Characterisation of organic solid forms and real-time in situ monitoring of their transformations using solid-state fluorescence

被引:28
作者
Frenette, Mathieu [1 ]
Cosa, Gonzalo [1 ]
Friscic, Tomislav [1 ]
机构
[1] McGill Univ, Dept Chem, Montreal, PQ H3A 0B8, Canada
基金
加拿大自然科学与工程研究理事会; 加拿大创新基金会;
关键词
STRUCTURAL-CHARACTERIZATION; PHARMACEUTICAL COCRYSTALS; INDOMETHACIN POLYMORPHS; AMORPHOUS STATE; AVRAMI-EQUATION; CO-CRYSTALS; CRYSTALLIZATION; KINETICS; SPECTROSCOPY; DRUG;
D O I
10.1039/c3ce40604k
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
We demonstrate the application of solid-state fluorescence spectroscopy for the real-time monitoring and characterisation of solid forms (e.g. polymorphs, solvates, cocrystals) of pharmaceutical molecules. This proof-of-principle study focuses on the pharmaceutical indomethacin which, although poorly fluorescent in solution, in the solid state yields highly fluorescent amorphous, polymorphic, solvate and cocrystal forms. We show that solid forms of indomethacin can be readily distinguished by their fluorescent properties and, by using a simple and readily available experimental set-up, we reveal that fluorescence spectroscopy can be used to quantify amorphous and crystalline forms in a mixture and to monitor the kinetics of their interconversion in situ and in real-time (30 seconds resolution or less).
引用
收藏
页码:5100 / 5106
页数:7
相关论文
共 68 条
[1]   Solubility Behavior and Solution Chemistry of Indomethacin Cocrystals in Organic Solvents [J].
Alhalaweh, Amjad ;
Sokolowski, Anders ;
Rodriguez-Hornedo, Nair ;
Velaga, Sitaram P. .
CRYSTAL GROWTH & DESIGN, 2011, 11 (09) :3923-3929
[2]   Kinetics of phase change I - General theory [J].
Avrami, M .
JOURNAL OF CHEMICAL PHYSICS, 1939, 7 (12) :1103-1112
[3]  
Avrami M., 1940, J CHEM PHYS, V8, P212, DOI DOI 10.1063/1.1750631
[4]  
Balch A. L., 2009, ANGEW CHEM INT EDIT, V48, P2
[5]   Indomethacin-saccharin cocrystal:: Design, synthesis and preliminary pharmaceutical characterization [J].
Basavoju, Srinivas ;
Bostrom, Dan ;
Velaga, Sitaram P. .
PHARMACEUTICAL RESEARCH, 2008, 25 (03) :530-541
[6]   Combining piracetam and lithium salts: ionic co-crystals and co-drugs? [J].
Braga, Dario ;
Grepioni, Fabrizia ;
Maini, Lucia ;
Capucci, Davide ;
Nanna, Saverio ;
Wouters, Johan ;
Aerts, Luc ;
Quere, Luc .
CHEMICAL COMMUNICATIONS, 2012, 48 (66) :8219-8221
[7]   The Prout-Tompkins rate equation in solid-state kinetics [J].
Brown, ME .
THERMOCHIMICA ACTA, 1997, 300 (1-2) :93-106
[8]  
Bucar D.-K., 2007, CHEM COMMUN, P525
[9]  
Bucar D.-K., 2009, CRYST GROWTH DES, V9, P1932
[10]   Lattice model for kinetics and grain-size distribution in crystallization [J].
Castro, M ;
Sánchez, A ;
Domínguez-Adame, F .
PHYSICAL REVIEW B, 2000, 61 (10) :6579-6586