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3-氨基-1-(间三氟甲基苯基)-6-甲基-1H-哒嗪-4-酮的多晶型物和溶剂化物的表征

Characterization of polymorphs and solvates of 3-amino-1-(m-trifluoromethylphenyl)-6-methyl-1H-pyridazin-4-one.

作者信息

Chauvet A, Masse J, Ribet J P, Bigg D, Autin J M, Maurel J L, Patoiseau J F, Jaud J

机构信息

Laboratoire de Chimie Générale et Minérale, Faculté de Pharmacie, Montpellier, France.

出版信息

J Pharm Sci. 1992 Aug;81(8):836-41. doi: 10.1002/jps.2600810824.

DOI:10.1002/jps.2600810824
PMID:1357154
Abstract

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 less than 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.

摘要

描述了通过差示扫描量热法(DSC)、微量分析、质子核磁共振光谱、热重分析、热显微镜、红外光谱和X射线衍射法对标题化合物(F2692;1)的两种多晶型物进行的表征。两种多晶型物均为晶体,在温度低于160℃时,II型更稳定。在不同加热速率下研究了热行为,并根据DSC数据计算了转变焓。描述了I型水悬浮液向水稳定的II型的转变,并测定了两种多晶型物的溶解热和固有水溶解速率。1还与二甲基亚砜和1-甲基-2-吡咯烷酮形成溶剂化物。通过热重分析、DSC和红外光谱对溶剂化物进行了研究。

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