酮洛芬/酸改性蒙脱土缓释体系的制备及体外释药研究

Preparation and in vitro Release of Ketoprofen/acid-montmorillonite

以盐酸改性蒙脱土为药物载体,采用离子交换法制备了酮洛芬/酸改性蒙脱土(KPF/acid-MMT)复合物.借助X射线衍射(XRD)、比表面积分析和扫描电子显微镜(SEM)等手段对复合物进行了结构表征;采用透析法研究了介质pH值对KPF/acid-MMT释放性能的影响;运用3种数学模型对其体外释放行为进行拟合.结果表明:经酸改性后,蒙脱土的比表面积由19.66 m^2/g增加到202.84 m^2/g,载药量由18.09%提高到37.24%;在人工模拟胃液(pH=1.2)和人工模拟肠液(pH=6.8)中,酮洛芬的累积释放量分别为18.6%和86.7%;零级动力学模型能更好地拟合和描述KPF/acid-MMT在人工模拟肠液中的体外释放行为.酸改性蒙脱土能有效提高药物的负载量,KPF/acid-MMT可实现药物的定向释放和缓释性能,有望制成肠道缓释口服药物制剂.

With acid-montmorillonite （ acid-MMT ） as the carrier of ketoprofe （ KPF ）, KPF/acid-MMT composite was prepared by ion-exchange method and characterized by powder XRD, BET, SEM, etc. The effect of the pH of release media on in vitro release of ketoprofen was assessed by the dialysis method. Three models for in vitro drug release were used to simulate the release performance of KPF from the KPF/acid-MMT composite. The results showed that the surface area of acid-MMT increased from 19. 66 m2/g to 202. 84 m2/g, and the drug-loading increased from 18.09% to 37.24% compared with MMT. In vitro release ability of KPF/ acid-MMT composite was affected by pH of the release solution. In the artificial gastric juice（ pH = 1.2） and in the artificial intestinal juice（ pH = 6.8）, the in vitro cumulative release amounts of the composites were 18.6% and 86.7%, respectively. The zero order kinetics model could be used to describe the variation of in vitro release rate.