Carvedilol (CVD) is an antihypertensive agent with short elimination half-life, pH-dependent solubility, and narrow absorption window. So, the present study aimed to prolong its gastric residence time that entailed a development of an optimized gastroretentive floating tablets (GRFTs) using 32 full factorial design. The tablets were fabricated by direct compression using hydroxypropyl methylcellulose and carbopol 940 as release retarding polymers. The quality attributes of the tablets were evaluated. The buoyancy lag time, total floating time, swelling ability and in vitro release studies were also carried out in 0.1 N HCl (pH 1.2) at 37 ± 0.5 °C. Statistical data analysis revealed that the optimized formulation containing 21.91% HPMC and 15% carbopol 940 had acceptable hardness, optimum floating behavior and 24h controlled-release pattern. The design succeeded to develop CVD-GRFTs with floating ability and controlled release behavior that could improve its solubility, and improve its availability at the best absorptive site.
Key words: floating, full factorial design, optimization, gastroretentive, swelling
|
