Home Journals Articles Updates About
CN
image
收藏切换
Preparation, characterization, transformation and solubility of imatinib-oxalate salt polymorphs
收藏切换
PDF
Zheng-yu FANG, Cheng XING, Wen-hui XING, Xue WANG, Ning-bo GONG*, Yang LÜ
Acta Pharmaceutica Sinica | 2021, 56(11) : 3153 - 3158
Less
收藏切换
Acta Pharmaceutica Sinica | 2021, 56(11): 3153-3158
• Original Articles •
Preparation, characterization, transformation and solubility of imatinib-oxalate salt polymorphs
Full
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
Outline
收藏切换

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
Appendix
Less
Year 2021 volume 56 Issue 11
PDF
173
64
Cite this Article
BibTeX
Article Info
doi: 10.16438/j.0513-4870.2021-1026
  • Receive Date：2021-07-10
  • Online Date：2025-12-18
  • Published：2021-11-12
Article Data
Affiliations
History
  • Received：2021-07-10
  • Revised：2021-08-13
Funding
Affiliations
    Beijing Key Laboratory of Polymorphic Drugs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
References
Share
https://castjournals.cast.org.cn/joweb/yxxb/EN/10.16438/j.0513-4870.2021-1026
Share to
QR

Scan QR to access full text

Cite this article
BibTeX
Citations
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
关闭全屏
  • BibTeX
  • EndNote
  • RefWorks
  • TxT
Links
Articles
Latest Articles
Most Read
Collections
Updates
Events
News
Multimedia
About
About Us
Contact
No. 86 Xueyuan South Road, Haidian District, Beijing
100081
010-62199257
qkjq@cast.org.cn

Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House