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Albendazole-cholic acid derivative as well as preparation method and application thereof

A technology for albendazole and derivatives, applied in the field of albendazole-cholic acid derivatives and their preparation, can solve the problems of unstable bioavailability, low water solubility, influence on treatment and the like, and achieves improved transport efficiency, The effect of increasing solubility and reducing crystallization tendency

Active Publication Date: 2021-08-06
QINGHAI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, albendazole is easy to crystallize, has extremely low water solubility, and is poorly absorbed in the gastrointestinal tract after oral administration, resulting in poor or unstable bioavailability, which directly affects the treatment.

Method used

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  • Albendazole-cholic acid derivative as well as preparation method and application thereof
  • Albendazole-cholic acid derivative as well as preparation method and application thereof
  • Albendazole-cholic acid derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] An albendazole-cholic acid derivative, made from raw materials comprising the following components and contents: 6g of albendazole; 5mL of cross-linking agent; 54mL of N,N-dimethylformamide; 20g of cholic acid; Dicyclohexylcarbodiimide 8g; 4-dimethylaminopyridine 0.5g.

[0053] Preparation of albendazole-cholic acid derivatives

[0054] S1, preparation of intermediates

[0055] Weigh 6g of albendazole with an analytical balance, accurately measure 5mL of 4-amino-1-butanol and 27mL of N,N-dimethylformamide with a graduated cylinder, place the three in a round-bottomed flask, and stir evenly; The bottom flask was placed on a heated constant temperature magnetic stirrer, and reacted at 90°C for 24 hours. The reaction progress was detected by thin-layer chromatography, and compared with the albendazole raw material of the control group, it was determined that an intermediate was formed. After the reaction, the reaction solution was slowly added to ice water, stirred at 50...

Embodiment 2

[0065] An albendazole-cholic acid derivative, made from raw materials comprising the following components and contents: 15g of albendazole; 15mL of crosslinking agent; 70mL of N,N-dimethylformamide; 35g of cholic acid; Dicyclohexylcarbodiimide 12g; 4-dimethylaminopyridine 1.6g.

[0066] The method for preparing albendazole-cholic acid derivatives is the same as in Example 1.

[0067] The mass of the finally obtained pure albendazole-cholic acid derivative was 496.6 mg.

Embodiment 3

[0069] An albendazole-cholic acid derivative is characterized in that it is made of raw materials comprising the following components and contents: 10g of albendazole; 10mL of crosslinking agent; 60mL of N,N-dimethylformamide; Cholic acid 27.2g; dicyclohexylcarbodiimide 10.5g; 4-dimethylaminopyridine 1.05g.

[0070] The method for preparing albendazole-cholic acid derivatives is the same as in Example 1.

[0071] The mass of the finally obtained pure albendazole-cholic acid derivative was 517.2 mg.

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Abstract

The invention relates to the field of biological medicine, and particularly discloses an albendazole-cholic acid derivative as well as a preparation method and application thereof. The albendazole-cholic acid derivative is prepared from the raw materials comprising the following components and contents: 6 to 15 g of albendazole, 5 to 15 mL of a liquid cross-linking agent, 54 to 70 mL of N,N-dimethyl formamide, 20 to 35 g of cholic acid, 8 to 12 g of dicyclohexylcarbodiimide, and 0.5 to 1.6 g of 2,4-dimethylaminopyridine. The preparation method comprises the steps: S1, preparing an intermediate; S2, connecting the intermediate with cholic acid; S3, carrying out crude separation on a silica gel column; and S4, carrying out fine separation on the silica gel column. The albendazole-cholic acid derivative can be used for treating echinococcosis of a human body or an animal body, and has the advantages that the crystallization trend of albendazole is reduced, the solubility of albendazole in a living body is improved, and the drug effect is enhanced; and in addition, the preparation method has the advantage of improving the purity of the obtained product.

Description

technical field [0001] This application relates to the field of biomedicine, more specifically, it relates to an albendazole-cholic acid derivative and its preparation method and application. Background technique [0002] Hydatid disease, also known as echinococcosis, is a zoonotic parasitic disease that is currently difficult to eradicate. Currently, the most common diseases worldwide are cystic echinococcosis caused by Echinococcus granulosus and alveolar echinococcosis caused by Echinococcus multilocularis. The route of transmission is the digestive tract, through the ingestion of parasite eggs, and the parasite eggs are excreted through the feces of the final host, causing serious health and economic burdens. As an intermediate host, humans eat insect eggs by mistake, and the eggs parasitic in the small intestine develop into larvae, which invade various organs in the body, mainly the liver and lungs. From the point of view of treatment methods, since early stage patie...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/32A61P33/02
CPCC07D235/32A61P33/02Y02A50/30
Inventor 胡春晖高瑞雪秦蒙李永臻
Owner QINGHAI UNIVERSITY
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