℃ or lower temperature, 800?r/min or higher stirring speed, and adding 0.6～0.8?mol/L ibuprofen ethanol solution to water with a volume ratio less than 1∶2 and solution infusion rate less than 8?mL/min. Under such conditions, a product of 4?μm mean particle size and over 92% recovery rate was prepared. The recrystallized product and ibuprofen material were characterized by XRD and SEM techniques. Furthermore, a dissolution experiment proved the advantages of the recrystalllized product.