Target-releasing polyethylene glycol modified paclitaxel medicine and preparation method thereof

A polyethylene glycol modification, paclitaxel technology, applied in the field of medicine, can solve the problems of unstable concentration, reduced blood drug concentration, phagocytosis, etc.

Inactive Publication Date: 2020-07-07
福建齐衡科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Patent application number CN103768046 discloses a paclitaxel nanocrystal for injection and its preparation method. After the prepared paclitaxel nanocrystal enters the body, it uses the targeted recognition of the reticuloendothelial system (RES) to act on tumor cells, but it is easy to It is swallowed as a foreign body, and the targeting is not strong. At the same time, it is easy to accumulate in RES-rich tissues, such as the liver and spleen, causing a sharp drop in blood drug concentration, requiring unstable concentration

Method used

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  • Target-releasing polyethylene glycol modified paclitaxel medicine and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Preparation of EBMB-PEG:

[0030] Add 10g of dried polyethylene glycol monomethyl ether (M=2000) into 20ml of dried tetrahydrofuran, add 0.5g of sodium hydride powder to it under the protection of nitrogen, immediately generate a lot of bubbles, stir at room temperature for 4 Hour.

[0031] Dissolve ethyl 4-bromomethylbenzoate in 5ml of dried tetrahydrofuran, add dropwise to the above reaction solution in an ice bath, the dropwise addition is completed within half an hour, continue the reaction for 2 hours, and add water to terminate the reaction. Remove tetrahydrofuran and water by rotary evaporation, then dissolve the product three times with 90ml of dichloromethane, combine all the dichloromethane, centrifuge to get the supernatant, and then use n-hexane to precipitate three times after rotary evaporation to remove most of the dichloromethane. Remove the solvent by rotary evaporation, then add 1 mol / ml sodium hydroxide aqueous solution to dissolve the crude product,...

Embodiment 2

[0042] Preparation of EBMB-PEG:

[0043] Add 10g of dried polyethylene glycol monomethyl ether (M=2000) into 20ml of dried tetrahydrofuran, add 0.5g of sodium hydride powder to it under the protection of nitrogen, immediately generate a lot of bubbles, stir at room temperature for 4 Hour.

[0044] Dissolve ethyl 4-bromomethylbenzoate in 5ml of dried tetrahydrofuran, add dropwise to the above reaction solution in an ice bath, the dropwise addition is completed within half an hour, continue the reaction for 2 hours, and add water to terminate the reaction. Remove tetrahydrofuran and water by rotary evaporation, then dissolve the product three times with 90ml of dichloromethane, combine all the dichloromethane, centrifuge to get the supernatant, and then use n-hexane to precipitate three times after rotary evaporation to remove most of the dichloromethane. Remove the solvent by rotary evaporation, then add 1 mol / ml sodium hydroxide aqueous solution to dissolve the crude product,...

Embodiment 3

[0055] Preparation of EBMB-PEG:

[0056] Add 10g of dried polyethylene glycol monomethyl ether (M=2000) into 20ml of dried tetrahydrofuran, add 0.5g of sodium hydride powder to it under the protection of nitrogen, immediately generate a lot of bubbles, stir at room temperature for 4 Hour.

[0057] Dissolve ethyl 4-bromomethylbenzoate in 5ml of dried tetrahydrofuran, add dropwise to the above reaction solution in an ice bath, the dropwise addition is completed within half an hour, continue the reaction for 2 hours, and add water to terminate the reaction. Remove tetrahydrofuran and water by rotary evaporation, then dissolve the product three times with 90ml of dichloromethane, combine all the dichloromethane, centrifuge to get the supernatant, and then use n-hexane to precipitate three times after rotary evaporation to remove most of the dichloromethane. Remove the solvent by rotary evaporation, then add 1 mol / ml sodium hydroxide aqueous solution to dissolve the crude product,...

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Abstract

The invention discloses a target-releasing polyethylene glycol modified paclitaxel medicine. The medicine comprises a paclitaxel-loaded TPP-PEG-EBMB micelle. A preparation method of the medicine comprises the following steps: S1, preparing EBMB-PEG from methoxypolyethylene glycol and ethyl 4-benzoate; S2, aminating the single end of the EBMB-PEG to obtain EBMB-PEG-NH2; S3, polymerizing the EBMB-PEG-NH2 with TPP to obtain TPP-PEG-EBMB; and S4, preparing the paclitaxel-loaded TPP-PEG-EBMB micelle, and performing modification on polyethylene glycol derivatives to improve the target property of paclitaxel mitochondria.

Description

technical field [0001] The invention belongs to the field of drugs, and in particular relates to a polyethylene glycol-modified paclitaxel drug for targeted release and a preparation method thereof. Background technique [0002] Malignant tumors have become a disease that seriously threatens human health. According to statistics, 21.75% of people who die due to diseases die of cancer every year. At present, a large number of studies have confirmed that the occurrence and development of tumors are closely related to cell apoptosis, and mitochondria have a regulatory effect on cell apoptosis. Paclitaxel is a mitochondria-mediated antitumor drug, which is clinically used in the treatment of various cancers such as breast cancer, lung cancer, nasopharyngeal cancer and ovarian cancer. The literature shows that paclitaxel can improve the permeability of mitochondrial membrane, increase the concentration of calcium ion in cytoplasm, decrease the potential of mitochondrial membrane...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/60A61K31/337A61K47/54A61P35/00A61K9/19A61K47/10A61K47/26A61K47/40
CPCA61K47/6907A61K47/60A61K31/337A61K47/542A61P35/00A61K9/19A61K47/26A61K47/10A61K47/40
Inventor 林金新杨建民黄达田永奇
Owner 福建齐衡科技有限公司
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