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Improving the Membrane Permeability of 5-Fluorouracil via Cocrystallization

机译：通过共结晶提高5-氟尿嘧啶的膜渗透性

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摘要

Pharmaceutical cocrystallization is proposed as a new method to enhance membrane permeability of a BCS class III model drug, 5-fluorouracil (5FU). Three cocrystals of 5FU, 5FU/3-hydroxybenzoic acid (1), 5FU/4-aminobenzoic acid (2), and 5FU/cinnamic acid (3), were successfully synthesized by a slurry method or a liquid-assisted grinding process. Spectroscopic methods, thermal analysis, and X-ray diffraction were used to characterize these new forms. The permeability was studied using a Franz diffusion cell and silicone membrane. All of the cocrystals showed improved membrane permeability compared to free 5FU. The cumulative amount per unit area of permeated 5FU in the first 10 h for 1-3 was increased by 41, 70, and 83%, and the steady penetration rates of 1-3 were increased by 38, 66, and 79%, respectively, as compared to the pure drug. Structure permeability correlation study finds a link between intermolecular interactions and molecular packing in cocrystals and their permeability behavior and has important implications for use of a cocrystallization approach to improve drugs' permeability in the pharmaceutical field.
机译：提出将药物共结晶作为提高BCS III类模型药物5-氟尿嘧啶（5FU）的膜通透性的新方法。通过淤浆法或液体辅助研磨法成功合成了5FU，5FU / 3-羟基苯甲酸（1），5FU / 4-氨基苯甲酸（2）和5FU /肉桂酸（3）的三个共晶体。光谱方法，热分析和X射线衍射被用来表征这些新形式。使用Franz扩散池和硅树脂膜研究渗透率。与游离5FU相比，所有共结晶均显示出改善的膜渗透性。 1-3的前10 h渗透5FU的单位面积累积量分别增加41％，70％和83％，稳定渗透率1-3分别增加38％，66％和79％ ，与纯药物相比。结构渗透性相关性研究发现了共晶中的分子间相互作用和分子堆积与渗透性之间的联系，对于在制药领域使用共结晶方法改善药物的渗透性具有重要意义。

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