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 β -Cyclodextrin and β - Cyclodextrin. Eplerenone solid dispersions were repared with various carri- ers 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 evapora- tion technique were demonstrated which comprise melti g point determina- tion, 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) contain- ing Eplerenone + Hp β -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 for- mulation, Fast dissolving tablets were formulated employing various disinte- grates 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 for- mulation follows zero-order release kinetics.