FORMULATION OF CARVEDILOL TABLETS EMPLOYING ?CD, CROSPOVIDONE, POLOXAMER - OPTIMIZATION BY 23 FACTORIAL DESIGN
V. Ramesh*, Rukesh Kumar Jat and K. P. R Chowdary
ABSTRACT
Carvedilol, a widely prescribed anti hypertensive drug belongs to class II under BCS classification and exhibit low and variable oral bioavailability due to its poor aqueous solubility. It needs enhancement in the dissolution rate in its formulation development to derive its maximum therapeutic efficacy. In the present study β-cyclodextrin (βCD), crospovidone and Poloxamer188 were tried to enhance the dissolution rate of Carvedilol in its tablet formulation development. The objective of the study is to optimize Carvedilol tablet formulation by 23 factorial design to achieve NLT 85% dissolution in 10 minutes. For optimization of Carvedilol tablets as per 23 factorial design the βCD, crospovidone and Poloxamer188 are considered as the three factors. The two levels of the factor A (βCD) are 1:1 and 1:5 ratio of
drug: βCD, the two levels of the factor B (crospovidone) are 2% and 30% of drug content and the two levels of factor C (Poloxamer188) are 0% and 2% of drug content. Eight Carvedilol tablet formulations employing selected combinations of the three factors i.e. βCD, crospovidone and Poloxamer188 as per 23 factorial design were formulated. The tablets were prepared by direct compression method and were evaluated. Carvedilol tablet formulations Fb and Fbc disintegrated rapidly with in 1min and gave very rapid dissolution of Carvedilol, above 99% in 10 min. Higher levels of βCD and lower levels of crospovidone gave low dissolution rates of Carvedilol tablets. The increasing order of dissolution rate (K1) observed with various formulations was F1 < Fc < Fa < Fac < Fabc < Fab
Keywords: Optimization, Carvedilol tablets, Factorial design, ?- Cyclodextrin, Crospovidone, Poloxamer188.
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