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Preparation method of polyethylene glycol-based water-soluble bufalin macromolecule prodrug

A technology of polyethylene glycol and bufalin, which is applied in the direction of pharmaceutical formulations, organic active ingredients, medical preparations of non-effective ingredients, etc., can solve the problems of restricting wide application, strong toxic side effects, etc. The method is simple and the effect of reducing toxic and side effects

Inactive Publication Date: 2016-08-17
SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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Problems solved by technology

However, its wide clinical application is greatly limited due to its strong toxic side effects and water insoluble defects.

Method used

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  • Preparation method of polyethylene glycol-based water-soluble bufalin macromolecule prodrug
  • Preparation method of polyethylene glycol-based water-soluble bufalin macromolecule prodrug
  • Preparation method of polyethylene glycol-based water-soluble bufalin macromolecule prodrug

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Embodiment 1

[0034] Example 1 Preparation of polyethylene glycol-based water-soluble bufalin macromolecular prodrug PEGS-bufalin

[0035] According to the following synthetic route,

[0036]

[0037] Passing steps:

[0038] (1) Preparation of PEG-MAH

[0039] 10 g monomethyl etherified polyethylene glycol (MPEG-OH, M n = 5000) and 0.2 g of triethylamine dissolved in 50 mL of dichloromethane, then transferred to an ice-water bath, and then maleic anhydride (0.3 g) dissolved in 10 mL of dichloromethane was added dropwise to the solution to react In 2 days, the obtained product was precipitated and purified in ice ether to prepare PEG-MAH;

[0040] (2) Preparation of PEGS-COOH

[0041] Dissolve 1.0 g PEG-MAH, 0.02 g triethylamine and 0.03 g propyl mercaptan in 10 mL DMF, o After reacting at C for 24 hours, the product obtained is precipitated and purified in ice ether to prepare PEGS-COOH;

[0042] (3) Preparation of PEGS-bufalin

[0043] Dissolve 100 mg PEGS-COOH, 12 mg bufafalin, and 1 mg 4-dimethylam...

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Abstract

The invention belongs to the technical field of a tumor targeted delivery and slow release drug delivery system. The invention relates to a preparation method of a polyethylene glycol-based water-soluble bufalin macromolecule prodrug PEGS-bufalin. PEG is used as a water-soluble element, bufalin is used as a model drug, easily degradable ester bonds are used for covalently linking PEG and bufalin, and the polyethylene glycol based water-soluble bufalin macromolecule prodrug (PEGS-bufalin for short). Tests show that the water-soluble bufalin macromolecule prodrug can effectively reduce toxic and side effects of bufalin and improve water solubility and tumor targeting. The preparation method is simple and is suitable for large scale production, especially is suitable for preparing the tumor targeted delivery and slow release drug delivery system with long cycle, biodegradability, sustained and controlled release, passive targeting, and tumor resistance, and especially is suitable for preparing a medicament for resisting intestinal cancer.

Description

technical field [0001] The invention belongs to the technical field of tumor targeted delivery and sustained release drug delivery system. The invention relates to a preparation method of a water-soluble macromolecular prodrug of bufalin based on polyethylene glycol, especially a preparation method of a macromolecular prodrug of water-soluble bufalin (PEGS-bufalin for short). Background technique [0002] Studies have disclosed that bufalin is the main active ingredient in bufa toxin, and has good therapeutic effects on various malignant tumors. However, its wide clinical application is greatly limited due to its strong toxic side effects and water insoluble defects. In recent decades, delivery systems based on biodegradable polymers have attracted much attention at home and abroad due to their unique advantages. Studies have shown that encapsulating drugs in targeted delivery carriers can effectively reduce the toxic and side effects of drugs, improve the solubility of dr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/585A61P35/00
Inventor 殷佩浩刘涛彭文汤庆丰邱艳艳许婕蔡杰姜婷赵汝楠唐礼瑞包益洁于卉石晓静邹瑜
Owner SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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