Grinding effect on levofloxacin hemihydrate

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• 作者：Rafael Nicolay Pereira (1)
  Cinira Fandaruff (1)
  Manoela Kl眉ppel Riekes (1)
  Gustavo A. Monti (3)
  Carlos Eduardo Maduro de Campos (2)
  Silvia Lucia Cuffini (1) (4)
  Marcos Antonio Segatto Silva (1)
  
  1. PGFAR ; University Federal of Santa Catarina ; Florian贸polis ; SC ; 88040-970 ; Brazil
  3. Faculty of Mathematics ; Astronomy and Physics (FAMAF) ; University National of C贸rdoba ; C贸rdoba ; Argentina
  2. University Federal of Santa Catarina ; Florian贸polis ; SC ; 88040-970 ; Brazil
  4. Instituto de Ci锚ncia e Tecnologia ; Universidade Federal de S茫o Paulo ; S茫o Paulo ; Brazil
  
• 关键词：Levofloxacin ; Hemihydrate ; Grinding ; Rehydration
• 刊名：Journal of Thermal Analysis and Calorimetry
• 出版年：2015
• 出版时间：February 2015
• 年：2015
• 卷：119
• 期：2
• 页码：989-994
• 全文大小：1,024 KB
• 参考文献：1. Bernstein J. Polymorphism in molecular crystals. 14th ed. Oxford: IUCr, Oxford; 2013.
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  5. Brittain HG. Polymorphism in pharmaceutical solids. In: Morris KR, editor. Structural aspects of hydrates and solvates. Milford: Discovery Laboratories, Inc; 2006.
  6. Nelson JM, Chiller TM, Powers JH, Angulo FJ. Fluoroquinolone-resistant / Campylobacter species and the withdrawal of fluoroquinolones from use in poultry: a public health success story. Clin Infect Dis. 2007;7:977鈥?0. CrossRef
  7. Kitaoka H, Wada C, Moroi R, Hakusui H. Effect of dehydration on the formation of levofloxacin pseudopolymorphs. Chem Pharm Bull. 1995;43(4):649鈥?3. CrossRef
  8. Reddy MS, Eswaraiah S, Reddy KR, Reddy SR, Prakash PJ. Novel anhydrous crystalline form of levofloxacin and process for preparation there of levofloxacin. United States Patent Application Publication, US 2004/0152701 A1, 2004.
  
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Chemistry
  Sciences
  Polymer Sciences
  Physical Chemistry
  Inorganic Chemistry
  Measurement Science and Instrumentation
  
• 出版者：Akad茅miai Kiad贸, co-published with Springer Science+Business Media B.V., Formerly Kluwer Academic
• ISSN：1572-8943

文摘

The grinding techniques were used in different pharmacotechnical process. The control of the effect of grinding in solid state properties of drugs is very important, mainly in hydrated drugs. Levofloxacin hemihydrate (LVF) is a good example of this type of compounds and a broad spectrum antibiotic of the fluoroquinolone drug class. The samples of LVF with and without grinding were studied using different characterization techniques such as thermogravimetry, differential scanning calorimetry, fourier-transformed infrared, X-ray powder diffraction, and hot stage microscopy. The purpose of the present study was to evaluate the effects of grinding in the dehydration and rehydration processes in levofloxacin hemihydrate. After heating, the samples lost water molecules and the rehydration process was modified depending on defects due to the grinding. At room temperature, the complete transformation to the hemihydrate form was detected only for the sample without grinding. On the other hand, the milled sample showed two phases, hydrate and anhydrate forms. Therefore, the defects in the crystalline structure would cause the irreversible transformation.