Chromatography

Biography

Biography: Ebru TÜRKÖZ ACAR

Abstract

Eplerenone (EP) is an antihypertensive agent in the pharmacological group of selective aldosterone receptor antagonists (SARAs). Th e chemical structure of EP is pregn-4-ene-7,21-dicarboxylic acid, 9,11 –epoxy-17-hydroxy-3-oxo, γ-lactone methyl ester (7α, 11α, 17α). EP is slightly soluble in water and its solubility is independent from pH. Low water soluble active agents could not off er an eff ective therapy for the patients. To overcome bioavailability problems related to this property, there are some alternative ways like chemical and polymorphic modifi cations of drugs or designing appropriate pharmaceutical dosage forms. To provide an eff ective treatment, colloidal drug carrier systems of EP were prepared in this study. Investigation of loading capacity and encapsulation effi ciency of these carriers and in vitro drug release profi les, in vivo evaluation offormulations, was highly depend on a reliable quantitative analytical method. Th ere are a few methods for the quantitative
determination of EP. Th ese methods mostly include expensive instruments such as LC–MS, but one exception using high
performance liquid chromatography (HPLC) with UV detection was found., To assess in vivo performance of EP formulations
in rats, the method was not suffi cient to provide specifi city. Th us, a new specifi c method for EP detection was needed by using
the simple extraction and detection techniques. To achieve the quantifi cation of EP in the rat plasma, an HPLC method was
developed and validated. EP spiked rat plasma samples were used for validation step. Th en, spiked plasma was extracted and
analyzed. Th e developed method was used to monitor the kinetic study results.