Class II in the Biopharmaceutical Classification System, eplerenone (EPL) is a selective aldosterone antagonist. Due to its poor solubility, EPL has limited bioavailability. Here, an innovative spray-drying method was used to transform a water soluble polymer into an amorphous dispersion of the EPL. Different polymer SOL/EPL ratios were tested to determine EPL’s solubility and dissolution enhancement properties. In order to learn more about the physical and chemical properties of this novel amorphous solid dispersion (ASD), methods like powder X-ray diffraction spectroscopy (PXRD), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), particle size distribution (PSD) using a Malvern instrument, and scanning electron microscopy (SEM) were used. There was no chemical interaction between the binary mixture of EPL and SOL which was confirmed from the FTIR spectra obtained. The enhancement in the solubility and dissolution of EPL and binary mixture prepared were due to the amorphous conversion of EPL in the SOL polymer (amorphous solid dispersion), which was confirmed from DSC thermogram, PXRD spectra obtained and was also confirmed from the solubility study, in-vitro dissolution study. Finally, ex-vivo intestinal absorption study performed on the goat intestine using amorphous solid dispersion and pure EPL, also improved intestinal absorption of EPL through amorphous solid dispersion prepared.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
customersupport@researchsolutions.com
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.