Investigation of Dry Granulation and Wet Granulation Effect on Dissolution Profile of the Developed Film Coated Tablets Containing Eplerenone

Deniz Ei̇,Gun G,Toprak C

doi:10.16966/2470-1009.164

Abstract

The objective is to observe and improve drug release of Eplerenone which is BCS Class II API by applying dry granulation and wet granulation process. Inspra 50 mg film coated tablets, manufactured by Pfizer, were taken as reference product to compare with dissolution profiles of dry granulation applied product and wet granulation applied product. Investigation of the effect of wet granulation process on dissolution profiles of Eplerenone 50 mg film coated tablets has been demonstrated out in the scope the study. While f2 similarity factor is 44.93 for dry granulation applied product, it is 60.62 for wet granulation applied product when compared to reference product. It comply that dissolution rate of wet granulation applied product is more proper to the specification than dry granulation applied product. The study demonstrates the effect of different granulation process on dissolution rate.

Highlights

Eplerenone with the CAS registry number of 107724-20-9 is a Selective Aldosterone Receptor Antagonist (SARA) and used for treatment of the patients with chronic heart failure and high blood pressure caused by resistant hypertension due to elevated aldosterone
In the scope of the study, dissolution test was applied on both reference product which is Inspra 50 mg film coated tablets and Eplerenone 50 mg film coated tablets which are produced by applying two different methods that are dry granulation and wet granulation
The results of dissolution rate profiles of reference product and dry granulation applied product and wet granulation applied product are given in the table 3 and table 4, respectively

Summary

Introduction

Eplerenone with the CAS registry number of 107724-20-9 is a Selective Aldosterone Receptor Antagonist (SARA) and used for treatment of the patients with chronic heart failure and high blood pressure caused by resistant hypertension due to elevated aldosterone. The molecular formula and weight of Eplerenone are C24H30O6 and 414.49 respectively [1]. Within the Biopharmaceutics Classification System (BCS), Eplerenone is class-II Active Pharmaceutical Ingredient (API) [2]. It is off-white to white powder which is soluble in Dichloromethane, slightly soluble in Methanol and insoluble in water [1]. The structure of the Eplerenone molecule is shown in below as figure 1. Eplerenone is found as tablet form with 25 mg and 50 mg dosage in the market and supplied from Pfizer as Inspra 25 mg film coated tablets and Inspra 50 mg film coated tablets

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Conclusion