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Clathrate compound of beta-cyclodextrin or derivatives of beta-cyclodextrin for Nifuroxazide and preparation method for preparation of clathrate compound

A technology of nifuryl hydrazide and cyclodextrin, which is applied in the fields of feed additives and veterinary drugs, can solve the problems of poor storage performance and poor solubility, and can increase the inclusion effect, improve the inclusion rate and quality of inclusion, and increase the increase in The effect of dissolution efficiency

Active Publication Date: 2012-09-19
SHANGHAI E K M BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve the problems of poor solubility, dissolution rate and poor storage performance of nifurofen hydrazide preparations in the prior art, the present invention provides a clathrate of nifurofarzide β-cyclodextrin or its derivatives and its Preparation method of preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Take 100g of nifurofarzide, dissolve it in 500ml of ethanol, add 25g of povidone K30 to dissolve and stir evenly; take another 800g of β-cyclodextrin, dissolve it in 39200ml of distilled water, heat to 40℃~45℃, make it Dissolve everything, set the stirring speed to 300 rpm, slowly add the nifurofarzide and povidone K30 alcohol solution dropwise into the β-CD aqueous solution, stop heating after the addition is complete, and continue stirring for 4 to 6 hours , stop stirring, put the reaction solution at 2°C-4°C and let it stand for 24 hours, filter it with suction, add distilled water from the filter, wash it twice with suction, and dry it at 35°C-40°C to obtain loose powdered nifurofol hydrazide β-cyclodextrin inclusion complex.

Embodiment 2

[0021] Take 100g of nifurofarzide, dissolve it in 1000ml of methanol, add 12.5g of povidone K30 to dissolve and stir evenly; take another 500g of hydroxypropyl-β-cyclodextrin (HP-CD), dissolve it in 12000ml of distilled water , heated to 40°C to 45°C to dissolve them all, set the stirring speed to 300 rpm, slowly add the nifurofen hydrazide and povidone K30 alcohol solution dropwise into the aqueous solution of hydroxypropyl-β-cyclodextrin , after all the drops are completed, stop heating, continue to stir for 4-6 hours, stop stirring, put the reaction solution at 2°C-4°C for 24 hours, filter it with suction, add distilled water from the filter and wash it twice , and dried under reduced pressure in vacuum to obtain a loose powdery nifurofen hydrazide hydroxypropyl-β-cyclodextrin inclusion complex.

Embodiment 3

[0023] The stirring process in Example 1 was changed to ultrasonic vibration for 20 minutes, and other operations were the same as in Example 1 to obtain a loose powdery nifurofen hydrazide β-cyclodextrin inclusion compound.

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Abstract

The invention relates to a clathrate compound of beta-cyclodextrin or derivatives of the beta-cyclodextrin for Nifuroxazide and a preparation method for a preparation of the clathrate compound. The clathrate compound consists of the following raw materials in weight ratio: 1 percent of Nifuroxazide, 0.125-0.25 percent of povidone K30 and 5-25 percent of beta-cyclodextrin or derivatives of the beta-cyclodextrin. The invention aims to solve the problems that traditional market products are low in water solubility and dissolution rate generally, sediments are often generated and colors are darkened during the application process and the like. According to the invention, clathration is performed on the Nifuroxazide by adopting the beta-cyclodextrin or the derivatives of the beta-cyclodextrin,so that the Nifuroxazide can be easily dissolved in water, and meanwhile, the stability of the Nifuroxazide is improved; the form of the preparation is expanded; the route of administration is enlarged; and an application effect is promoted.

Description

technical field [0001] The present invention relates to the technical field of veterinary medicine, and at the same time relates to the field of feed additives, and also relates to a preparation of nifurofen hydrazide cyclodextrin inclusion compound, specifically a preparation of nifurofarzide β-cyclodextrin or its derivatives Preparation method of clathrate and preparation. Background technique [0002] Nifuroxazide, also known as Nifurazide, is a nitrofuran antineoplastic drug in human medicine, and is commonly used in clinical treatment of colitis and diarrhea. Nifurofen hydrazide has a broad antibacterial spectrum, high antibacterial activity, and low inhibitory concentration. It has no cross-resistance with sulfonamides, quinolones and other antibiotics. Its antibacterial activity is hardly affected by other organic substances, and its effect is stable. Because this product can effectively prevent and treat intestinal or urinary system diseases caused by E. Feed by an...

Claims

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Application Information

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IPC IPC(8): A61K47/40A61K47/32A61K31/345A61P35/00A61P31/04A61P1/00A61P1/12A61P13/00A23K1/17A23K20/195
Inventor 张奎昌张婷婷张路
Owner SHANGHAI E K M BIOTECH
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