دورية أكاديمية
Mechanochemically Induced Solid-State Transformations of Levofloxacin.
| العنوان: | Mechanochemically Induced Solid-State Transformations of Levofloxacin. |
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| المؤلفون: | Kadri L; School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, College Green, Dublin 2 D02 PN40, Ireland.; The Science Foundation Ireland Research Centre for Pharmaceuticals (SSPC), Limerick V94 T9PX, Ireland., Carta M; Department of Mechanical, Chemical and Materials Engineering, University of Cagliari, CSGI Research Unit, via Marengo 2, Cagliari 09123, Italy., Lampronti G; Department of Materials Science & Metallurgy, University of Cambridge, 27 Charles Babbage Road, Cambridge CB3 0FS, United Kingdom., Delogu F; Department of Mechanical, Chemical and Materials Engineering, University of Cagliari, CSGI Research Unit, via Marengo 2, Cagliari 09123, Italy., Tajber L; School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, College Green, Dublin 2 D02 PN40, Ireland.; The Science Foundation Ireland Research Centre for Pharmaceuticals (SSPC), Limerick V94 T9PX, Ireland. |
| المصدر: | Molecular pharmaceutics [Mol Pharm] 2024 Jun 03; Vol. 21 (6), pp. 2838-2853. Date of Electronic Publication: 2024 Apr 25. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 101197791 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1543-8392 (Electronic) Linking ISSN: 15438384 NLM ISO Abbreviation: Mol Pharm Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Washington, DC : American Chemical Society, c2004- |
| مواضيع طبية MeSH: | Levofloxacin*/chemistry , X-Ray Diffraction*/methods, Powders/chemistry ; Kinetics ; Drug Compounding/methods ; Anti-Bacterial Agents/chemistry ; Calorimetry, Differential Scanning/methods ; Crystallization ; Chemistry, Pharmaceutical/methods |
| مستخلص: | Levofloxacin hemihydrate (LVXh) is a complex fluoroquinolone drug that exists in both hydrated and anhydrous/dehydrated forms. Due to the complexity of such a compound, the primary aim of this study was to investigate the amorphization capabilities and solid-state transformations of LVXh when exposed to mechanical treatment using ball milling. Spray drying was utilized as a comparative method for investigating the capabilities of complete LVX amorphous (LVXam) formation. The solid states of the samples produced were comprehensively characterized by powder X-ray diffraction, thermal analysis, infrared spectroscopy, Rietveld method, and dynamic vapor sorption. The kinetics of the process and the quantification of phases at different time points were conducted by Rietveld refinement. The impact of the different mills, milling conditions, and parameters on the composition of the resulting powders was examined. A kinetic investigation of samples produced using both mills disclosed that it was in fact possible to partially amorphize LVXh upon mechanical treatment. It was discovered that LVXh first transformed to the anhydrous/dehydrated form γ (LVXγ), as an intermediate phase, before converting to LVXam. The mechanism of LVXam formation by ball milling was successfully revealed, and a new method of forming LVXγ and LVXam by mechanical forces was developed. Spray drying from water depicted that complete amorphization of LVXh was possible. The amorphous form of LVX had a glass transition temperature of 80 °C. The comparison of methods highlighted that the formation of LVXam is thus both mechanism- and process-dependent. Dynamic vapor sorption studies of both LVXam samples showed comparable stability properties and crystallized to the most stable hemihydrate form upon analysis. In summary, this work contributed to the detailed understanding of solid-state transformations of essential fluoroquinolones while employing greener and more sustainable manufacturing methods. |
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| فهرسة مساهمة: | Keywords: ball milling; fluoroquinolone; kinetics; levofloxacin; mechanochemistry; phase transformation; spray drying |
| المشرفين على المادة: | 6GNT3Y5LMF (Levofloxacin) 0 (Powders) 0 (Anti-Bacterial Agents) |
| تواريخ الأحداث: | Date Created: 20240425 Date Completed: 20240603 Latest Revision: 20240607 |
| رمز التحديث: | 20240607 |
| مُعرف محوري في PubMed: | PMC11151213 |
| DOI: | 10.1021/acs.molpharmaceut.4c00008 |
| PMID: | 38662637 |
| قاعدة البيانات: | MEDLINE |
Find this issue from the American Chemical Society | تدمد: | 1543-8392 |
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| DOI: | 10.1021/acs.molpharmaceut.4c00008 |