萘普生在介孔分子筛MCM-41中的负载及其溶出性能

Dissolution of Naproxen in Mesoporous Molecular Sieve MCM-41

用含氨基的偶联剂修饰介孔分子筛MCM-41的表面,将修饰前和修饰后的介孔分子筛分别负载难溶性药物萘普生(NAP),利用X射线衍射、傅里叶变换红外光谱、差示扫描量热分析、扫描电子显微镜、透射电子显微镜和N2吸附-脱附分析等技术分别对其进行了结构表征和性能测试。结果表明,药物分子存在于分子筛的孔道中。负载在MCM-41中的萘普生溶出速率远优于原料药,60 min时大约溶出70%。氨基修饰后的药物释放速率比修饰前有所减慢,表明可通过氨基修饰调节释放速率。

The poorly-water soluble drug naproxen（NAP） was loaded on modified and unmodified mesoporous molecular sieves MCM-41.The drug-loaded samples were characterized by X-ray diffraction（XRD）,Fourier transform infrared spectroscopy（FT-IR）,differential scanning caborimetry（DSC）,scanning electron microscopy（SEM） analysis,transmission electron microscopy（TEM） analysis,nitrogen adsorption/desorption isotherms,respectively.The results showed that the hexagonal mesoporous structure was still remained after loading with drug molecules,which were entrapped inside the mesopores.The dissolution rate of NAP released from mesoporous molecular sieves MCM-41 was faster compared with the dissolution rate of pure NAP.In simulated intestinal fluid,the MCM-41-NAP and MCM-41-NH2-NAP exhibited 70% mass fraction burst release within 60 min.Remarkably,the dissolution rate of NAP released from all mesoporous materials is faster compared with the dissolution rate of pure NAP.At the same time,the release rate of NAP from the functionalized mesoporous materials was effectively controlled compared with that of the unmodified materials.