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首页> 外文期刊>Crystal growth & design >Sparfloxacin Multicomponent Crystals: Targeting the Solubility of Problematic Antibiotics
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Sparfloxacin Multicomponent Crystals: Targeting the Solubility of Problematic Antibiotics

机译：Sparfloxacin多组分晶体：靶向有问题的抗生素的溶解度

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摘要

The design of novel pharmaceutical multicomponent crystal forms has been reported as an efficient approach to tailor their physicochemical properties, including solubility. Sparfloxacin is a fluoroquinolone antibiotic widely used mainly in respiratory tract infections, but its safety profile is controversial due to photosensitivity reactions, and therefore the development of alternative forms that may contribute to the intake of lower dosages is desirable. Herein we report five novel molecular salts of sparfloxacin with generally regarded as safe coformers. All of the compounds present the typical S 1) 1)(6) intramolecular synthon in SPAR molecules, and a direct interaction between SPAR~(+) and the anionic coformers is also verified. Only salts 2 and 5 present a C 1) 1)(8) chain due to the direct interaction of SPAR molecules via N–H_(NH2,SPAR)···O_(COOH,SPAR). The new forms have been fully characterized, presenting adequate RH and temperature stability; more importantly, they are more soluble in water than sparfloxacin itself. The observed improvement in the physicochemical properties, in particular the 1 order higher aqueous solubility of the citrate salt, may contribute positively to obtain a better safety profile of the drug, as lower dosages may be possible.
机译：据报道，新型药物多组分晶型的设计是调整其物理化学性质（包括溶解度）的有效方法。司帕沙星是一种主要用于呼吸道感染的氟喹诺酮类抗生素，但由于光敏反应，其安全性存在争议，因此，开发有助于低剂量摄入的替代形式是可取的。在此，我们报告了五种新的司帕沙星分子盐，它们通常被认为是安全的共形物。所有化合物在SPAR分子中都呈现典型的s1）1）（6）分子内合成子，并且SPAR~（+）与阴离子共形物之间存在直接相互作用。由于SPAR分子通过N–H_（NH2，SPAR）·O_（COOH，SPAR）直接相互作用，只有2和5的盐呈现出C 1）（8）链。新形式已被充分表征，呈现出足够的相对湿度和温度稳定性；更重要的是，它们比司帕沙星本身更易溶于水。所观察到的物理化学性质的改善，尤其是柠檬酸盐的水溶性提高了1个数量级，可能有助于获得更好的药物安全性，因为较低的剂量可能是可能的。

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  • 来源
    《Crystal growth & design》 |2021年第2期|共11页
  • 作者

    Mariama Djaló; Andreia E. S. Cunha; Jo?o P. Luís; Sílvia Quaresma; Auguste Fernandes; Vania André; M. Teresa Duarte;

  • 作者单位

    Centro de Química Estrutural Instituto Superior Técnico Universidade de Lisboa Av. Rovisco Pais;

    Centro de Química Estrutural Instituto Superior Técnico Universidade de Lisboa Av. Rovisco Pais;

    Centro de Química Estrutural Instituto Superior Técnico Universidade de Lisboa Av. Rovisco Pais;

    Centro de Química Estrutural Instituto Superior Técnico Universidade de Lisboa Av. Rovisco Pais;

    Centro de Química Estrutural Instituto Superior Técnico Universidade de Lisboa Av. Rovisco Pais;

    Centro de Química Estrutural Instituto Superior Técnico Universidade de Lisboa Av. Rovisco Pais;

    Centro de Química Estrutural Instituto Superior Técnico Universidade de Lisboa Av. Rovisco Pais;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 晶体学;
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