应用卡波姆971PNF制备胃内漂浮型缓释片及其体外评价

目的：研制以卡波姆971PNF为骨架材料的新型胃内漂浮型缓释片。方法：分别以诺氟沙星和盐酸二甲双胍为难溶性和易溶性模型药物，以卡波姆971PNF和碳酸氢钠为主要辅料制成胃内漂浮型缓释片，转篮法测定了漂浮片的释放度并检测其漂浮性能：结果：卡波姆971PNF含量在10％，左右时，对诺氟沙星有明显的缓释作用，碳酸氢钠对释放速率有影响，随着卡波姆971PNF含量的增加，诺氟沙星趋向于零级释放：卡波姆971PNF含量在20％，左右时，对盐酸二甲双胍有明显的缓释作用，碳酸氢钠对释放速率影响不明显，其体外释放行为符合ITiguchi方程。卡波姆971PNF及碳酸氢钠均对漂浮性能有影响，而硬度对漂浮性能影响小结论：以卡波姆971PNF制备的胃内漂浮型缓释片具有起漂快，漂浮时间长，缓释效果好，制备工艺简单等优点

Preparation and in vitro Evaluation of Gastric Floating and Sustained-release Tablets Using Carbopol 971PNF

AIM:To develop a novel gastric floating sustained-release tablet using Carbopol 971PNF as matrix material. METHOD:The tablets containing Carbopol 971PNF and sodium bicarbonate as main excipients,and norfloxacin and metformin hydrochloride as an insoluble and a soluble model drug respectively were prepared. In vitro release rates of gastric floating and sustained-release tablets were measured by the basket method and their floating abilities were also tested. RESULT:When the content of Carbopol 971 PNF was at about 10%, the release rate of norfloxacin was obviously sustained, and sodium bicarbonate also had an effect on the release profile. With increasing the content of Carbopol 971 PNF, the release profile of norfloxacin was inclined to zero order. When the content of Carbopol 971 PNF was at about 20%, the in vitro release rate of metformin hydrochloride was obviously sustained and could be fitted Higuchi equation well, while sodium bicarbonate had little effect on the release profile. Both Carbopol 971PNF and sodium bicarbonate can affect the floating abilities of tablets while hardness had little effect on them. CONCLUSION:The tablets prepared using Carbopol 971PNF had advantages of short onset time of floating, long duration of floating and good sustained-release effect. They were easy to prepare.