Combinations of Carbapenem with Fluoroquinolones or 1,3,4 -Oxadiazole-2 -Thione Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation

Noor A. Waheed

doi:10.11648/j.jddmc.20160205.11

Abstract

The present work describes the preparation and evaluation of an ophthalmic eye drops of antibacterial agent. The active ingredients (mereopenem, fluoroquinolones & 1,3,4 oxadiazole -2-thione derivatives) have been used in the formulation as eye drops with different doses as broad spectrum antibiotics to minimize the emergence of resistance lesion such as conjunctivitis or corneal ulcers. The experimental effectiveness of single or combination ophthalmic preparation as eye drop is well documented against different types of bacteria e.g. P.aeruginosa and other G(+)ve & G(-)ve bacteria. Other parameters pH, sterility, particulates and contents were calculated. All solutions are sterile, clear, isotonic and pH (5.1-6.3). These solutions didn’t cause any eye irritation in rabbits after daily application for four consecutive days. The potential clinical significant of combination therapy over monotherapy for different types of bacteria has been a controversial subjects for many years especially for ophthalmic purposes. The mechanism of carbapenem and fluoroquinolones are well known, while oxadiazole derivative is expected to inhibit p-amino benzoic acid. The uses of combination drug is thought to minimize the emergence of resistance, safe, potent and increase their synergistic activities.

Highlights

Recent efforts towards combating antibiotic resistance in bacteria have focused on on G+ve bacteria; multidrug-resistant G-ve bacteria pose a significant risk to public health
Five monotherapy solution were tested their activities against different G(+)ve and G(-)ve bacterial activities, and compare their activities with new combination of menopenem (5mg/ml) with fluoroquinolones (Ciprofloxacin, Olfoxacin, Moxifloxacin) 0.3mg/ml or new synthetic oxadiazole-2-thione 0.3mg/ml
All the newly synthesized compounds were evaluated for in vitro antibacterial activity against gram positive and gram negative bacterial strains such as Staphylococcus aureus, Escherichia coli and Pseudomonas aureginosa at concentration 100μg/mL by disc diffusion method by using DMSO as solvent control and nutrient agar was employed as culture media

Summary

Introduction

Recent efforts towards combating antibiotic resistance in bacteria have focused on on G+ve bacteria; multidrug-resistant G-ve bacteria pose a significant risk to public health. Three different synthetic antimicrobial agents were prepared as a septic solution in different concentrations. Derivatives as New Broad Spectrum Bactericidal Antibiotics for Ophthalmic Preparation

Results

Conclusion