有序介孔二氧化硅改善双嘧达莫的溶出速率

Research on improving dissolution rate of dipyridamole with ordered mesoporous silica

目的:制备有序介孔二氧化硅FDU-12改善双嘧达莫的溶出速率。方法:使用三嵌段共聚物F127和1,3,5-三甲苯制备FDU-12,并以FDU-12为载体,通过吸附平衡法将双嘧达莫(DP)载入FDU-12孔道中。使用透射电镜观察载体FDU-12的形态和结构,并通过氮气吸附和脱吸附分析测定FDU-12的孔径及比表面积,应用差示扫描量热法,X射线衍射法和傅里叶红外光谱法分析载药样品(FDU-DP)中药物的存在状态,并通过体外溶出实验考察其体外溶出度。结果:结构表征证明成功制备了FDU-12,并且FDU-12的介孔孔道有效抑制了双嘧达莫重结晶。体外溶出试验表明双嘧达莫的溶出速率得到显著的提高。结论:FDU-12改善了水难溶性药物双嘧达莫的溶出速率。

Objective： To prepare ordered mesoporous silica FDU-12 to improve the dissolution rate of dipyridamole. Methods： FDU-12 that acted as a carrier was synthesized using Pluronic F127 triblock copolymer and 1,3,5-trimethylbenzene. Dipyridamole（ DP） was loaded onto FDU-12 by adsorption equilibrium method. The structure and morphology of the FDU-12 were investigated by transmission electron microscopy. Nitrogen adsorption / desorption analysis determined the pore size and specific surface area of FDU-12. Differential scanning calorimetry,powder X-ray diffraction and fourier transform infrared spectroscopy were used to analyze the existing state of dipyridamole in drug-loaded sample（ FDU-DP）. In vitro dissolution experiment was performed to determine the dissolution rate. Results： FDU-12 was synthesized successfully and the mesopores effectively suppressed crystallinity of dipyridamole by structure characterization. The in vitro dissolution test showed that the dissolution rate of dipyridamole was improved significantly. Conclusion： FDU-12 is thought to be a promising way to improve the dissolution rate of dipyridamole.