<p>Synthesis, Characterization, and Pharmacodynamics Study of Enrofloxacin Mesylate</p>

Abstract

Introduction: Enrofloxacin is used in the treatment of a wide variety of bacterial infections in mammals. However, its poor solubility limits the clinical use. Methods: In order to improve the solubility of enrofloxacin, the enrofloxacin mesylate (EM) were obtained by a chemical synthesis method. The characterization of EM was carried out using ultraviolet scan (UV), synchronous thermal analysis (SDT), fourier transform infrared spectrometer (FTIR) and mass spectrometry (MS), nuclear magnetic resonance (NMR) and X-ray powder diffraction analysis (XRPD). Acute toxicity of EM in Kunming mice was studied. Besides, pharmacokinetic studies were performed in New Zealand rabbits at a single oral dose of 10 mg/kg, and the antibacterial activity of EM was also evaluated. Results: EM was successfully synthesized and purified. The stoichiometric ratio of mesylate to enrofloxacin was 1:1 and the aqueous solubility of EM was 483.01±4.06 mg/mL, the solubility of EM was about 2000 times higher than enrofloxacin. The oral lethal dose (LD 50 ) of EM was 1168.364 mg/kg, and the pharmacokinetics indicated that the oral relative bioavailability of EM was about 1.79 times and 1.48 times higher than that of enrofloxacin and enrofloxacin hydrochloride, respectively. In addition, the in vitro antibacterial activity of EM was not significantly changed compared with enrofloxacin and enrofloxacin hydrochloride. Conclusion: EM has higher solubility, low toxicity for oral use, and increases the oral bioavailability in rabbit. This study may be of benefit for the development of new enrofloxacin drugs.

Design of experiments and Derringer's desirability function in optimisation and validation of RP-HPLC method for the analysis of enrofloxacin and its impurities

“…Ethyl group attached to the piperazine nitrogen atom increases lipophilicity and tissue penetration, while reducing central nervous system toxicity by reducing binding of the drug to the GABA receptors in brain. Both fluorine and cyclopropyl enhance antibacterial activity [3]. N-Dealkylation yields in an active metabolite ciprofloxacin which is widely used in human medicine.…”

Enhancing the Bioavailability of a Novel Enrofloxacin Salt by Inhibiting Precipitation via a Crystallization Inhibitor

“…Enrofloxacin (ENR) is a key third-generation fluoroquinolone antibiotic agent widely used for veterinary purposes. , ENR inhibits the main enzymes of the microbial cell, deoxyribonucleic acid (DNA) gyrase, in a selective manner (type II topoisomerase) and DNA topoisomerase IV, thus killing bacteria. , ENR can also treat urinary tract infections, respiratory tract infections, intestine tract infections, and skin and tissue infections in poultry, pigs, and cattle . Furthermore, ENR can treat bacterial diseases and mycoplasma infections in aquaculture. , ENR easily dissolves in methylene chloride, sodium hydroxide solution, and acetonitrile; is slightly soluble in methanol; and is poorly soluble in water.…”

Fabrication of PVC Enrofloxacin-Selective Electrodes for Estimating Enrofloxacin in Pure Form and as Preparation Formula

“…1 shows the chemical structure of enrofloxacin. The literature has revealed several logical strategies for quantitative assessment of enrofloxacin by spectrophotometry [7][8][9] , HPLC 10,11 , fluorescence 12,13 , and electrochemical technique 14 . The aim of this study is to foster an original particle-specific terminal method to determine enrofloxacin ionselective electrodes in drug measurement.…”