DESIGN, FORMULATION AND EVALUATION OF SUSTAINED RELEASE TABLETS FOR ANTIHYPERLIPIDEMIC AGENTAbstract
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, 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. 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).
K. V. Gopaiah *, G. S. N. K. Rao, R. K. Gunda and P. R. Manchineni
Department of Pharmaceutics, K. L. E. F., K. L. College of Pharmacy, Vaddeswaram, Guntur, Andhra Pradesh, India.
11 November 2018
24 November 2018
15 December 2018
31 December 2018