Abstract
Purpose: The main objective of present research investigation is to formulate the sustained release formulation of Rosuvastatin. Rosuvastatin, an antihyperlipidemic agent, belongs BCS class-II agent.Methods: The SR tablets of Rosuvastatin were prepared employing different concentrations of HPMCK4M and SCMC in different combinations by Direct Compression using 32 factorial design. 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: 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 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 dependent variables. Validity of developed polynomial equations were verified by designing 2 check point 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 & 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).
Highlights
Oral administration is the most convenient, popularly used route of administration for both conventional and novel drug delivery systems
Sustained release tablets of Rosuvastatin were prepared and optimized by 32 factorial design in order to select the best combination of different Polymers, HPMCK4M, sodium carboxy methyl cellulose (SCMC) and to achieve the desired prolong/sustained release of drug from the dosage form/ Formulation
The two factorial parameters involved in the development of formulations are, quantity of HPMCK4M & SCMC polymers as independent variables (X1, X2), and In vitro dissolution parameters such as t10%, t50%, t75% & t90% as dependent variables
Summary
Oral administration is the most convenient, popularly used route of administration for both conventional and novel drug delivery systems. Sustained release (SR) tablet formulations offer better patient compliance, maintain uniform drug levels, reduce dose and side effects, and increase the safety margin for high-potency drugs [3]. The goal of a sustained release dosage form is to maintain therapeutic blood or tissue levels of the drug for an extended period. This is usually accomplished by attempting to obtain zero-order release from the dosage form. Zero-order release constitutes the drug release from the dosage form that is independent of the amount of drug in the delivery system Systems that are designated as prolonged release can be considered as attempts at achieving sustained release delivery [4,5,6,7]
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