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

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

Active Publication Date: 2015-07-15
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 pharmaceutical chemistry field, and relates to a parenteral administration preparation comprising 4-(3,5-dimethoxyphenyl)-5-(3-hydroxy-4-methoxyphenyl)imidazole or pharmaceutically acceptable salts thereof and mannitol. The invention also relates to a preparing method of the preparation and an application of the preparation in drugs for treating tumor. The preparation can be preserved for a long time, has fewer related materials, is low in moisture absorption and good in appearance, and enables storage and transportation conditions to be simplified.

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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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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