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The effect of solvent on crystal transformation process of prasugrel hydrogen sulfate and its mechanism
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Min LU1, Yue GONG1, Wei DU1, Xue-kui WANG1, Na TANG1, Qiu-xiang YIN2
Chinese Journal of New Drugs | 2021, 30(17) : 1616 - 1620
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Chinese Journal of New Drugs | 2021, 30(17): 1616-1620
The effect of solvent on crystal transformation process of prasugrel hydrogen sulfate and its mechanism
Full
Min LU1, Yue GONG1, Wei DU1, Xue-kui WANG1, Na TANG1, Qiu-xiang YIN2
Affiliations
  • 1Tianjin University of Science and Technology, College of Chemical Engineering and Materials Science, Tianjin 300457, China
  • 2School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China
Published: 2021-09-15
Outline
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Objective:

To determine the stable relationship of the polymorph system of prasugrel hydrogen sulfate, to clarify the influence rule of solvent on the polymorph nucleation of prasugrel hydrogen sulfate, and to reveal the crystal transformation mechanism of prasugrel hydrogen sulfate.

Methods:

In this study, crystal forms Ⅰ and Ⅱ of prasugrel hydrogen sulfate were selected as the research subjects, focusing on their solvent-mediated transcrystallisation proces, the off-line monitoring of the crystal form composition of suspended solid phase and the change of the solution concentration with time during the crystallization process. The influence mechanism of solvent on the crystal transformation process was also revealed.

Results:

Solvent-mediated crystallization of Prasugrel hydrogen sulfate form Ⅰ to form Ⅱ was monitored by X-ray diffraction, the results of which indicated that the rate-determining step during this process was the nucleation and growth of the prasugrel hydrogen sulfate form Ⅱ.

Conclusion:

Consider the crystal transformation rate of prasugrel hydrogen sulfate in three solvents, including butanone, MIK and methyl acetate, and the solubility relationship of crystal form Ⅱ in them, it can be concluded that the nucleation process of prasugrel hydrogen sulfate form Ⅱ is affected not only by solubility, but also by the strength of hydrogen bond between the molecules.

prasugrel hydrogen sulfate  /  polymorphs  /  solvent-mediated polymorphic transformation  /  X-ray diffraction  /  nucleation and growth
卢敏, 宫月, 杜威, 王学魁, 唐娜, 尹秋响. 溶剂对普拉格雷硫酸氢盐晶型转变过程的影响机制. 中国新药杂志, 2021 , 30 (17) : 1616 -1620 .
Min LU, Yue GONG, Wei DU, Xue-kui WANG, Na TANG, Qiu-xiang YIN. The effect of solvent on crystal transformation process of prasugrel hydrogen sulfate and its mechanism[J]. Chinese Journal of New Drugs, 2021 , 30 (17) : 1616 -1620 .
Year 2021 volume 30 Issue 17
40
6
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  • Online Date:2026-10-28
  • Published:2021-09-15
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  • Accepted:2021-05-07
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    1Tianjin University of Science and Technology, College of Chemical Engineering and Materials Science, Tianjin 300457, China
    2School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, 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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