Formulation development and evaluation of metoprolol succinate sustainedrelease tablets using 32 factorial design

摘要

The main objective of present investigation is to formulate the sustained release tablet of Metoprolol Succinate using 32 factorial design. Metoprolol Succinate, is a selective β1blocker, to treat Hypertension & Heart Failure. The SR tablets of Metoprolol Succinate were prepared employing different concentrations of HPMCK15M and HPMCK100M in different combinations as a rate retardants by Direct Compression technique using 32 factorial design. The quantity of rate retarders, HPMCK15M and HPMCK100M required to achieve the 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. Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, In-vitro drug release. From the Results it was concluded that all the formulation were found to be with in the Pharmacopoeial limits and the Invitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations(C1, C2). According to SUPAC guidelines the formulation (F5) containing combination of 10% HPMCK15M and 10% HPMCK100M, is the most similar formulation (f2=92.38 & No significant difference, t= 0.0216) to marketed product (Metocard). The selected formulation (F5) follows Higuchi’s kinetics, the mechanism of drug release was found to be Super case II transport (Non-Fickian, n= 0.981).