Polymorphism and desolvation of flupirtine maleate

被引:13
作者
Landgraf, KF [1 ]
Olbrich, A [1 ]
Pauluhn, S [1 ]
Emig, P [1 ]
Kutscher, B [1 ]
Stange, H [1 ]
机构
[1] ASTA Med AG, Dresden, Germany
关键词
flupirtine maleate; polymorphism; modification; desolvation; X-ray diffractometry; polarization microscopy; thermoanalysis;
D O I
10.1016/S0939-6411(98)00054-X
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
Crystallizates of the analgesic agent flupirtine maleate (Katadolon(R); ASTA Medica, Dresden, Germany) obtained from isopropanol are examined by X-ray diffractometry, polarization microscopy and thermoanalysis. Depending on the crystallizing conditions, the modifications A and B as well as an isopropanol solvate are observed. The inversion temperature A --> B of the enantiotropic modifications is 164 degrees C (differential scanning calorimetry (DSC) onset). During thermal desolvation, modification B is formed well below the inversion temperature. In concentrated isopropanol suspensions, the solvate and modification B are rapidly transformed into modification A. It is shown bow phase-pure products consisting of modification A, which is better wettable with water and stable at room temperature, can be obtained. (C) 1998 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:329 / 337
页数:9
相关论文
共 2 条
[1]
Meyer K., 1968, PHYSIKALISCH CHEMISC
[2]
von Bebenburg W., 1989, DE patent, Patent No. 3133519