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Article

Impact of Crystal Habit on Solubility of Ticagrelor

Department of Chemistry, Zhejiang University, Hangzhou 310028, China
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Authors to whom correspondence should be addressed.
Crystals 2019, 9(11), 556; https://doi.org/10.3390/cryst9110556
Received: 17 September 2019 / Revised: 19 October 2019 / Accepted: 23 October 2019 / Published: 24 October 2019
(This article belongs to the Special Issue Pharmaceutical Crystals)
Drugs with poor biopharmaceutical performance are the main obstacle to the development and design of medicinal preparations. The anisotropic surface chemistry of different surfaces on the crystal influences its physical and chemical properties, such as solubility, tableting, etc. In this study, the antisolvent crystallization and rapid-cooling crystallization were carried out to tune the crystal habits of ticagrelor (TICA) form II. Different crystal habits of ticagrelor (TICA) form II (TICA-A, TICA-B, TICA-C, TICA-D, and TICA-E) were prepared and evaluated for solubility. The single-crystal diffraction (SXRD) indicated that TICA form II belongs to the triclinic P1 space group with four TICA molecules in the asymmetric unit. The TICA molecules are generated through intermolecular hydrogen bonds along the (010) direction, forming an infinite molecular chain, which are further stacked by hydrogen bonds between hydroxyethoxy side chains, forming molecular circles composed of six TICA molecules along bc directions. Thus, in the case of TICA form II, hydrogen bonds drive growth along one axis (b-axis), which results in the formation of mostly needle-shape crystals. Morphology and face indexation reveals that (001), (010) and (01-1) are the main crystal planes. Powder diffractions showed that five habits have the same crystal structure and different relative intensity of diffraction peak. The solubility of the obtained crystals showed the crystal habits affect their solubility. This work is helpful for studying the mechanism of crystal habit modification and its effect on solubility. View Full-Text
Keywords: ticagrelor; crystal structure; crystal habit; solubility; dissolution ticagrelor; crystal structure; crystal habit; solubility; dissolution
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MDPI and ACS Style

Ren, Y.; Shen, J.; Yu, K.; Phan, C.U.; Chen, G.; Liu, J.; Hu, X.; Feng, J. Impact of Crystal Habit on Solubility of Ticagrelor. Crystals 2019, 9, 556. https://doi.org/10.3390/cryst9110556

AMA Style

Ren Y, Shen J, Yu K, Phan CU, Chen G, Liu J, Hu X, Feng J. Impact of Crystal Habit on Solubility of Ticagrelor. Crystals. 2019; 9(11):556. https://doi.org/10.3390/cryst9110556

Chicago/Turabian Style

Ren, Yan, Jie Shen, Kaxi Yu, Chi U. Phan, Guanxi Chen, Jiyong Liu, Xiurong Hu, and Jianyue Feng. 2019. "Impact of Crystal Habit on Solubility of Ticagrelor" Crystals 9, no. 11: 556. https://doi.org/10.3390/cryst9110556

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