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Florfenicol-beta-cyclodextrin inclusion complex and preparation method thereof

A technology of cyclodextrin inclusion complex and florfenicol is applied in the directions of pharmaceutical formulations, non-active medical preparations, antibacterial drugs, etc. Benicol has poor water solubility and other problems, and achieves the effects of high inclusion rate, high bioavailability and high preparation efficiency.

Inactive Publication Date: 2016-12-07
FOSHAN UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In view of the deficiencies in the prior art, the present invention is to provide a Florfenicol-β-cyclodextrin inclusion compound with high inclusion rate and high yield and a preparation method thereof, aiming at solving the problem of poor water solubility of Florfenicol at present. , When used as a drug to treat chronic bacterial diseases of aquatic animals, the bioavailability is low, and its drug effect cannot be fully exerted

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] This embodiment provides a preparation method of florfenicol-β-cyclodextrin inclusion compound, wherein the preparation method is:

[0035] A. Add 35ml of distilled water to 0.005mol of β-cyclodextrin, heat and dissolve to make a saturated solution A;

[0036] B. Add 13ml of ethanol to 0.005mol of Florfenicol to prepare solution B;

[0037] C. Place solution A on a magnetic stirrer, and gradually drop solution B into solution B at a constant speed of 500r / min under the condition of constant temperature heating at 80°C to obtain clathrate solution; keep stirring, stop heating, and fill the clathrate solution The container is placed in a water bath and stirred to room temperature, and the initial temperature of the water bath is room temperature;

[0038] D. After refrigerating the cooled inclusion solution for 24 hours, suction filter to obtain the precipitate, wash the precipitate with 5-7ml of ethanol, and then dry the precipitate at 55°C to obtain the florfenicol...

Embodiment 2

[0041] This embodiment provides a preparation method of florfenicol-β-cyclodextrin inclusion compound, wherein the preparation method is:

[0042] A. Add 20ml of distilled water to 0.005mol of β-cyclodextrin, heat and dissolve to make a saturated solution A;

[0043] B. Add 5ml of ethanol to 0.005mol of Florfenicol to prepare solution B;

[0044] C. Put solution A on a magnetic stirrer, and gradually drop solution B into solution B at a constant speed of 500r / min under the condition of constant temperature heating at 75°C to obtain inclusion solution; The container is placed in a water bath and stirred to room temperature, and the initial temperature of the water bath is room temperature;

[0045] D. After refrigerating the cooled inclusion solution for 24 hours, suction filter to obtain the precipitate, wash the precipitate with 5-7ml of ethanol, and then dry the precipitate at 55°C to obtain the florfenicol-β-cyclodextrin inclusion compound .

[0046] Experimental res...

Embodiment 3

[0048] This embodiment provides a preparation method of florfenicol-β-cyclodextrin inclusion compound, wherein the preparation method is:

[0049] A. Add 50ml of distilled water to 0.005mol of β-cyclodextrin, heat and dissolve to make a saturated solution A;

[0050] B. Add 20ml of ethanol to 0.005mol of Florfenicol to prepare solution B;

[0051] C. Put solution A on a magnetic stirrer, and gradually drop solution B into solution B at a constant speed of 500r / min under the condition of constant temperature heating at 85°C to obtain clathrate solution; The container is placed in a water bath and stirred to room temperature, and the initial temperature of the water bath is room temperature;

[0052] D. After refrigerating the cooled inclusion solution for 24 hours, suction filter to obtain the precipitate, wash the precipitate with 5-7ml of ethanol, and then dry the precipitate at 55°C to obtain the florfenicol-β-cyclodextrin inclusion compound .

[0053] Experimental re...

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Abstract

The invention provides a florfenicol-β-cyclodextrin inclusion compound and a preparation method thereof, wherein the preparation method is: A. Add distilled water to β-cyclodextrin, heat and dissolve to make a saturated solution A; B. Add ethanol to Florfenicol to prepare solution B; C. Place solution A on a magnetic stirrer, and gradually drop solution B into solution B at a constant temperature of 75-85°C at a constant speed of 500r / min to obtain clathrate solution; The combined liquid container is placed in a water bath and stirred to room temperature; D. After the cooled clathrate solution was refrigerated for 24 hours, the precipitate was obtained after suction filtration, and the precipitate was washed with ethanol, and then dried at 55°C to obtain the florfenicol-β-cyclodextrin inclusion compound. The preparation method is simple in operation and high in preparation efficiency, and the prepared florfenicol-β-cyclodextrin inclusion compound has a high inclusion rate and a greatly improved yield, and is suitable for large-scale production for preventing and controlling aquatic animals. bacterial disease.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a florfenicol-β-cyclodextrin inclusion compound and a preparation method thereof. Background technique [0002] Florfenicol (Florfenicol) is an excellent animal-specific broad-spectrum antibiotic, which is widely used clinically in various acute and chronic bacterial diseases of fish, shrimp, crab, shellfish and other aquatic animals. However, due to the extremely poor water solubility of florfenicol, when fish and shrimps are splashed and soaked for medication, the drug absorption is poor and the bioavailability is low, which greatly affects the curative effect of the drug. Therefore, the development of new formulations of florfenicol soluble powder is carried out to improve the solubility and release rate of florfenicol, which is conducive to the rapid absorption of fish and shrimp through gills and skin, improves bioavailability, and fully exerts the curative effect, making it more su...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/165A61P31/04
CPCA61K31/165
Inventor 杨鸿马可杨少林张平李瑞欣邓桦蒲文珺
Owner FOSHAN UNIVERSITY
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