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 Impact of Crystal Habit on Solubility of Ticagrelor
Tác giả hoặc Nhóm tác giả: Yan Ren, Jie Shen, Kaxi Yu, Chi Uyen Phan, Guanxi Chen, Jiyong Liu, Xiurong Hu and
Jianyue Feng
Nơi đăng: crystals (a journal of MPDI); Số: 9;Từ->đến trang: 556-571;Năm: 2019
Lĩnh vực: Y - Dược; Loại: Bài báo khoa học; Thể loại: Quốc tế
TÓM TẮT
ABSTRACT
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
[ crystals-09-00556-v2.pdf ]
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