CHARACTERIZATION OF POLYMORPHS AND SOLVATES OF 3-AMINO-1-(META-TRIFLUOROMETHYLPHENYL)-6-METHYL-1H-PYRIDAZIN-4-ONE

被引:12
作者
CHAUVET, A
MASSE, J
RIBET, JP
BIGG, D
AUTIN, JM
MAUREL, JL
PATOISEAU, JF
JAUD, J
机构
[1] CTR RECH PIERRE FABRE MED,DEPT RECH CHIM,17 AVE JEAN MOULIN,F-81106 CASTRES,FRANCE
[2] FAC PHARM MONTPELLIER,CHIM GEN & MINERALE LAB,F-34100 MONTPELLIER,FRANCE
[3] CTR ELABORAT MAT & ETUDES STRUCT,OPT ELECTR LAB,CNRS,F-31055 TOULOUSE,FRANCE
关键词
D O I
10.1002/jps.2600810824
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The characterization of two polymorphs of the title compound (F2692; 1) by differential scanning calorimetry (DSC), microanalysis, proton nuclear magnetic resonance spectroscopy, thermogravimetry, thermomicroscopy, infrared spectroscopy, and X-ray diffractometry is described. Both polymorphs are crystalline, with form II being more stable at temperatures <160-degrees-C. The thermal behavior was studied at different rates of heating, and the enthalpies of transition were calculated from DSC data. The transformation of aqueous suspensions of form I to the water-stable form II is described, and the heats of solution and intrinsic aqueous dissolution rates of both polymorphs were determined. 1 also formed solvates with dimethyl sulfoxide and 1-methyl-2-pyrrolidinone. The solvates were studied by thermogravimetry, DSC, and infrared spectroscopy.
引用
收藏
页码:836 / 841
页数:6
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