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Magnesium ceftiofur as well as preparation method and using method thereof

A technology of ceftiofur and ceftiofur hydrochloride, which is applied in pharmaceutical formulas, medical preparations containing active ingredients, antibacterial drugs, etc., can solve the problem of slow metabolism of benzylethylenediamine ceftiofur and achieve effective blood drug concentration , low technical threshold and other issues, to achieve the effect of prolonging the drug action time, improving drug value and low cost

Active Publication Date: 2015-05-13
SIVEA QINGDAO BIOPHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are also many defects in these patents. The technical thresholds of the aforementioned three patents are relatively low, and it is easy for those skilled in the art to break through. The last patent is due to the very slow metabolism of benzylethylenediamine ceftiofur. The disadvantage is that it is difficult to achieve effective blood drug concentration in a short time, so further optimization and improvement are needed

Method used

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  • Magnesium ceftiofur as well as preparation method and using method thereof
  • Magnesium ceftiofur as well as preparation method and using method thereof
  • Magnesium ceftiofur as well as preparation method and using method thereof

Examples

Experimental program
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Effect test

preparation Embodiment 1

[0028] The preparation method of Ceftiofur Magnesium of the present invention comprises the following steps:

[0029] (1) Add 1 mol (560 g) of ceftiofur hydrochloride into 2240 ml of tetrahydrofuran and stir thoroughly; then add 224 ml of water for injection and fully stir to obtain solution A;

[0030] (2) in solution A, add 0.5mol (20.15g) gradually and the magnesia superfine powder that particle size is 150 microns, stir while adding, react to obtain solution B, promptly contain product ceftiofur magnesium in solution B;

[0031] (3) filter solution B, get upper layer solution C 2000mL; add the carbon tetrachloride that is equal to the volume of upper layer solution C and fully extract solution C, obtain extraction solution 2000mL;

[0032] (4) Evaporate the extract to dryness at 37°C and 10kPa to obtain a white powder; wash the white powder with 1500 mL of acetone three times, 500 mL each time, and evaporate to dryness to obtain 550 g of ceftiofur magnesium.

[0033] The ...

Embodiment 2

[0061]Metabolic kinetics experiment of ceftiofur magnesium in cows

[0062] 1. Injection Preparation

[0063] Prepare the obtained ceftiofur magnesium (W / W, 10%) with soybean oil for injection (W / W, 20%), propylene glycol (W / W, 11%), PEG-200 (W / W, 9%), Lecithin (W / W, 7%), Ethyl Oleate (W / W, 13%), Cyclodextrin (W / W, 9%), Water for Injection (W / W, 21%) After mixing, an injection solution with a mass fraction of 10% is prepared, and the injection solution is a suspension.

[0064] 2. Materials and Reagents

[0065] High-performance liquid chromatography, adult Holstein lactating cows, disposable syringes, blood collection devices, 10% ceftiofur magnesium injection, and imported ceftiofur injection (Yizuda) were used as control drugs.

[0066] 3. Experimental operation

[0067] Take 20 adult Holstein lactating cows that have not been treated with any antibiotics within one month. After collecting 5ml blood samples, divide them into 2 groups, 10 cows in each group; According t...

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Abstract

The invention relates to magnesium ceftiofur, and belongs to the field of special curative activity of a compound or a pharmaceutical preparation. The magnesium ceftiofur is prepared by virtue of ceftiofur hydrochloride and medicinal oxidase, and the structural formula of the magnesium ceftiofur is provided. Meanwhile, the invention provides a preparation method and a using method of the magnesium ceftiofur; the magnesium ceftiofur disclosed by the invention has a same antibacterial activity as the ceftiofur hydrochloride and the magnesium ceftiofur has the properties of antibiotics; the action time of drugs can be prolonged through magnesium ions; meanwhile, the magnesium ceftiofur can supplement magnesium ions to a human body, so that the medicinal value of the magnesium ceftiofur is improved; and the magnesium ceftiofur disclosed by the invention is simple in preparation process, low in cost and applicable to industrial production.

Description

technical field [0001] The invention relates to ceftiofur magnesium, which belongs to the field of specific therapeutic activity of compounds or pharmaceutical preparations. Background technique [0002] Ceftiofur is the first third-generation cephalosporin antibiotic synthesized in the 1980s for use in animals. It has broad-spectrum and potent antibacterial effects on both Gram-positive and Gram-negative bacteria. Ceftiofur is a semi-synthetic antibiotic, which is mainly made into sodium salt freeze-dried powder and hydrochloride suspension to treat animal bacterial diseases. At present, the ceftiofur preparations reported in the market and literature include ceftiofur hydrochloride suspension injection, ceftiofur sodium powder injection or freeze-dried powder injection, ceftiofur crystal suspension injection and ceftiofur dibenzyl ethyl Diamine salt preparations. The above-mentioned preparations have been proved to be safe, efficient and stable preparation forms through ...

Claims

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Application Information

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IPC IPC(8): C07D501/36C07D501/04A61K31/546A61P31/04
Inventor 王荣迁冯展波
Owner SIVEA QINGDAO BIOPHARM CO LTD
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