Formulation Development and Evaluation of liquisolid compacts of Epelerenone Hydrochloride
DOI:
https://doi.org/10.61096/ijpar.v8.iss1.2019.99-110Keywords:
Liquisolid compacts, eplerenone hydrochloride, Avicel PH 102, Lactose monohydrate and Syloid 244 FP, XRD, FTIR.Abstract
Eplerenone hydrochloride is a poorly water soluble drug, which is an aldosterone receptor antagonist used in the management of chronic heart failure. The rate of its oral absorption is often controlled by dissolution rate in the gastro intestinal tract. The aim of the present research work was to improve the solubility and dissolution properties of insoluble drug, eplerenone hydrochloride by liquisolid technique. Liquisolid compacts of eplerenone hydrochloride were formulated by dispersing the drug in various non volatile liquid vehicles. Several formulations were prepared using a new mathematical model to calculate the appropriate powder and liquid ingredients required to produce acceptably flowing and compressible mixtures. Avicel PH 102, Lactose monohydrate and Syloid 244 FP were used as carrier materials and Aerosil was used as coating material. The effect of different concentrations of drug on the dissolution rate was studied and it was observed that the liquisolid compacts containing 25%w/w of drug in solvent with lactose monohydrate and Aerosil in the ratio of 10:1 gave the maximum dissolution rate when compared with other formulations. Optimized formulation was compressed into tablets after addition of sodium starch glycolate as a disintegrant in a concentration of 5% of the total weight of tablet and evaluated. Enhanced drug release rates were observed when compared to pure drug and conventional tablet. This is due to increased wetting properties and surface of drug available for dissolution. It was further confirmed from the ex vivo studies that the liquisolid formulation has shown improved rate of permeation than the pure drug and conventional tablet. The crystalline state of eplerenone drug state was changed to amorphous state due to liquisolid formation and was confirmed by X-ray diffraction study. Fourier transform infrared spectroscopy results revealed that there was no interaction between drug and excipients.
