Stability of Cefuroxime Axetil Oral Suspension at Different Temperature Storage Conditions

Alija Uzunović,Edina Vranić

doi:10.17305/bjbms.2008.3005

Alija Uzunović, Edina Vranić

Open Access

https://doi.org/10.17305/bjbms.2008.3005

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Abstract

Stability testing of an active substance or finished product provides information of the variation of drug substance or final product with time influenced by a variety of environmental factors such as temperature, humidity and light. Knowledge gained from stability studies enables understanding of the effects of the environment on the drugs. The aim of our study was to determine the stability of cefuroxime axetil oral suspension at different temperature storage conditions (stored at room /20 degrees C/ and refrigerated /5 degrees C/ conditions). Determination of cefuroxime (as cefuroxime axetil) was performed by dissolution testing. Fractions of the released cefuroxime axetil were compared using f2 value. After interpolating data for dissolution profiles at room and refrigerated conditions the following f2values were obtained: 62,56; 56,32 and 36,18 on 3rd, 6th and 10th day, respectively. These values indicate similarities in drug release from analyzed cefuroxime axetil oral suspension on 3rd, 6th day, and differences on 10th day. Based on our results, we may assume that cefuroxime axetil oral suspension preserves its stability for 10 days after reconstitution under room and refrigerated conditions. It is obvious, according to the f2 value obtained on the 10th day, that there is a difference between the released cefuroxime axetil from oral suspension at room (87,68%) and refrigerated (92,35%) conditions. Concentration changes can be caused by the mechanisms associated with drug release and hydrolytical decomposition of the sample and higher temperatures during longer period of storage.

Highlights

Cefuroxime axetil ( -acetoxyethyl ester of cefuroxime) is orally active prodrug of cefuroxime, second generation semi-synthetic cephalosporine antibiotic
Cefuroxime axetil is absorbed from gastrointestinal tract and rapidly hydrolyzed by nonspecific esterase in the intestinal mucosa and blood releasing microbiologically active form, cefuroxime
Cefuroxime axetil (Figure .) has a carbamoyl group in position, which accounts for considerable metabolic stability, and a methoxyimino group in position, which provides resistance to β-lactamase attack and, together with a furyl ring, contributes to the antibacterial properties of the molecule by enhancing its activity against Gram-negative bacteria

Summary

Introduction

Cefuroxime axetil ( -acetoxyethyl ester of cefuroxime) is orally active prodrug of cefuroxime, second generation semi-synthetic cephalosporine antibiotic. For the preparation of pharmaceutical formulations only the amorphous form is used It has better physicochemical and biological properties than the crystalline form, e.g. significantly higher solubility and bulk density as well as higher degree of absorption after oral administration ( , ). Due to their possible composition, pharmaceuticals are especially sensitive to environmental factors. Stability testing of an active substance or finished product provides information on how the quality of drug substance or drug product varies with time influenced by a variety of environmental factors such as temperature, humidity and light. Determination of cefuroxime (as cefuroxime axetil) was performed by dissolution testing

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