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增强 NSAIDs 在含环丙沙星药物制剂中的溶解度。

Enhanced NSAIDs Solubility in Drug-Drug Formulations with Ciprofloxacin.

机构信息

Laboratorio de Estudios Cristalográficos, IACT, CSIC-Universidad de Granada, Avda. de las Palmeras 4, 18100 Armilla, Spain.

Department of Inorganic Chemistry, Faculty of Pharmacy, University of Granada, 18071 Granada, Spain.

出版信息

Int J Mol Sci. 2023 Feb 7;24(4):3305. doi: 10.3390/ijms24043305.

Abstract

Drug-drug salts are a kind of pharmaceutical multicomponent solid in which the two co-existing components are active pharmaceutical ingredients (APIs) in their ionized forms. This novel approach has attracted great interest in the pharmaceutical industry since it not only allows concomitant formulations but also has proved potential to improve the pharmacokinetics of the involved APIs. This is especially interesting for those APIs that have relevant dose-dependent secondary effects, such as non-steroidal anti-inflammatory drugs (NSAIDs). In this work, six multidrug salts involving six different NSAIDs and the antibiotic ciprofloxacin are reported. The novel solids were synthesized using mechanochemical methods and comprehensively characterized in the solid state. Moreover, solubility and stability studies, as well as bacterial inhibition assays, were performed. Our results suggest that our drug-drug formulations enhanced the solubility of NSAIDs without affecting the antibiotic efficacy.

摘要

药物共晶盐是一种药物多组分固体,其中共存的两个成分是以离子形式存在的活性药物成分(APIs)。这种新方法引起了制药行业的极大兴趣,因为它不仅允许同时进行配方,而且还证明了改善所涉及 APIs 的药代动力学的潜力。对于那些具有相关剂量依赖性次要作用的 APIs 来说,这尤其有趣,例如非甾体抗炎药(NSAIDs)。在这项工作中,报道了涉及六种不同 NSAIDs 和抗生素环丙沙星的六种多药物共晶盐。新型固体使用机械化学方法合成,并在固态下进行了全面表征。此外,还进行了溶解度和稳定性研究以及细菌抑制测定。我们的结果表明,我们的药物共晶配方提高了 NSAIDs 的溶解度,而不影响抗生素的疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36d3/9964002/255a80d0a217/ijms-24-03305-sch001.jpg

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