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甲磺酸恩诺沙星的合成、表征及药效学研究。

Synthesis, Characterization, and Pharmacodynamics Study of Enrofloxacin Mesylate.

机构信息

Department of Pharmacy, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, Sichuan, People's Republic of China.

College of Pharmacy, Southwest Minzu University, Chengdu, Sichuan, People's Republic of China.

出版信息

Drug Des Devel Ther. 2020 Feb 24;14:715-730. doi: 10.2147/DDDT.S239307. eCollection 2020.

DOI:10.2147/DDDT.S239307
PMID:32158191
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7047841/
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) 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.

摘要

简介

恩诺沙星被广泛用于治疗哺乳动物的多种细菌性感染。但是，其较差的水溶性限制了其临床应用。

方法

为了提高恩诺沙星的水溶性，采用化学合成法得到恩诺沙星甲磺酸酯（EM）。采用紫外扫描（UV）、同步热分析（SDT）、傅里叶变换红外光谱（FTIR）和质谱（MS）、核磁共振（NMR）和X 射线粉末衍射分析（XRPD）对 EM 进行了表征。研究了 EM 对昆明小鼠的急性毒性。此外，在新西兰兔单次口服 10mg/kg 剂量下进行了药代动力学研究，并评价了 EM 的抗菌活性。

结果

成功合成并纯化了 EM。甲磺酸酯与恩诺沙星的摩尔比为 1:1，EM 的水溶解度为 483.01±4.06mg/mL，EM 的溶解度约为恩诺沙星的 2000 倍。EM 的口服半数致死量（LD）为 1168.364mg/kg，药代动力学研究表明，EM 的口服相对生物利用度分别约为恩诺沙星和恩诺沙星盐酸盐的 1.79 倍和 1.48 倍。此外，EM 的体外抗菌活性与恩诺沙星和恩诺沙星盐酸盐相比没有明显变化。

结论

EM 具有更高的水溶性、低口服毒性和增加兔体内的口服生物利用度。这项研究可能有助于开发新的恩诺沙星药物。

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