Abstract

FORMULATION AND EVALUATION OF STOMACH SPECIFIC FLOATING TABLET OF ANTI-ULCER DRUG

*Kapoor D, Vyas RB, Lad C, Patel M, Sharma S

ABSTRACT

The objective of the present study was to develop floating tablets of lafutidine in order to achieve an extended retention in the upper GIT which may enhance the absorption and improve the bioavailability. The tablets were prepared by gas generation technique using different ratio and concentrations of Methocel K 100, Methocel K 15. Polymer with lower viscosity was found to be beneficial than higher viscosity polymer in improving the release properties of gastroretentive FDDS. Lafutidine a newly developed histamine H2-receptor antagonist was retained in the stomach and assist in improving the oral sustained delivery of drugs in the gastrointestinal tract. The prepared tablets of various formulations were characterized for a total floating time, buoyancy lag time, and percentage drug released. The dried floating granules were characterized for determination of angle of repose, Hausner’s ratio, Carr’s index and porosity. The floating tablets were evaluated for determination of weight variation, hardness, friability, content uniformity, floating lag time, total floating time, in–vitro drug release study, stability studies. The flow properties of prepared floating tablets were found to be excellent. Tablets showed satisfactory characteristics with respect to weight, hardness and friability data. The formulation code LFT6 having Methocel K15 showed superior results it may be constructive for prolonged drug release in the stomach to get better the bioavailability and abridged the dose frequency. In-vitro floatability studies revealed that most of the tablets still floated for more than 9 hours because of their low densities. Lessen in the citric acid level increased the floating lag time but tablets floated for longer duration. An amalgamation of sodium bicarbonate (70mg) and citric acid (20mg) was found to achieve optimum in vitro buoyancy. The drug liberation from the tablets was adequately sustained and non-fickian transport of the drug from tablets was confirmed. Optimized floating tablets showed no significant changes in the physical appearance, drug content, total buoyancy time, and also in vitro dissolution pattern after storage at 40°C/75% relative humidity for 3 months. All the prepared floating tablets exhibited excellent drug release.

Keywords: Gastroretentive drug delivey system, Methocel, Lafutidine, Non-fickian diffusion, Stability studies