C-type crystal form of ceritinib, preparation method therefor and application thereof
A technology of ceritinib and crystal form, which is applied in organic chemical methods, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of ceritinib's poor water solubility, poor oral absorption, and limited clinical application, etc. Achieve the effect of good reproducibility, easy control and simple preparation method
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Embodiment 1
[0032] This embodiment provides a type C crystal form of Ceritinib. The X-ray powder diffraction pattern of the crystal form measured by Cu-Kα rays has 2θ angles of 4.9°, 9.4°, 9.9°, 12.2°, There are characteristic peaks at 13.7°, 14.2°, 14.4°, 14.9°, 15.6°, 16.5°, 17.0°, 17.7°, 18.9°, 20.6°, 22.0°, 25.0°, 26.6°, 25.9° and 28.5°, such as figure 1 Shown.
[0033] The type C crystal form of Ceritinib of this example was measured at about 100°C-120°C with a characteristic peak of endothermic and then exothermic by differential scanning calorimetry, and a characteristic melting peak was measured at about 172.9°C. Such as figure 2 Shown.
[0034] The thermogravimetric analysis diagram and infrared spectrum diagram of the C-type crystal form of Ceritinib of this embodiment are as follows image 3 with Figure 4 Shown.
[0035] The type C crystal form of Ceritinib in this example was prepared by the following method:
[0036] Place 1.0g of ceritinib in an Erlenmeyer flask, add 50 mL of met...
Embodiment 2
[0040] This example provides a type C crystal form of Ceritinib, and the qualitative determination results are the same as in Example 1.
[0041] The type C crystal form of Ceritinib in this example was prepared by the following method:
[0042] Place 1.0 g of Ceritinib in an Erlenmeyer flask, and add 50 mL of methanol. Use a magnetic stirrer to stir, and heat in a water bath at 40°C until completely dissolved to obtain a ceritinib solution; place the ceritinib solution in a refrigerator at 5°C to cool and crystallize. After the solid precipitated, it was filtered and dried under reduced pressure at room temperature. 0.95 g of white crystalline powder is obtained, which is the C crystal form of Ceritinib, and the yield is 95%.
Embodiment 3
[0044] This example provides a type C crystal form of Ceritinib, and the qualitative determination results are the same as in Example 1.
[0045] The type C crystal form of Ceritinib in this example was prepared by the following method:
[0046] Place 1.0 g of Ceritinib in an Erlenmeyer flask, and add 50 mL of methanol / acetone (volume ratio 2:1). Use a magnetic stirrer to stir, and heat in a water bath at 40°C to completely dissolve to obtain a ceritinib solution; place the ceritinib solution in a refrigerator at 5°C to cool and crystallize. After the solid precipitated, it was filtered and dried under reduced pressure at room temperature. 0.93 g of white crystalline powder is obtained, which is the type C crystal form of Ceritinib, and the yield is 93%.
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