Acta Pharm. 61 (2011) 303-312

full paper

Original research paper

Effect of formulation parameters on the drug release and floating properties of gastric floating two-layer tablets with acetylsalicylic acid

CANAN HASÇIÇEK, GÜNSELI YÜKSEL-TILKAN, BERNA TÜRKMEN and NURTEN ÖZDEMIR

nozdemir@pharmacy.ankara.edu.tr

Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Technology, 06100-Tandogan, Ankara, Turkey

Accepted Accepted July 12, 2011

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 mechanism.

Keywords: acetylsalicylic acid, two-layer floating tablet, gastric retention, hydroxypropyl methylcellulose, chitosan