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Beta-cyclodextrin/amoxicillin inclusion complex, as well as preparation method and application thereof

A technology of amoxicillin and cyclodextrin, which is applied in the directions of active ingredients of heterocyclic compounds, pharmaceutical formulations, medical preparations of non-active ingredients, etc. The content of cillin polymer, reducing the probability of allergic reaction, etc., can improve the phenomenon of deliquescence and agglomeration, expand the scope of clinical use, and improve the palatability.

Inactive Publication Date: 2015-04-29
LUOYANG HUIZHONG ANIMAL MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The invention significantly improves the stability, mechanical processing performance and dissolution characteristics of amoxicillin, and improves the pharmaceutical performance by cooperating with potassium clavulanate, but fails to control the content of amoxicillin polymers to reduce the probability of allergic reactions. Solve the problem of deliquescence and caking of amoxicillin soluble powder

Method used

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  • Beta-cyclodextrin/amoxicillin inclusion complex, as well as preparation method and application thereof
  • Beta-cyclodextrin/amoxicillin inclusion complex, as well as preparation method and application thereof
  • Beta-cyclodextrin/amoxicillin inclusion complex, as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation of Example 1β-cyclodextrin / amoxicillin inclusion compound and 1% amoxicillin soluble powder

[0026] 1. Weigh 2.8g of β-cyclodextrin and add it to 10ml of distilled water to make a suspension;

[0027] 2. Add lg amoxicillin and lg micropowder silica gel, mix and grind for 3 hours;

[0028] 3. Cool at room temperature, filter, wash the solid with water and dry to obtain β-cyclodextrin / amoxicillin inclusion compound;

[0029] 4. Pulverize the β-cyclodextrin / amoxicillin inclusion complex through an 80-mesh sieve, and mix it with 95.2 g of anhydrous glucose to obtain 100 g of amoxicillin soluble powder.

Embodiment 2

[0030] Preparation of Example 2 β-cyclodextrin / amoxicillin inclusion compound and 20% amoxicillin soluble powder

[0031] 1. Weigh 56g of β-cyclodextrin and add it to 200ml of distilled water to make a suspension;

[0032] 2. Add 20g of amoxicillin and 0.2g of micropowder silica gel, mix and grind for 5 hours;

[0033] 3. Cool at room temperature, filter, wash the solid with water and dry to obtain β-cyclodextrin / amoxicillin inclusion compound;

[0034] 4. Pulverize the β-cyclodextrin / amoxicillin inclusion complex through an 80-mesh sieve, and mix it with 23.8 g of anhydrous glucose to obtain 100 g of amoxicillin soluble powder.

Embodiment 3

[0035] Example 3 Preparation of β-cyclodextrin / amoxicillin inclusion compound and 10% amoxicillin soluble powder

[0036] 1. Weigh 28g of β-cyclodextrin and add it to 100ml of distilled water to make a suspension;

[0037] 2. Add 10g of amoxicillin and 0.5g of micropowder silica gel, mix and grind for 5 hours;

[0038] 3. Cool at room temperature, filter, wash the solid with water and dry to obtain β-cyclodextrin / amoxicillin inclusion compound;

[0039] 4. Pulverize the inclusion complex of β-cyclodextrin / amoxicillin through an 80-mesh sieve, and mix with 61.5 g of anhydrous glucose to obtain 100 g of amoxicillin soluble powder.

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Abstract

The invention discloses a beta-cyclodextrin / amoxicillin inclusion complex and a preparation process thereof. The beta-cyclodextrin / amoxicillin inclusion complex is prepared from the following components in percentage by mass: 15-35 percent of amoxicillin, 40-80 percent of beta-cyclodextrin and 0.1-30 percent of aerosil. The preparation process adopts a technology of molecular inclusion complexation by adopting beta-cyclodextrin. The beta-cyclodextrin / amoxicillin inclusion complex has the advantages of low polymer impurity content, hardly deliquescence or casing in storing process, excellent palatability and the like.

Description

technical field [0001] The invention belongs to the technical field of veterinary pharmaceutical preparations, and specifically relates to a β-cyclodextrin / amoxicillin inclusion compound and a preparation process thereof, and the use of the β-cyclodextrin / amoxicillin inclusion compound in the preparation of veterinary drugs. application. Background technique [0002] Amoxicillin, also known as amoxicillin, is a semi-synthetic β-lactam antibiotic, first introduced to the market by BEECHAM in 1972. It has strong bactericidal effect and strong cell penetrating ability, and is easily absorbed by oral administration and injection. , amoxicillin oil for injection and amoxicillin long-acting injection oil have been widely used in the treatment of sensitive bacterial infections in pigs, cattle and poultry. [0003] Due to the β-lactam structure, amoxicillin is prone to intermolecular polymerization and forms sensitizing polymer impurities, making the allergic reaction of its prepa...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/43A61K47/04A61P31/04
Inventor 张许科刘兴金张晓会
Owner LUOYANG HUIZHONG ANIMAL MEDICINE
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