新型左氧氟沙星盐型共晶的设计与组装及性质分析

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[中图分类号］R944 ［文献标志码］A [文章编号] 2096-5532（2025）04-0483-06

doi：10.11712/jms.2096-5532.2025.61.069

[Abstract]ObjectiveToprepareacocrystalof theantimicrobial drug levofloxacin（LEF）and thephenolicacid compound galic acid（GA）forimproving physicochemical propertiesandantimicrobialperformanceMethodsThesolid-statemilingand solutionmethods wereused topreparetheLEF-GAcocrystal，andthetechniquessuchassinglecrystal/powder X-raydiraction， Fouriertransforminfrared spectroscopy，anddiferentialscaningcalorimetrywereusedforcharacterization；theHirsfeldsurface analysis wasusedtoperformtheoreticalcalculationsonintermolecularinteractions；theFranzdifusioncellmethodwasused toinvestigatethepermeationbehaviorofthecocrystal，andthediscdiffusionmethodwasusedtoinvestigateantimicrobialactivity. ResultsTheformationof thecocrystal wasdeterminedasanewsolid phase，andits precisecrystal structure wascharacterizedas a saltcocrystalwithbothcharge-asistant hydrogenbondsandclasscal neutralhydrogenbonds.The strong interactionintheco crystal lattice decreased from 83.0% of LEF to 75.4% ，permeation flux was increased by 2.52 times compared with LEF，and cumulativediffusionwasincreasedby1.99timescomparedwithLEF.Inaddition，thecocrystalhadbeterantimicrobialactivities than LEFagainst both Escherichia coli and Staphylococus aureus.ConclusionThis study prepares the salt cocrystalofLEF for the first time and achieves the enhancement in the permeability and antimicrobial effect of LEF.

[Keywords] levofloxacin；gallic acid；permeability；anti-bacterial agents

全球每年有上千万人死于细菌感染[1]。（剩余9360字）