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Veterinary danofloxacin mesylate slow-release microsphere preparation as well as preparation method and application of veterinary danofloxacin mesylate slow-release microsphere preparation

A technology of dafloxacin mesylate and slow-release microsphere preparations, applied in the field of veterinary dafloxacin mesylate slow-release microsphere preparations and its preparation, can solve the problem of low encapsulation rate of drug loading, toxicity Side effects, environmental pollution and other problems, to achieve the effect of long maintenance time of effective concentration, high drug loading, and less environmental pollution

Inactive Publication Date: 2012-07-11
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The average particle size of dafloxacin mesylate microspheres prepared by this patent application is 10~11 μm, which can meet the requirements of intramuscular injection, but the drug loading (2.0~6.3wt%) and encapsulation efficiency (8.1%~ 16.5%) is low, and used a large amount of organic reagents such as isopropanol, ether, sherwood oil, liquid paraffin, formaldehyde, glutaraldehyde etc. in the preparation process, and these reagents all have certain toxic and side effects to people and animals, ether , Petroleum ether and other reagents are flammable, explosive, and volatile. There are potential safety hazards when used and pollute the environment.

Method used

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  • Veterinary danofloxacin mesylate slow-release microsphere preparation as well as preparation method and application of veterinary danofloxacin mesylate slow-release microsphere preparation
  • Veterinary danofloxacin mesylate slow-release microsphere preparation as well as preparation method and application of veterinary danofloxacin mesylate slow-release microsphere preparation
  • Veterinary danofloxacin mesylate slow-release microsphere preparation as well as preparation method and application of veterinary danofloxacin mesylate slow-release microsphere preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0042] The preparation method of the present embodiment dafloxacin mesylate sustained-release microspheres is as follows:

[0043] (1) Accurately weigh 1.56 g of zinc acetate and 2.1 g of calcium chloride, and dissolve them in 35 mL of deionized water to obtain a cross-linking agent containing 6% calcium chloride and 4% zinc acetate.

[0044] (2) Accurately weigh 2.0 g of sodium alginate (Sigma-Aldrich, the same below), add 100 mL of deionized water, stir until completely dissolved, then add 0.2 g of sodium bisulfite, and magnetically stir until completely dissolved in a 50°C water bath dissolved to obtain a 2.0% sodium alginate solution.

[0045] (3) Accurately weigh 2.0 g of dafloxacin mesylate crude drug (purity 100.5%, purchased from Zhejiang Xinchang Guobang Veterinary Medicine Factory, the same below), dissolve it with 4-5 mL of deionized water, and add it to step (2) ) in the sodium alginate solution obtained, magnetically stirred under the condition of a water bath at...

Embodiment 2

[0054] The preparation method of the present embodiment dafloxacin mesylate sustained-release microspheres is as follows:

[0055] (1) Accurately weigh 1.56 g of zinc acetate and 2.8 g of calcium chloride, dissolve them in 35 mL of deionized water, and obtain a cross-linking agent containing 8% calcium chloride and 4% zinc acetate.

[0056] (2) Accurately weigh 2.0g of sodium alginate, add 100mL of deionized water, stir until completely dissolved, then add 0.2g of sodium bisulfite, stir magnetically in a water bath at 50°C until completely dissolved, and obtain 2.0% sodium alginate solution.

[0057] (3) Accurately weigh 2.0 g of dafloxacin mesylate crude drug with a purity of 100.5% (the source manufacturer is the same as in Example 1), dissolve it in 4 to 5 mL of deionized water, and add it to the sodium alginate solution obtained in (2). , 50 ° C under the condition of a water bath, magnetic stirring, so that it is evenly mixed to obtain an aqueous solution.

[0058] (4) ...

Embodiment 3

[0065] The preparation method of the present embodiment dafloxacin mesylate sustained-release microspheres is as follows:

[0066] (1) Accurately weigh 1.56 g of zinc acetate and 2.8 g of calcium chloride, dissolve them in 35 mL of deionized water, and obtain a cross-linking agent containing 8% calcium chloride and 4% zinc acetate.

[0067] (2) Accurately weigh 2.0g of sodium alginate, add 100mL of deionized water, stir until completely dissolved, then add 0.2g of sodium bisulfite, stir magnetically in a water bath at 50°C until completely dissolved, and obtain 2.0% sodium alginate solution.

[0068] (3) Accurately weigh 2.0 g of dafloxacin mesylate crude drug, dissolve it in 4-5 mL of deionized water, add it to the sodium alginate solution obtained in (2), and stir magnetically in a water bath at 50°C to mix Uniformly, an aqueous phase solution was obtained.

[0069] (4) Measure 100 mL of soybean oil for injection, add 5.0 g of span-80, and stir evenly to obtain an oil phas...

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Abstract

The invention relates to a veterinary danofloxacin mesylate slow-release microsphere preparation as well as a preparation method and application of the veterinary danofloxacin mesylate sow-release microsphere preparation. The veterinary danofloxacin mesylate slow-release microsphere preparation comprises effective components in percentage by weight: 11.45-21.01 percent of danofloxacin mesylate and 78.99-88.55 percent of sodium alginate polysaccharide cross-linking polymer as a carrier. The veterinary danofloxacin mesylate slow-release microsphere preparation is prepared by adopting an emulsion chemical cross-linking method. The preparation method comprises the following steps of: firstly, mixing the danofloxacin mesylate, sodium alginate and an antioxidant to form an aqueous phase solution; dropping a cross-linking agent under the condition of emulsification and curing to form microsphere; and secondly, carrying out washing, centrifuging, filtering and drying to obtain the danofloxacin mesylate slow-release microsphere preparation of which the average particle size is 8-9mum. The preparation process of the preparation is simple and feasible; raw materials used for the preparation have better biocompatibility, biodegradability and stability; the prepared danofloxacin mesylate slow-release microsphere preparation has the characteristics of safety, no toxicity, high drug-loading rate (11.45-21.01 percent), high encapsulation rate (59.54-88.20 percent), long-acting effect, slow release and the like; after the danofloxacin mesylate slow-release microsphere preparation is injected in swine muscle, the effective concentration can be maintained for several days; and the veterinary danofloxacin mesylate slow-release microsphere preparation is suitable for treating respiratory tract and digestive tract infection of livestock caused by sensitive bacteria.

Description

technical field [0001] The invention relates to the technical field of preparation of new dosage forms of veterinary drugs, in particular to a veterinary dafloxacin mesylate sustained-release microsphere preparation and a preparation method and application thereof. Background technique [0002] Danofloxacin mesylate is a special fluoroquinolone drug for animals. It was successfully developed and launched by Pfizer of the United States in 1988 and has been widely used in the world. Dafloxacin mesylate has a wide antibacterial spectrum, strong bactericidal activity, low toxicity, good water solubility, wide distribution in the body, no cross-resistance with other antibacterial drugs, can be administered in multiple ways, absorbs rapidly, and has high bioavailability high. The drug shows strong antibacterial activity against Gram-positive bacteria, Gram-negative bacteria, intracellular pathogens, mycoplasma and some drug-resistant strains, and is often used in the treatment of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4709A61K47/36A61P31/04
Inventor 袁宗辉方萤玉王玉莲潘源虎黄玲利陶燕飞陈冬梅彭大鹏戴梦红刘振利
Owner HUAZHONG AGRI UNIV
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