Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Technology 06100-Tandogan, Ankara, Turkey.
Acta Pharm. 2011 Sep 1;61(3):303-12. doi: 10.2478/v10007-011-0028-0.
Floating dosage forms of acetylsalicylic acid, used for its antithrombotic effect, were developed to prolong gastric residence time and increase bioavailability. In the two-layer tablet formulation, hydroxypropyl methylcellulose (HPMC) of high viscosity and an effervescent mixture of citric acid and sodium bicarbonate formed the floating layer. The release layer contained the drug, direct tableting agent and different types of matrix-forming polymers such as HPMC of low viscosity, sodium carboxymethylcellulose and chitosan. Tablets were prepared using a direct compression technique. The effect of formulation variables on physicochemical and floating properties and the drug release from tablets were investigated. Floating ability was dependent on the amount of effervescent agent and gel-forming polymer of the floating layer. Drug release was prolonged to 8 hours by changing the type and viscosity of the matrix-forming polymer in the drug-loading layer and all formulations showed a diffusion release mechanisms.
为了延长胃内停留时间并提高生物利用度,开发了用于抗血栓作用的阿司匹林浮动剂型。在双层片剂制剂中,高粘度的羟丙基甲基纤维素(HPMC)和柠檬酸与碳酸氢钠的泡腾混合物形成了浮动层。释放层包含药物、直接压片剂和不同类型的基质形成聚合物,如低粘度的 HPMC、羧甲基纤维素钠和壳聚糖。片剂采用直接压缩技术制备。研究了制剂变量对物理化学性质和片剂的漂浮性能以及药物释放的影响。漂浮能力取决于浮层中泡腾剂和凝胶形成聚合物的用量。通过改变药物层中形成基质的聚合物的类型和粘度,将药物释放时间延长至 8 小时,所有制剂均显示出扩散释放机制。