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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

Inactive Publication Date: 2015-11-18
WUHAN YINGPURUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility of ceritinib, resulting in poor oral absorption, greatly limiting its clinical application

Method used

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  • C-type crystal form of ceritinib, preparation method therefor and application thereof
  • C-type crystal form of ceritinib, preparation method therefor and application thereof
  • C-type crystal form of ceritinib, preparation method therefor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

The present invention provides a C-type crystal form of ceritinib. In an X-ray powder diffraction pattern obtained by use of Cu-K alpha ray measurement, the C-type crystal form of the ceritinib has characteristic peaks at an 2Theta angle of 4.9 degrees, 9.4 degrees, 9.9 degrees, 12.2 degrees, 13.7 degrees, 14.2 degrees, 14.4 degrees, 14.9 degrees, 15.6 degrees, 16.5 degrees, 17.0 degrees, 17.7 degrees, 18.9 degrees, 20.6 degrees, 22.0 degrees, 25.0 degrees, 26.6 degrees, 25.9 degrees and 28.5 degrees. The present invention also provides a preparation method for the C-type crystal form of the ceritinib, and an application. The C-type crystal form of the ceritinib provided by the present invention is high in crystallinity and high in water solubility. The preparation method for the C-type crystal form of the ceritinib is simple, liable to control, liable to prepare the C-type crystal form, and good in reproducibility; and the oral bioavailability of ceritinib is remarkably improved.

Description

Technical field [0001] The invention relates to a type C crystal form of ceritinib, a preparation method and application thereof, and belongs to the technical field of new crystal forms of medicine. Background technique [0002] Polymorphism refers to the phenomenon that solid substances are arranged in two or more different spatial arrangements to form a solid state with different physical and chemical properties. It is of great significance in the pharmaceutical industry for the crystal form research and solid-state characterization of pharmaceutical active ingredients (API). The same drug with different crystal forms may have significant differences in biochemical properties such as stability, solubility, and bioavailability, thereby affecting the efficacy of the drug. If there is no good evaluation and selection of the best drug crystal form for research and development, the crystal form may change in the later clinical stage, which will lead to the change of drug efficacy a...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/506A61P35/00A61P35/02
CPCC07B2200/13C07D401/12
Inventor 杨博
Owner WUHAN YINGPURUI PHARMA CO LTD
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