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Preparation, characterization, transformation and solubility of imatinib-oxalate salt polymorphs
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Zheng-yu FANG, Cheng XING, Wen-hui XING, Xue WANG, Ning-bo GONG*, Yang LÜ
Acta Pharmaceutica Sinica | 2021, 56(11) : 3153 - 3158
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Acta Pharmaceutica Sinica | 2021, 56(11): 3153-3158
• Original Articles •
Preparation, characterization, transformation and solubility of imatinib-oxalate salt polymorphs
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Zheng-yu FANG, Cheng XING, Wen-hui XING, Xue WANG, Ning-bo GONG*, Yang LÜ
Affiliations
  • Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2021-11-12 doi: 10.16438/j.0513-4870.2021-1026
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The three polymorphs (Ⅰ, Ⅱ, Ⅲ) and one amorphous (Ⅳ) form of imatinib-oxalate new salt were prepared and characterized by powder X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis and infrared spectroscopy, and transformation rules among the four salts were analyzed. The solubility of polymorph Ⅱ was investigated by high performance liquid chromatography. The results show that polymorph Ⅱ was stable but polymorph Ⅰ, Ⅲ and amorphous Ⅳ were unstable at room temperature. Polymorph I transformed into polymorph Ⅱ at room temperature. At relative humidity 90%, polymorph Ⅰ, Ⅱ and amorphous Ⅳ transformed into polymorph Ⅲ, but polymorph Ⅲ transformed into amorphous Ⅳ at 70 ℃. The solubility of imatinib was significantly improved after being salted with oxalic acid, and the equilibrium solubility of polymorph Ⅱ in pH 6.8 buffer solution and pure water was increased by 4.1 and 21.2 fold, respectively, as compared to bulk drug. This research provides guidance for the development and quality control of a new salt form of imatinib.

imatinib  /  salt  /  characterization  /  transformation  /  solubility
Zheng-yu FANG, Cheng XING, Wen-hui XING, Xue WANG, Ning-bo GONG, Yang LÜ. Preparation, characterization, transformation and solubility of imatinib-oxalate salt polymorphs[J]. Acta Pharmaceutica Sinica, 2021 , 56 (11) : 3153 -3158 . DOI: 10.16438/j.0513-4870.2021-1026
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doi: 10.16438/j.0513-4870.2021-1026
  • Receive Date：2021-07-10
  • Online Date：2025-12-18
  • Published：2021-11-12
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  • Received：2021-07-10
  • Revised：2021-08-13
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    Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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