DESIGN, DEVELOPMENT AND EVALUATION OF LABETALOL HCl GASTRO RETENTIVE FLOATING TABLETS

Abstract

The main aim of present research study is to formulate the floating tablets of Labetalol HCl using 32 factorial design. Labetalol HCl, non selective α, -βadreno receptor antagonist, Indicated for treatment of Hypertension/moderate Heart Failure. The Floating tablets of Labetalol HCl were prepared employing different concentrations of HPMCK4M and sodium bicarbonate in different combinations by Direct Compression technique. The concentration of HPMCK4M and sodium bicarbonate required to achieve desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. 9 formulations were designed and are evaluated for hardness, friability, thickness, % drug content, Floating Lag time, In-vitro drug release. From the Results concluded that all the formulation were found to be within the Pharmacopoeial limits and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept, slope & regression coefficient were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations. According to SUPAC guidelines the formulation (F8) containing combination of 20% HPMCK4M and 3.75% sodium bicarbonate, is the most identical formulation which meets the objective of work. The selected formulation (F8) follows Higuchi’s kinetics, and the mechanism of drug release was found to be NonFickian Diffusion (n= 1.033, Super Case-II transport).