DESIGN, FORMULATION AND EVALUATION OF SUSTAINED RELEASE TABLETS FOR ANTIHYPERLIPIDEMIC AGENT

Purpose: The main objective of the present research investigation is to formulate the sustained release formulation of Rosuvastatin. Rosuvastatin, an antihyperlipidemic agent, belong BCS class-II agent. Methods: The SR tablets of Rosuvastatin were prepared to employ different concentrations of HPMCK4M and SCMC in different combinations by direct compression using 3² factorial designs. The concentration of polymers, HPMCK4M, and SCMC required to achieve the desired drug release was selected as independent variables, X_1, and X₂ respectively whereas, time required for 10% of drug dissolution (t_10%), 50% (t_50%), 75% (t_75%) and  90% (t_90%)  were selected as dependent variables. Results and Discussion: 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 within the Pharmacopoeial limits and the in-vitro dissolution profiles of all formulations were fitted into different kinetic models, the statistical parameters like intercept, slope & regression coefficient were calculated. Polynomial equations were developed for dependent variables. The validity of developed polynomial equations was verified by designing 2 checkpoint formulations (C₁, C₂). According to SUPAC guidelines the formulation (F₄) containing 30 mg of HPMCK4M and 40 mg of SCMC, is the most similar formulation (similarity factor f₂ = 89.561, dissimilarity factor f₁ = 1.543 and no significant difference, t=0.0056) to marketed product (CRESTOR). Conclusion: The selected formulation (F₄) follows zero order, Higuchi’s kinetics, and the mechanism of drug release was found to be non-Fickian diffusion (n= 0.963).