Enhancement of Eplerenone Dissolution Rate via Sonoprecipitation: Formulation, Evaluation, Analysis and Stability Testing (RSPT2.5)

Abstract

Eplerenone is a selective mineralocorticoid receptor antagonist. It is used as an oral antihypertensive drug, it has very low solubility in water as according to (BCS) it belongs to Class II. This study aims to improve the solubility of poorly water-soluble eplerenone by using sonoprecipitation technique to increase the dissolution rate. Improving solubility of eplerenone is done by making eplerenone sonocrystal formulation to form a uniform and spherical shape of microcrystals using probe sonicator, followed by evaluation of the prepared sonocrystals by particle size measurement using zetasizer, Fourier transform infrared (FTIR) to determine the interaction between stabilizers (Poloxamer 188 and polyethylene glycol 6000) and drug sonocrystals, differential scanning calorimetry (DSC) to observe the changes occurred in eplerenone during spherical formulation process while X-ray diffraction (XRD) to obtain diffraction patterns for eplerenone, physical mixture, and formulations. The determination of drug content for the prepared soncrocrystal formulations was also performed. In addition, the drug release of the prepared formulae was studied and compared to pure eplerenone by in vitro dissolution. Results show that particle size range from 132nm to 455nm, FTIR and DSC shows that there’s no interaction between stabilizers and drug sonocrystals while XRD indicates the change of the drug into amorphous leading to increase the solubility, the dissolution rate was improved for all the formulations when compared with pure eplerenone. Therefore, it is concluded that the sonoprecipitation technique could be a useful technique to improve the solubility of eplerenone with a reduction in particle size, and enhanced dissolution properties.