氨来呫诺口腔贴片的制备、黏附及释药特性评价

Preparation,Adhesion and Drug Release Characteristics of Amlexanox Buccal Tablets

目的优化氨来呫诺口腔贴片的制备工艺,评价其黏附和释药特性。方法以直压型卡波姆71GNF和甘露醇200SD为辅料,采用粉末直接压片法制备氨来呫诺口腔贴片(amlexanox buccal tablets,ABT)。以新鲜鸡蛋膜为人体黏膜替代品,采用改良后的桨法测定ABT的体外释放度,采用药典方法测定ABT的崩解时间;以健康志愿者为受试对象测定ABT在人体口腔内的黏附时间和释放度。结果优化后的氨来呫诺口腔贴片中卡波姆与甘露醇的用量比为1∶1.5,体内黏附时间和释放度与体外测定数据具有良好的相关性。结论粉末直接压片制备氨来呫诺口腔贴片工艺简单、重复性好,适合工业化生产,采用改良后的桨法能较好地预测ABT在人体内的释药行为,通过体外崩解时间的测定可在一定程度上预测体内黏附时间。

Objective To optimize the preparation process of Amlexanox Buccal Tablets（ABT） and to evaluate its adhesion and release characteristics. Methods ABT was prepared by direct powder compression using carbomer 71GNF and mannitol 200SD as auxiliary ma- terial. Egg film was used to substitute oral mucosa. The modified paddle experiment was applied to determine drug release rate. The dis- integration time was tested according to Chinese pharmacopoeia method. The in vivo tests were carried out by healthy volunteers to de- termine the adhesion and release characteristics. Results The optimal ratio of carbomer 71GNF and mannitol 200SD was 1 ： 1.5. Drug release rate and the adhesion time in vivo had good correlation with in vitro. Conclusion Direct powder compression technology for the preparation of ABT is simple, reproducible and suitable for industrial production. The modified paddle experiment and disintegration test can be used to predict in vivo drug release rate and adhesive time.