Synthesis, Characterization, and Pharmacodynamics Study of Enrofloxacin Mesylate

Drug Design, Development and Therapy
Lin-Lin PeiHua-Lin Fu

Abstract

Enrofloxacin is used in the treatment of a wide variety of bacterial infections in mammals. However, its poor solubility limits the clinical use. 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. 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 (LD50) 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 ...Continue Reading

References

Aug 1, 1997·Journal of Pharmaceutical and Biomedical Analysis·M LizondoJ Estelrich
May 27, 2014·International Journal of Pharmaceutics·G Prem KumarD B Raju
Jul 9, 2016·Langmuir : the ACS Journal of Surfaces and Colloids·Ashish K SarkerR Stephen Brown
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Nov 6, 2017·International Journal of Pharmaceutics·Wenqi WuHolger Grohganz
Sep 25, 2019·Materials Science & Engineering. C, Materials for Biological Applications·Xinnuo XiongHui Li

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Methods Mentioned

BETA
nuclear
X-ray
nuclear magnetic resonance
NMR

Software Mentioned

SPSS
SPSS19
DAS

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