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Preparation, characterization and improved solubility of ticagrelor salts
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Hong-mei YU, Zheng-yu FANG, Cheng XING, Kun HU, Ning-bo GONG*, Yang LU:
Acta Pharmaceutica Sinica | 2021, 56(2) : 570 - 576
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Acta Pharmaceutica Sinica | 2021, 56(2): 570-576
• Original Articles •
Preparation, characterization and improved solubility of ticagrelor salts
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Hong-mei YU, Zheng-yu FANG, Cheng XING, Kun HU, Ning-bo GONG*, Yang LU:
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: 2021-02-12 doi: 10.16438/j.0513-4870.2020-1470
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Four salts of ticagrelor, ticagrelor-3, 5-dinitrobenzoic acid, ticagrelor-pyrazinamide, ticagrelor-Dproline and ticagrelor-L-proline were prepared by solvent suspension and liquid-assisted grinding to improve the solubility of ticagrelor. The compounds were characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry, nuclear magnetic resonance spectroscopy, elemental analysis, and the intermolecular salt-bonding forces were analyzed. The equilibrium solubility of salts and pure drug in hydrochloride buffer pH 1.2 and phosphate buffer pH 6.8 were measured by high-performance liquid chromatography.Ticagrelor was salted with 3, 5-dinitrobenzoic acid, pyrazinamide, D-proline, L-proline all in a stoichiometric ratio of 1∶1; with the exception of ticagrelor-D-proline, the solubility of the other three salts provided significantly improved solubility in hydrochloride buffer pH 1.2, and the equilibrium solubility of ticagrelor-3, 5-dinitrobenzoic acid was increased by approximately 1.7 folds as compared to pure drug. Salt-forming technology is convenient and can improve the solubility of ticagrelor.

salt  /  ticagrelor  /  characterization  /  equilibrium solubility
Hong-mei YU, Zheng-yu FANG, Cheng XING, Kun HU, Ning-bo GONG, Yang LU:. Preparation, characterization and improved solubility of ticagrelor salts[J]. Acta Pharmaceutica Sinica, 2021 , 56 (2) : 570 -576 . DOI: 10.16438/j.0513-4870.2020-1470
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Article Info
doi: 10.16438/j.0513-4870.2020-1470
  • Receive Date：2020-09-09
  • Online Date：2025-12-18
  • Published：2021-02-12
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  • Received：2020-09-09
  • Revised：2020-12-04
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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
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Genus		 种数
Number of
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Percentage of total
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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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