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Enrofloxacin/sulfobutylether-beta-cyclodextrin inclusion compound, preparation method and medicinal preparation thereof

A technology of cyclodextrin inclusion complex and sulfobutyl ether, which is applied in the preparation method and pharmaceutical preparation thereof, in the field of enrofloxacin/sulfobutyl ether-β-cyclodextrin inclusion complex, and can solve the problem of poor solubility in water and other problems, to achieve the effect of improved stability, good curative effect and good oral palatability

Inactive Publication Date: 2013-02-13
CHONGQING ACAD OF ANIMAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The technical problem to be solved by the present invention is to provide an inclusion compound of enrofloxacin and its pharmaceutical preparation in view of the characteristics of enrofloxacin, such as bitter taste and poor solubility in water, which have significantly improved solubility in water phase and high stability. , good palatability

Method used

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  • Enrofloxacin/sulfobutylether-beta-cyclodextrin inclusion compound, preparation method and medicinal preparation thereof
  • Enrofloxacin/sulfobutylether-beta-cyclodextrin inclusion compound, preparation method and medicinal preparation thereof
  • Enrofloxacin/sulfobutylether-beta-cyclodextrin inclusion compound, preparation method and medicinal preparation thereof

Examples

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Effect test

Embodiment 1

[0047] Example 1: Weigh 6 grams of sulfobutyl ether-β-cyclodextrin (substitution degree 7), 1 gram of enrofloxacin, and dissolve them in 75 ml of water and 25 ml of ethanol respectively, and mix the two solutions after dissolving , heated and stirred at 55°C for 1 hour, cooled to room temperature, and filtered to obtain a solution, which was then spray-dried to obtain enrofloxacin / sulfobutyl ether-β-cyclodextrin inclusion compound.

Embodiment 2

[0048] Example 2: Weigh 3 grams of sulfobutyl ether-β-cyclodextrin (degree of substitution: 4), 1 gram of enrofloxacin, and dissolve them in 65 ml of water and 35 ml of methanol respectively, and mix the two solutions after dissolving , heated and stirred at 45°C for 36 hours, cooled to room temperature, filtered to obtain a solution, and the obtained solution was freeze-dried, which was enrofloxacin / sulfobutyl ether-β-cyclodextrin inclusion compound.

Embodiment 3

[0049] Example 3: Weigh 1 gram of sulfobutyl ether-β-cyclodextrin (substitution degree 7), 1 gram of enrofloxacin, and dissolve them in 25 ml of water and 75 ml of propanol respectively, and mix the two The solution was heated and stirred at 65°C for 2 hours, cooled to room temperature, filtered to obtain the solution, and the obtained solution was freeze-dried, which was enrofloxacin / sulfobutyl ether-β-cyclodextrin inclusion compound.

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Abstract

The invention relates to an enrofloxacin / sulfobutylether-beta-cyclodextrin inclusion compound, a preparation method and a medicinal preparation thereof. The inclusion compound comprises sulfobutylether-beta-cyclodextrin and enrofloxacin in a weight ratio of 1-10:1, and sulfobutylether-beta-cyclodextrin respectively has the average degree of substitution of 1, 4 and 7. The preparation method comprises the following steps: (1) weighing raw materials in a mass ratio of sulfobutylether-beta-cyclodextrin to enrofloxacin of 1-10:1, and respectively dissolving in a solvent which is water, ethanol solvent or mixture of water and ethanol solvent; and (2) mixing the two liquids prepared in the step (1) to perform an inclusion reaction. The medicinal preparation can be oral preparation and injection, wherein the oral preparation can be tablets, soluble powder and oral liquid; and the injection can be injection liquid and lyophilized powder. The medicinal preparation has the advantages of remarkably improved solubility in water phase, improved stability, excellent palatability, good curative effect and low toxic and side effects.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to an enrofloxacin / sulfobutyl ether-β-cyclodextrin inclusion compound, a preparation method and a pharmaceutical preparation thereof. Background technique [0002] Enrofloxacin is a chemically synthesized quinolone antibacterial drug, also known as ethyl ciprofloxacin and ethyl ciprofloxacin. Enrofloxacin is a special drug for animals, which is used for the treatment of skin infections, urinary tract infections, respiratory tract infections and wound infections. The structure of enrofloxacin is as follows: [0003] [0004] Enrofloxacin is light yellow or light orange crystalline powder in appearance; odorless, bitter in taste; color gradually changes to orange red when exposed to light. Soluble in chloroform, slightly soluble in dimethylformamide, slightly soluble in methanol, very slightly soluble in water; soluble in sodium hydroxide test solution, melting point 221-226°C, easy to ab...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/496A61P31/04
Inventor 王建华李成洪
Owner CHONGQING ACAD OF ANIMAL SCI
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