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目的:考察基于渗透泵酶触发原理的5-氨基水杨酸(5-ASA)结肠定位微丸的体内释药行为,评价其结肠定位释药特性。方法:将5-ASA结肠定位微丸(微丸组)与5-ASA羧甲基纤维素钠混悬溶液(对照组)分别给大鼠灌胃,于规定时间间隔从大鼠心脏取血,并取出胃、小肠、盲肠、结肠及其内容物,计算相对靶向释药指数(DDI值);扫描电镜观察不同部位的微丸表面结构。结果:微丸组在胃、小肠、盲肠、结肠中的DDI值分别为11.09,12.08,187.25,181.68。扫描电镜观察结肠内微丸有清晰可见的孔径。结论:5-ASA结肠定位微丸具有良好的结肠定位释药性。
OBJECTIVE: To investigate the in vivo release behavior of 5-aminosalicylic acid (5-ASA) colon-targeting pellets based on the principle of osmotic pump enzyme triggering and to evaluate the colon-specific release characteristics. Methods: The rats were gavaged with 5-ASA colonic pellets (pellets group) and 5-ASA sodium carboxymethylcellulose suspension solution (control group) respectively. Blood was drawn from the rat's heart at regular intervals, The stomach, small intestine, cecum, colon and their contents were removed and the relative target release index (DDI) was calculated. The surface structure of the pellets at different sites was observed by scanning electron microscopy. Results: The DDI values of pellets in the stomach, small intestine, cecum and colon were 11.09, 12.08, 187.25 and 181.68, respectively. Scanning electron microscopy colon pellets have clearly visible pore size. CONCLUSION: 5-ASA colon-targeted pellets have good colon-site release properties.