Pharmaceutically acceptable salt of cariprazine and crystal form thereof, and preparation method therefor and use thereof
AssigneeShanghai Yunsanova Biotechnology Co., Ltd
InventorsShuhuan Ying, Zhixiang Chen, Xian Zhang, Tao Zhu, Tingting Wang, Shuang Liu
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Abstract
A pharmaceutically acceptable salt of cariprazine, a preparation method therefor, a pharmaceutical composition containing same, and the use thereof are provided. The pharmaceutically acceptable salt of cariprazine is a salt formed from the free base of cariprazine and an organic acid having six or more carbon atoms, and has relatively good solubility and stability.
Claims19
A pharmaceutically acceptable salt of cariprazine of formula I, selected from at least one of crystalline forms A, F, D, B, C, E, G and I of cariprazine embonate:
- wherein:
- an X-ray powder diffraction graph of the crystalline form A of cariprazine embonate has characteristic peaks at 2θ values of 4.8°±0.2°, 13.1°±0.2°, 18.7°±0.2°, 20.1°±0.2°, 21.0°±0.2°, and 26.1°±0.2°, wherein the cariprazine embonate is formed with cariprazine and embonic acid in a molar ratio of 1:1;
- an X-ray powder diffraction graph of the crystalline form F of cariprazine embonate has characteristic peaks at 2θ values of 4.9°±0.2°, 13.6°±0.2°, 19.2°±0.2°, 21.0°±0.2°, 24.0°±0.2°, and 26.3°±0.2°, wherein the cariprazine embonate is formed with cariprazine and embonic acid in a molar ratio of 1:1;
- an X-ray powder diffraction graph of the crystalline form D of cariprazine embonate has characteristic peaks at 2θ values of 9.6°±0.2°, 11.9°±0.2°, 16.6°±0.2°, 20.4°±0.2°, 24.5°±0.2°, and 25.3°±0.2°, wherein the cariprazine embonate is formed with cariprazine and embonic acid in a molar ratio of 1:1, and the cariprazine embonate contained about 0.67 ethanol molecules;
- an X-ray powder diffraction graph of the crystalline form B of methanol solvate of cariprazine embonate has characteristic peaks at 2θ values of 5.2°±0.2°, 10.5°±0.2°, 14.0°±0.2°, 14.4°±0.2°, 17.5°±0.2°, 21.3°±0.2°, 21.9°±0.2°, 22.9°±0.2°, and 26.2°±0.2°;
- an X-ray powder diffraction graph of the crystalline form C of acetone solvate of cariprazine embonate has characteristic peaks at 2θ values of 8.6°±0.2°, 13.0°±0.2°, 16.8°±0.2°, 17.3°±0.2°, 18.2°±0.2°, 18.5°±0.2°, 19.8°±0.2°, 22.1°±0.2°, and 23.5°±0.2°;
- an X-ray powder diffraction graph of the crystalline form E of cariprazine embonate has characteristic peaks at 2θ values of 11.0°±0.2°, 12.8°±0.2°, 13.8°±0.2°, 15.5°±0.2°, 15.9°±0.2°, 17.9°±0.2°, 18.4°±0.2°, 20.7°±0.2°, and 23.4°±0.2°;
- an X-ray powder diffraction graph of the crystalline form G of acetonitrile solvate cariprazine embonate has characteristic peaks at 2θ values of 8.7°±0.2°, 10.0°±0.2°, 13.6°±0.2°, 14.3°±0.2°, 17.5°±0.2°, 18.0°±0.2°, 20.3°±0.2°, 23.2°±0.2°, and 25.1°±0.2°;
- and
- an X-ray powder diffraction graph of the crystalline form I of acetonitrile solvate cariprazine embonate has characteristic peaks at 2θ values of 10.0°±0.2°, 14.9°±0.2°, 16.3°±0.2°, 17.7°±0.2°, 18.5°±0.2°, 19.0°±0.2°, 21.1°±0.2°, 22.1°±0.2°, and 24.5°±0.2°.
The pharmaceutically acceptable salt of cariprazine of formula I that is a crystalline form I of cariprazine embonate.
Dependencies are inferred from the claim text.