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Crystal form A of diphenyl imidazole anticancer drug and preparation method thereof

A dimethoxyphenyl, crystal form technology, applied in the field of medicinal chemistry, can solve the problems of different dissolution, absorption, influence on drug bioavailability, clinical efficacy and safety, etc., and achieve the effects of good water solubility and good stability

Inactive Publication Date: 2015-11-04
NANJING SANHOME PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These differences may also lead to different dissolution and absorption in the body, thereby affecting the bioavailability, clinical efficacy and safety of the drug

Method used

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  • Crystal form A of diphenyl imidazole anticancer drug and preparation method thereof
  • Crystal form A of diphenyl imidazole anticancer drug and preparation method thereof
  • Crystal form A of diphenyl imidazole anticancer drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1C118

[0037] Example 1 Preparation of C118P crystal form A

[0038] Weigh 1 kg of 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl) imidazole phosphate disodium salt (C118P) into a 50L reactor, and add 1 kg of After stirring to dissolve in water, slowly add 12L of a mixed solvent of acetone and isopropanol with a volume ratio of 1:2 to the solution, crystallize at 0-5°C for 24 hours, filter with suction, and dry the solid under vacuum at 35°C and crush , Grinding to obtain the A crystal form of C118P.

Embodiment 2C118

[0039] Example 2 Preparation of C118P crystal form A

[0040] Weigh 1kg of 4-(3,5-Dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole phosphate disodium salt (C118P) into a 50L reactor, and add 1.5kg After stirring and dissolving, slowly add 6L of a mixed solvent of acetone and isopropanol with a volume ratio of 1:2 to the solution, crystallize at 0-5°C for 24 hours, filter with suction, and vacuum dry the obtained solid at 35°C. C118P crystal form A was obtained by crushing and grinding.

Embodiment 3C118

[0041] Example 3 Preparation of C118P crystal form A

[0042] Weigh 10 mg of 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl) imidazole phosphate disodium salt (C118P) into a 3ml glass bottle, and add 0.5 acetone ml to obtain a suspension. The resulting suspension was stirred at room temperature and protected from light for 3 days, and the resulting solid was collected by centrifugal separation.

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Abstract

The invention belongs to the field of medical chemistry and in particular relates to a new crystal form of a drug 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl) imidazole disodium phosphate with an anticancer effect, a preparation method of the crystal form, a composition comprising the crystal form and an application of the crystal form or the composition comprising the crystal form to drug preparation. The crystal form has good water solubility and stability and is suitable for preparation development.

Description

Technical field [0001] The invention belongs to the field of medicinal chemistry, and specifically relates to the anti-cancer drug 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl) imidazole phosphate disodium A new crystal form, a preparation method thereof, a composition containing the crystal form, and the use of the crystal form or a composition containing the crystal form in the preparation of medicines. Background technique [0002] Microtubules are slender and rigid cylindrical tubular structures assembled by tubulin. They are widely found in eukaryotic cells and are closely related to the maintenance of cell morphology, cell movement and cell division. For example, in the process of mitosis, microtubules play a very critical role. The microtubules form a spindle, which pulls the chromatids to the poles of the cell, and then causes the middle of the cell to shrink and divide into two. Cancer is characterized by the unlimited and endless division and proliferation of c...

Claims

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Application Information

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IPC IPC(8): C07F9/6506A61K31/675A61P35/00
Inventor 王勇刘晓蓉张雁张波谢同张仓
Owner NANJING SANHOME PHARMACEUTICAL CO LTD
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