globalchange  > 影响、适应和脆弱性
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
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