4-(3,5-Dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole preparation

A technology of dimethoxyphenyl and methoxyphenyl, applied in the field of medicinal chemistry

Active Publication Date: 2021-02-19
NANJING SANHOME PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, many problems are faced in the study of this type of pharmaceutical preparations, such as the long-term stability of the preparation, the control of related substances, the hygroscopicity of the preparation, and the appearance of the product, etc.

Method used

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  • 4-(3,5-Dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole preparation
  • 4-(3,5-Dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole preparation
  • 4-(3,5-Dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] This example is a formulation of 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole phosphate disodium salt in the form of an injection (Formulation A).

[0061] 1. Recipe

[0062]

[0063] 2. Preparation steps

[0064] (1) Weigh the prescribed amount of mannitol and put it into a 50mL beaker;

[0065] (2) Measure 40mL of water for injection at 40°C with a graduated cylinder, add it to the above beaker, and stir to dissolve;

[0066] (3) Weigh the prescribed amount of C118P, add it into the beaker and stir to dissolve completely;

[0067] (4) Drain to a 50mL volumetric flask, wash the beaker several times with a little water for injection and import it into the volumetric flask, and dilute to 50mL;

[0068] (5) Filter with a 0.45 μm filter membrane, and then filter with a 0.22 μm filter membrane;

[0069] (6) Dispense the liquid medicine into vials.

Embodiment 2

[0071] This example is a formulation of 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole phosphate disodium salt in the form of an injection (Formulation B).

[0072] 1. Recipe

[0073]

[0074] According to the method of Example 1, the above C118P preparation was prepared.

Embodiment 3

[0076] This example is a formulation of 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole in the form of an injectable solution (Formulation C).

[0077] 1. Recipe

[0078]

[0079] According to the method of embodiment 1, carry out the preparation of preparation.

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Abstract

The invention belongs to the field of medicinal chemistry and relates to a preparation for parenteral administration, which comprises 4-(3,5-dimethoxyphenyl)-5-(3-hydroxyl-4-methoxyphenyl) imidazole or Its pharmaceutically acceptable salts and mannitol. The present invention also relates to the preparation method of the preparation of the present invention and the application of the preparation in medicine for treating tumors. The preparation of the invention can be stored for a long time, has few related substances, low hygroscopicity, good appearance, and can simplify storage and transportation conditions and the like.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, in particular to a gastrointestinal medicine containing 4-(3,5-dimethoxyphenyl)-5-(3-hydroxyl-4-methoxyphenyl)imidazole or a pharmaceutically acceptable salt thereof external drug preparations. Background technique [0002] 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole is a known compound with the following structure: [0003] [0004] This compound has been disclosed in Chinese patent application CN201110422678.5, which is incorporated herein by reference in its entirety. CN201110422678.5 reported that 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole has tubulin polymerization inhibitory activity. 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole is a derivative of Combretastatin A4, which is a new type of tubulin inhibitor, It specifically acts on tumor neovascularization, has strong selectivity to tumor blood vessels, has little effect on oth...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/4164A61K47/10A61P35/00
Inventor 王勇张云李玉秀张仓
Owner NANJING SANHOME PHARMACEUTICAL CO LTD
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