Formulation and In-Vitro Evaluation of Eplerenone Fast Disintegrating Tablets by Solid Dispersion technique

Abstract

Eplerenone, a BCS class II drug with low bioavailability and t_1/2  of 3-6 hrs is primarily used to treat Congestive Heart Failure (CHF) and hypertension. So, to develop the biological performance of Eplerenone, solid dispersion along with oral disintegrates was prepared by employing HP beta-Cyclodextrin and beta-Cyclodextrin. Eplerenone solid dispersions were repared with various carriers in varying ratios of carrier and drug respectively (0.5:1, 1:1 and 1.5:1). Results of prepared Eplerenone solid dispersions through solvent evaporation technique were demonstrated which comprise melti g point determination, solubility, entrapment efficiency, drug content uniformness and in-vitro  breakup studies. Characterization of solid state was done by FT-IR. From comparison of all the formulation characteristics, formulation (F3) containing Eplerenone + Hp beta-cyclodextrin (1:1.5) showed better results y solvent evaporation technique. As maximum drug was released from F3 at the end of 60 min, this formulation was decided as the best. From the optimized formulation, Fast dissolving tablets were formulated employing various disintegrates in varying concentrations. The pre and post compression parameters were calculated and the results were pecified. All the results were within the acceptable range. An in-vitro drug discharge study of the formulated drug was done victimisation pH 6.8 buffers. F6 formulation containing crospovidone (13.5mg) exhibited 97.36% drug release within 20mins. The optimized formulation follows zero-order release kinetics.