氧氟沙星在金属阳离子存在下的水溶性

C. Eboka, H. Okeri
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引用次数: 0

摘要

氧氟沙星属于氟喹诺酮类药物,已被广泛用于治疗对其他抗生素具有耐药性的微生物感染。然而,金属阳离子和抗酸剂对氧氟沙星的生物利用度和抗菌活性有不利影响。人们提出了许多原因来解释观察到的影响。为了进一步了解氧氟沙星-金属阳离子相互作用如何影响氧氟沙星的可用性和活性,本研究采用分光光度法研究了氧氟沙星在金属阳离子存在下的水溶性。所研究的所有阳离子都不同程度地提高氧氟沙星的水溶性。硫酸亚铁使氧氟沙星的溶解度增加最多。其次是柠檬酸铁铵、硫酸镁、氢氧化铝和碳酸钙。氯化钾和碳酸氢钠产生了非常轻微的增加。在所有情况下,氧氟沙星的溶解度随着每种金属阳离子量的增加而增加。观察到的结果可归因于形成可溶性离子羧酸氧氟沙星盐和金属阳离子的配合物。讨论了金属阳离子存在下氧氟沙星水溶性的提高对氧氟沙星生物利用度和抗菌活性的影响。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The aqueous solubility of ofloxacin in the presence of metallic cations
Ofloxacin belongs to the class of fluoroquinolones which has found widespread use in the treatment of microbial infections resistant to  other antibiotics. However, metallic cations and anti-acids have been found to adversely affect the bioavailability and antibacterial activity of ofloxacin. Many reasons have been suggested to explain the observed effects. In order to gain further understanding of how ofloxacin-metallic cation interaction affects ofloxacin availability and activity, the aqueous solubility of ofloxacin was investigated in the presence of some metallic cations spectrophometrically in this study. All the cations investigated increased the aqueous solubility of ofloxacin to varying extents. Ferrous sulphate produced the greatest increase in the solubility of ofloxacin. It was followed by ferric ammonium citrate, magnesium sulphate, aluminium hydroxide and calcium carbonate. Potassium chloride and sodium bicarbonate produced very slight increases. In all the cases, the solubility of ofloxacin increased as the amount of each metallic cation increased. The observed results can be attributed to formation of soluble ionic ofloxacin carboxylate salts and complexes of the metallic cations. The implication of such increase of the aqueous solubility of ofloxacin in the presence of metallic cations on the bioavailability and antibacterial activity of ofloxacin is discussed.
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