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Trometamol salt in compound of cillin category, and preparation method

A technology of cillin tromethamine salt and azlocillin tromethamine salt, which is applied in the field of derivatives of cillin antibiotic compounds and their preparation, and can solve problems such as incompatibility, hypernatremia, and high risk

Inactive Publication Date: 2007-07-25
GUANGDONG ZHONGKE DRUG R&D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many problems in the use process, such as: 1) there is vascular irritation, and long-term use can easily cause symptoms such as vasculitis; 2) most of them exist in the form of sodium salts, and sodium ions enter the human body in such a large amount Patients with diabetic bacterial infection, neurosurgery patients with severe neurosurgery, patients with heart and kidney insufficiency, or patients with high blood pressure are at high risk, which can easily cause hypernatremia and cause adverse reactions; 3) Some varieties have incompatibility and are inconvenient to use; 4) Muscle There is muscle irritation when injecting; etc.

Method used

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  • Trometamol salt in compound of cillin category, and preparation method
  • Trometamol salt in compound of cillin category, and preparation method
  • Trometamol salt in compound of cillin category, and preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Embodiment 1: the preparation of azlocillin trometamol

[0045] In a 250ml three-necked flask, add 12.1g (0.1mol) of tromethamine and 20ml of 60% ethanol, and drop into 20ml of 80% ethanol solution containing 46.2g (0.1mol) of azlocillinic acid under high temperature stirring, and stir until The mixture was clarified, stirred at room temperature for 2 hours, and the mixed reactants were dropped into 300ml (5-10°C) acetone solution to obtain white powdery crystals. The solid powder was filtered with suction, and the solid was washed with a small amount of acetone. Vacuum drying under the condition of phosphorus oxide for 24 hours yielded 51.3 g of powdery solid with a yield of 88.0%. Content analysis: (HPLC method) contained 79.0-80.8% of azlocillinic acid. The product was analyzed by elements (theoretical value: C49.4% H6.0% N14.4% O24.7% S5.5%; measured value: C49.6% H5.8% N14.7% O24.5% S5. 4%), NMR, MS, UV, IR and HPLC analysis, the product is azlocillin tromethamine...

Embodiment 2

[0046] Embodiment 2: the preparation of amoxicillin tromethamine

[0047] In a 250ml three-necked flask, add 12.1g (0.1mol) of tromethamine, 4ml of methanol, and 2ml of water, stir at high temperature, add 33.3g (0.1mol) of amoxicillin, stir until it is completely dissolved, and then stir for 2 hours. Dropped into 500ml of acetone at high temperature, a large amount of white crystalline powder was precipitated, the solid was filtered by suction, washed with a small amount of acetone, and dried at high temperature under phosphorus pentoxide for 24 hours to obtain 29.8g of white crystalline amoxicillin tromethamine. Yield: 89.5%, content analysis (HPLC method): containing 72.6-74.0% of amoxicillin acid. The product was analyzed by elements (theoretical value: C52.9% H6.6% N11.9% O21.1% S7.0%; measured value: C52.7% H6.5% N12.2% O21.3% S6. 8%), NMR, MS, UV, IR and HPLC analysis, the product is amoxicillin tromethamine salt, and the purity is 99.4% in terms of amoxicillin.

Embodiment 3

[0048] Embodiment 3: the preparation of ampicillin tromethamine

[0049] In a 250ml three-necked flask, add 12.1g (0.1mol) of tromethamine, 4ml of methanol, and 2ml of water, stir at high temperature, add 34.9g (0.1mol) of ampicillin, stir to completely dissolve and then stir for 1 hour, put the mixture in Drop it into 500ml of acetone at high temperature to precipitate a large amount of white crystalline powder, filter the solid with suction, wash with a small amount of acetone, and dry at high temperature under phosphorus pentoxide for 24 hours to obtain 41.7g of white crystalline ampicillin tromethamine salt. Yield: 88.8%, content analysis (HPLC method): containing 73.8-75.0% of ampicillin acid. The product was analyzed by elements (theoretical value: C51.1% H6.4% N11.9% O23.8% S6.8%; measured value: C51.2% H6.5% N12.0% O23.6% S6. 7%), NMR, MS, UV, IR and HPLC analysis, the product is ampicillin tromethamine salt, and the purity in terms of ampicillin is 99.2%.

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PUM

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Abstract

This invention discloses trometamol salts of cillin compounds, or their hydrates that can be used to treat bacillosis. As hown in formula 1, the salts comprise trometamol salts of azlocillin, amoxicillin, ampicillin, oxazacillin, furbucillin, cloxacillin, mezlocillin, mecillinam, piperacillin, ticarcillin, floxacillin, hetacillin, cloxacillin and penicillin. This invention provides drug compositions with the salts shown in formula 1 as the active components, and their application in drugs for treating bacillosis.

Description

Technical field: [0001] The invention belongs to the medical field of compounds, and relates to derivatives of cillin antibiotic compounds and a preparation method thereof. Background technique: [0002] Penicillin drugs belong to the penicillin class of antibiotics, including aminopenicillins (including ampicillin, amoxicillin, bamicillin, pampicillin, etc.), and are mainly used for penicillin-sensitive Gram-positive bacteria and some Gram-negative bacteria such as large intestine Bacillus, Proteus mirabilis, Salmonella, Shigella and influenza bacilli, etc.; anti-staphylococcal penicillins (including cloxacillin, dicloxacillin, oxacillin, flucloxacillin, methicillin, nafcillin, etc.) , also has a good effect on β-lactamase-producing Staphylococcus; anti-pseudomonal penicillins (including carbenicillin, mezlocillin, piperacillin, ticarcillin, etc.), have a more natural effect on grass-positive bacteria Penicillin or aminopenicillin is poor, but has antibacterial activity ag...

Claims

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Application Information

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IPC IPC(8): C07D499/44C07D499/74C07D499/76A61K31/43A61K31/431A61P31/04
Inventor 陈文展王伟
Owner GUANGDONG ZHONGKE DRUG R&D
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