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Preparation method of conjugated docosahexaenoic acid and docetaxel targeting drug

A technology of docosahexaenoic acid and docetaxel, which is applied in the field of preparation of docosahexaenoic acid-conjugated docetaxel targeted drugs, can solve the problem of allergic reactions, high viscosity and docetaxel in patients. Paclitaxel has low water solubility and other problems, and achieves the effect of improving bioavailability, mild test conditions, and enhancing anti-cancer effect.

Inactive Publication Date: 2017-07-28
NORTHEAST FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the water solubility of docetaxel is very small. The docetaxel currently used clinically is dissolved in Tween-80, and Tween-80 is hemolytic and viscous, which will cause allergic reactions in patients.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] (1) Preparation of docetaxel-docosahexaenoic acid: mix docetaxel, 4-dimethylaminopyridine, 1,3-dicyclohexylcarbodiimide, and DHA in dichloromethane , the reaction was stirred at room temperature for 2 h using a magnetic stirrer, and nitrogen protection was introduced during the reaction. After the reaction was completed, it was diluted with ether, and the reaction mixture was washed with aqueous hydrochloric acid, water, and water-saturated sodium chloride, respectively, and the cleaning solution was collected.

[0025] (2) Drying of docetaxel-docosahexaenoic acid: it is a long process for anhydrous sodium sulfate to fully absorb water. This test utilizes anhydrous sodium sulfate to dry the reactant, and anhydrous sodium sulfate is added to the reaction solution , Dry the reactant for 40h.

[0026] (3) Separation of docetaxel-docosahexaenoic acid: DTX-DHA was separated by silica gel column chromatography. Soak the silica gel in concentrated hydrochloric acid for 24 ho...

Embodiment 2

[0028] (1) Preparation of docetaxel-docosahexaenoic acid: mix docetaxel, 4-dimethylaminopyridine, 1,3-dicyclohexylcarbodiimide, and DHA in dichloromethane , the reaction was stirred at room temperature for 3 h using a magnetic stirrer, and nitrogen protection was introduced during the reaction. After the reaction was completed, it was diluted with ether, and the reaction mixture was washed with aqueous hydrochloric acid, water, and water-saturated sodium chloride, respectively, and the cleaning solution was collected.

[0029] (2) Drying of docetaxel-docosahexaenoic acid: it is a long process for anhydrous sodium sulfate to fully absorb water. This test utilizes anhydrous sodium sulfate to dry the reactant, and anhydrous sodium sulfate is added to the reaction solution , Dry the reactant for 48h.

[0030] (3) Separation of docetaxel-docosahexaenoic acid: DTX-DHA was separated by silica gel column chromatography. Soak the silica gel in concentrated hydrochloric acid for 24 ho...

Embodiment 3

[0032] (1) Preparation of docetaxel-docosahexaenoic acid: mix docetaxel, 4-dimethylaminopyridine, 1,3-dicyclohexylcarbodiimide, and DHA in dichloromethane , the reaction was stirred at room temperature for 2 h using a magnetic stirrer, and nitrogen protection was introduced during the reaction. After the reaction was completed, it was diluted with ether, and the reaction mixture was washed with aqueous hydrochloric acid, water, and water-saturated sodium chloride, respectively, and the cleaning solution was collected.

[0033] (2) Drying of docetaxel-docosahexaenoic acid: it is a long process for anhydrous sodium sulfate to fully absorb water. This test utilizes anhydrous sodium sulfate to dry the reactant, and anhydrous sodium sulfate is added to the reaction solution , Dry the reactant for 40h.

[0034] (3) Separation of docetaxel-docosahexaenoic acid: DTX-DHA was separated by silica gel column chromatography. Soak the silica gel in concentrated hydrochloric acid for 24 ho...

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Abstract

The invention discloses a synthetic method for preparing a water-soluble targeting antitumor drug; the anticancer synthetic drug prepared by using the synthetic method has stable chemical properties. The synthesis in the method includes one-step reaction of DHA (docosahexaenoic acid) in site 2' of docetaxel. The method includes: mixing docetaxel, 4-dimethylaminopyridine, 1,3-dicyclohexylcarbodiimide and DHA, dissolving the mixture in dichloromethane, and stirring at room temperature for reacting; after reacting, diluting, washing, drying, and isolating by means of column chromatography to obtain the drug. After the preparation of the targeting anticancer drug, the water solubility of the anticancer drug docetaxel can be enhanced; as docosahexaenoic acid has targeting property, the anticancer action of the docosahexaenoic acid can be enhanced significantly.

Description

technical field [0001] The invention belongs to the field of targeted anticancer drugs, and relates to a preparation method of docetaxel-coupled docetaxel targeted drugs. Background technique [0002] Docetaxel, also known as docetaxel, is a taxane anti-tumor drug synthesized based on the chemical substance paclitaxel in the yew tree. Its mechanism of action is similar to that of paclitaxel, that is, to promote tubulin polymerization , Inhibit the depolymerization of microtubules, inhibit cell division, thereby destroying the mitosis of tumor cells. Docetaxel is used in the treatment of various cancers, especially locally advanced breast cancer and non-small cell lung cancer. However, the water solubility of docetaxel is very small, and the docetaxel currently used clinically is dissolved in Tween-80, and Tween-80 is hemolytic and highly viscous, which may cause allergic reactions in patients. Therefore, it is very important to develop water-soluble docetaxel formulations....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/55A61K47/54A61K31/337A61K31/232A61P35/00
CPCA61K31/337A61K31/232
Inventor 祖元刚姜守刚吴磊袁颖洁谭笑张星垚魏亮吴比
Owner NORTHEAST FORESTRY UNIVERSITY
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