Formulation Development and Optimization of Febuxostat Tablets by Direct Compression Method

Abstract

ABSTRACTThe aim of this study was to develop a simple and cost‐effective Febuxostat film coated tablet formulation by the direct compression method. To obtain the best optimized product, nine different formulations were developed using a central composite rotatable design. Avicel PH‐102, Magnesium stearate, and croscarmellose sodium were taken as independent variables. Micromeritic properties of powder blend showed excellent flow properties and were within USP limits. Tablets were compressed and before coating the core was tested for weight variations, hardness, thickness, friability disintegration, and dissolution. Tablets were film coated using hydroxypropyl methylcellulose 5cps, titanium dioxide, polyethylene glycol, and Instacoat blue, and again tested for the weight variations, assay, and single point dissolution. Three different dissolution media, i.e., 0.1 N HCl (pH 1.2) and phosphate buffer pH 4.5 and 6.8, were used for calculating the percentage release of Febuxostat and their release pattern was compared with an innovator brand by using the model‐independent methods such as similarity (f2), dissimilarity (f1), and model‐dependent methods such as first‐order, Hixson Crowell, and Weibull methods. The results revealed that Trial‐06 showed the maximum similarity, i.e., 81.18, 75.15, and 67.19 in three different pH dissolution media. Dissimilarity factor was also comparable in Trial 06, i.e., 5.21, 11.27, and 6.01 at pH 1.2, 4.5, and 6.8, respectively. Model‐dependent approaches showed the maximum r2 values for Trial 06, i.e., greater than 0.900 for all models in the above‐mentioned pH, whereas the overall release kinetics followed the Weibull model. Selected formulation was kept at 40 ± 5°C and 75 ± 2% relative humidity for accelerated stability studies, and no specific change was observed.