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Acta Pharmaceutica, Vol. 70 No. 4, 2020.

Original scientific paper

https://doi.org/10.2478/acph-2020-0041

Synthesis and evaluation of bisulfate/mesylate-conjugated chlortetracycline with high solubility and bioavailability

DENG LIU orcid id orcid.org/0000-0002-1671-7706 ; Key Laboratory of Biorheological Science and Technology, Ministry of Education, Bioengineering College, Chongqing University, Chongqing, 400044, People’s Republic of China
PEIXING CHEN orcid id orcid.org/0000-0002-1671-7706 ; Key Laboratory of Biorheological Science and Technology, Ministry of Education, Bioengineering College, Chongqing University, Chongqing, 400044, People’s Republic of China
XU YANG ; Key Laboratory of Biorheological Science and Technology, Ministry of Education, Bioengineering College, Chongqing University, Chongqing, 400044, People’s Republic of China
JIANHUA WANG orcid id orcid.org/0000-0002-9188-6382 ; Key Laboratory of Biorheological Science and Technology, Ministry of Education, Bioengineering College, Chongqing University, Chongqing, 400044, People’s Republic of China

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Abstract

The aim of this work is to improve the solubility and bioavailability of chlortetracycline and the function of the immune response. Chlortetracycline bisulfate and chlortetracycline mesylate were successfully synthesized and characterized with several techniques, including spectroscopy, chromatography and mass spectrometry, which demonstrated that the C4-dimethylamino group of chlortetracycline can accept a proton from sulfuric acid and methanesulfonic acid to form the corresponding salts. In addition, chlortetracycline bisulfate and chlortetracycline mesylate were more soluble in water than chlortetracycline hydrochloride, but the antibacterial activity was not enhanced. The influences of chlortetracycline hydrochloride, chlortetracycline bisulfate and chlortetracycline mesylate on chlortetracycline and immunoglobulin concentrations in mouse serum were also investigated. These results suggested that the chlortetracycline bisulfate and chlortetracycline mesylate have good bioavailability and strong immune response and have potential applications in animal breeding and formulation technologies.

Keywords

chlortetracycline; pharmaceutical salt; solubility; bioavailability; antibacterial activity; immunoglobulin

Hrčak ID:

234973

URI

https://hrcak.srce.hr/234973

Publication date:

31.12.2020.

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