Key Laboratory of Biorheological Science and Technology, Ministry of Education Bioengineering College, Chongqing University, Chongqing, 400044 People's Republic of China.
Acta Pharm. 2020 Dec 1;70(4):483-498. doi: 10.2478/acph-2020-0041.
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.
本工作旨在提高土霉素的溶解度和生物利用度，并增强其免疫应答功能。成功合成并通过多种技术（包括光谱学、色谱法和质谱法）对土霉素硫酸氢盐和土霉素甲磺酸盐进行了表征，结果表明土霉素 C4-二甲基氨基可从硫酸和甲磺酸接受质子，从而形成相应的盐。此外，土霉素硫酸氢盐和土霉素甲磺酸盐在水中的溶解度均高于盐酸土霉素，但抗菌活性并未增强。还研究了盐酸土霉素、土霉素硫酸氢盐和土霉素甲磺酸盐对小鼠血清中土霉素和免疫球蛋白浓度的影响。这些结果表明，土霉素硫酸氢盐和土霉素甲磺酸盐具有良好的生物利用度和较强的免疫应答能力，在动物养殖和制剂技术方面具有潜在的应用前景。
