DOI: 10.1016/j.jcou.2015.11.006
Scopus记录号: 2-s2.0-84949604564
论文题名: Pharmaceutical co-crystals of the anti-inflammatory drug diflunisal and nicotinamide obtained using supercritical CO2 as an antisolvent
作者: Cuadra I.A. ; Cabañas A. ; Cheda J.A.R. ; Martínez-Casado F.J. ; Pando C.
刊名: Journal of CO2 Utilization
ISSN: 22129820
出版年: 2016
卷: 13 起始页码: 29
结束页码: 37
语种: 英语
英文关键词: Carbon dioxide
; Nicotinamide
; Pharmaceutical co-crystals
; Supercritical antisolvent diflunisal
Scopus关键词: Acetone
; Amides
; Carbon
; Carbon dioxide
; Carboxylic acids
; Cobalt
; Crystalline materials
; Drug products
; Environmental impact
; Grinding (machining)
; Negative impedance converters
; Organic solvents
; Supercritical fluid extraction
; Active pharmaceutical ingredients
; Anti-inflammatory drugs
; Co-crystals
; Diflunisal
; Nicotinamide
; Physicochemical property
; Solution crystallization
; Stoichiometric compositions
; Crystal structure
英文摘要: A method based on using supercritical CO2 as an antisolvent (SAS method) is explored as a co-crystallization technique. Co-crystallization is an emerging and powerful technique to improve the physicochemical properties of an active pharmaceutical ingredient. The solid-state and solution co-crystallization methods usually employed present several disadvantages. The one-step SAS method has a low environmental impact and overcomes some of the difficulties associated to conventional methods. The 2:1 co-crystals of the anti-inflammatory drug diflunisal (DIF) and nicotinamide (NIC) are prepared for the first time by SAS. Drug concentrations corresponding to the co-crystal stoichiometric composition are used. The influence of the SAS parameters temperature (35 and 40 °C), pressure (10.0 and 12.0 MPa), drug concentration (two levels) and solvent (acetone and ethanol) in the co-crystal formation is studied. A crystalline material in the form of needles of uniform width and more variable length is obtained. For comparison purposes, pure DIF and NIC are also processed by SAS. Co-crystals are characterized in terms of crystallinity, thermal behavior, coformer interactions and drug release; their dissolution rate improves with respect to that of pure DIF. SAS co-crystals exhibit the same crystal structure, melting point and FTIR spectrum as those previously obtained by liquid assisted ball mill grinding and solution crystallization. © 2015 Elsevier Ltd.
资助项目: Ministerio de Economía y Competitividad
; Ministerio de Economía y Competitividad
; Ministerio de Economía y Competitividad
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资源类型: 期刊论文
标识符: http://119.78.100.158/handle/2HF3EXSE/52929
Appears in Collections: 影响、适应和脆弱性
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Recommended Citation:
Cuadra I.A.,Cabañas A.,Cheda J.A.R.,et al. Pharmaceutical co-crystals of the anti-inflammatory drug diflunisal and nicotinamide obtained using supercritical CO2 as an antisolvent[J]. Journal of CO2 Utilization,2016-01-01,13