文章基本信息

标题：Preparation, characterization and antimicrobial assessment of selected ciprofloxacin salts
本地全文：下载
作者：Imad I. Hamdan ; Dina El-Sabawi ; Rula Darwish 等
期刊名称：Acta Pharmaceutica
电子版ISSN：1846-9558
出版年度：2021
卷号：71
期号：3
页码：365-382
DOI：10.2478/acph-2021-0028
语种：English
出版社：Sciendo
摘要：The formation of salts is considered a simple strategy to modify the physicochemical properties of active pharmaceutical ingredients. In this study, seven novel binary and ternary organic salts of ciprofloxacin (CP) were prepared with benzoic acid (BA), acetylsalicylic acid (ASA),p-coumaric acid (PCMA) andp-aminosalicylic acid (PASA). They were characterized by spectroscopic techniques and differential scanning calorimetry. Solubility and partition coefficients values were also measured. Evaluation of the antimicrobial activity of the organic salts againstStaphylococcus aureusandStaphylococcus epidermidisrevealed that most of the new salts had higher antimicrobial activity than CPHCl against both strains. The most active compounds againstS. epidermidisandS. aureuswere CP-PASA and CPPCMA, resp., which were up to fourteen times more potent than parent CP-HCl. Our findings indicated a strong correlation between the lipophilicity of the formed salts and their antimicrobial activity and showed that an optimum value of lipophilicity (logP= 0.75) seemed to be necessary to maximize the antimicrobial activity. These findings highlighted the improved physical, thermal and antimicrobial properties of the new salts of CP that can aid in providing higher bioavailability than CP-HCl.