| 摘要 |
The present invention relates to the field of pharmaceutical chemistry. Disclosed herein is a crystalline form of azilsartan medoxomil potassium, which is substantially pure. The crystalline form is crystalline form A, form B, form C, form D, form E, form F, form G, form H, form I, form J, form K or form L. The substantially pure crystalline forms of azilsartan medoxomil potassium of the invention generally have good properties such as high solubility, high bioavailability, good stability, long shelf life and good antistatic property. The crystalline forms of azilsartan medoxomil potassium generally exhibit an excellent performance in reducing clinical systolic blood pressure (SBP) and average 24-hour SBP. Disclosed herein are methods of preparing the substantially pure crystalline forms of azilsartan medoxomil potassium, pharmaceutical compositions comprising the crystalline forms, and preparation methods and uses thereof. |
| 主权项 |
1. A crystalline form of azilsartan medoxomil potassium, wherein the crystalline form is form A, form B, form C, form D, form E, form F, form G, form H, form I, form J, form K or form L and wherein:
a) form A has an X-ray powder diffraction pattern comprising peaks at 7.41, 10.74, 18.19, 22.83, 23.29, 23.66 and 24.80 degrees +/−5% in term of two theta; b) form B has an X-ray powder diffraction pattern comprising peaks at 23.01, 23.11, 26.01, and 28.32 degrees +/−5% in term of two theta; c) form C has an X-ray powder diffraction pattern comprising peaks at 6.20 and 18.70 degrees +/−5% in term of two theta; d) form D has an X-ray powder diffraction pattern comprising peaks at 6.18, 15.22, 18.62, 19.34, 23.54, 24.88, and 26.94 degrees +/−5% in term of two theta; e) form E has an X-ray powder diffraction pattern comprising peaks at 6.16, 13.34, 16.22, 18.58, 19.88, 21.46, 22.86, 26.84, 28.28, and 33.62 degrees +/−5% in term of two theta; f) form F has an X-ray powder diffraction pattern comprising peaks at 17.96, 22.52, and 23.32 degrees +/−5% in term of two theta; g) form G has an X-ray powder diffraction pattern comprising peaks at 6.18, 13.32, 14.10, 14.44, 16.02, 17.80, 18.70, 21.30, 22.70, 22.90, 23.70, 24.38, 24.74, 26.90, 28.28, and 40.50 degrees +/−5% in term of two theta; h) form H has an X-ray powder diffraction pattern comprising peaks at 6.18, 13.32, 14.10, 14.36, 17.34, 18.72, 22.80, 23.56, and 27.02 degrees +/−5% in term of two theta; i) form I has an X-ray powder diffraction pattern comprising peaks at 6.06, 12.10, 13.86, 15.00, 18.72, 19.54, 21.54, 23.04, 23.88, 25.44, and 28.36 degrees +/−5% in term of two theta; j) form J has an X-ray powder diffraction pattern comprising peaks at 13.18, 15.90, 20.18, 21.10, 22.22, 22.52, 23.24, and 23.98 degrees +/−5% in term of two theta; k) form K has an X-ray powder diffraction pattern comprising peaks at 6.06, 12.48, 13.22, 13.92, 14.34, 14.62, 15.84, 18.60, 20.14, 20.92, 22.66, 23.66, 24.00, and 26.86 degrees +/−5% in term of two theta; or l) form L has an X-ray powder diffraction pattern comprising peaks at 10.34, 18.26, 20.92, 22.10, and 24.06 degrees +/−5% in term of two theta. |
