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Azlocillin sodium crystal preparation and preparation method thereof

A new penicillin and crystal technology, applied in the field of new penicillin crystal preparations and its preparation, can solve the problems of product safety, production safety, safety hazards, poor product stability, and long production cycle, so as to achieve less allergies, good stability, and reduce stimulating effect

Active Publication Date: 2014-11-05
BAIDE LIXI HEALTH CARE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The product obtained by this method is an amorphous powder with poor product stability, long production cycle and high cost
The traditional solvent crystallization process usually requires the use of a large amount of acetone and ethyl acetate solvents, especially acetone has a low flash point, which is very easy to cause combustion
Therefore, the traditional production process of new penicillin has great potential safety hazards both in terms of product safety and production safety.

Method used

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  • Azlocillin sodium crystal preparation and preparation method thereof
  • Azlocillin sodium crystal preparation and preparation method thereof
  • Azlocillin sodium crystal preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Dissolve 1.5kg of commercially available crude penicillin (that is, the purity of new penicillin is not higher than 85%) in a mixed solvent composed of 1.0kg of methanol and 2.0kg of methyl ethyl ketone; stir at room temperature for 1h, then add 100g of activated carbon for adsorption and filter solution, the filtrate was cooled to 0°C, stirred for 1 hour until a large amount of crystals were precipitated; the crystals were washed with a mixed solution of methanol and methyl ethyl ketone (weight ratio 1:2), and dried under reduced pressure at 30°C to obtain the first refined new Penicillin product 1.23kg.

[0030] Add 1.23 kg of neopenicillin obtained above into 30 kg of methyl ethyl ketone solvent (temperature 55° C.), and stir until completely dissolved. Then the solution was filtered through a high-efficiency filter to a crystallization tank, and then the temperature was gradually lowered to 35° C. and concentrated under reduced pressure at this temperature to the re...

Embodiment 2

[0035] Dissolve 1.5kg of commercially available crude penicillin (that is, the purity of new penicillin is not higher than 85%) in a mixed solvent composed of 0.8kg of methanol and 1.6kg of methyl ethyl ketone; stir at room temperature for 1h, then add 100g of activated carbon for adsorption and filter to dissolve liquid, the filtrate was cooled to 2.5°C, and stirred for 1.2h until a large amount of crystals precipitated; the crystals were washed with a mixed solution of methanol and methyl ethyl ketone (1:2 by weight), and dried under reduced pressure at 25°C to obtain the first refined new Penicillin product 1.18kg.

[0036] Add 1.18 kg of neopenicillin obtained above into 25 kg of methyl ethyl ketone solvent (temperature 50° C.), and stir until completely dissolved. Then the solution was filtered through a high-efficiency filter to a crystallization tank, and then the temperature was gradually lowered to 30° C. and concentrated under reduced pressure at this temperature to ...

Embodiment 3

[0039] Dissolve 1.5kg of commercially available crude penicillin (that is, the purity of new penicillin is not higher than 85%) in a mixed solvent composed of 1.5kg of methanol and 3.0kg of methyl ethyl ketone; stir at room temperature for 1h, then add 100g of activated carbon for adsorption and filter to dissolve liquid, the filtrate was cooled to 5°C, and stirred for 1.5h until a large amount of crystals precipitated; the crystals were washed with a mixed solution of methanol and methyl ethyl ketone (1:2 by weight), and dried under reduced pressure at 35°C to obtain the first refined new Penicillin product 1.10kg.

[0040] Add 1.10 kg of neopenicillin obtained above into 35 kg of methyl ethyl ketone solvent (temperature 60° C.), and stir until completely dissolved. Then the solution was filtered through a high-efficiency filter to a crystallization tank, and then the temperature was gradually lowered to 40° C. and concentrated under reduced pressure at this temperature to th...

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Abstract

The invention discloses an azlocillin sodium crystal preparation and a preparation method thereof. The preparation method comprises the following steps: step 1, dissolving a crude azlocillin sodium product in a mixed solvent of methanol and ethyl methyl ketone, adding active carbon for adsorption, carrying out filtering, cooling the obtained filtrate to allow a crystal to be precipitated, washing the crystal with a mixed solution of methanol and ethyl methyl ketone and carrying out pressure-reduced drying so as to obtain a primary refined azlocillin sodium product; and step 2, dissolving the primary refined azlocillin sodium product in a hot ethyl methyl ketone solution, carrying out press filtration with a high-efficiency filter, subjecting obtained mixed liquor to cooling, pressure reduction and concentration, then carrying out cooling to allow a crystal to be precipitated and subjecting the precipitated crystal to filtering and pressure-reduced drying so as to obtain the azlocillin sodium crystal preparation. The azlocillin sodium crystal preparation provided by the invention has the advantages of a small particle size, uniform particle size distribution, good fluidity, simple crystallization process, low residual quantity of the organic solvent, high stability, good security, small toxic and side effects, low proneness to allergy, etc.

Description

technical field [0001] The invention relates to a new penicillin crystal preparation and a preparation method thereof, belonging to the field of pharmaceutical compounds. Background technique [0002] New penicillin (English name: Azlocillin Sodium), its chemical name is: (2S, 5R, 6R)-3,3-dimethyl-6-[(R)-2-(2-oxo-1-imidazole Alkylcarboxamido)-2-phenylacetamido]-7-oxo-4-thia-1-azabicyclo[3,2,0]heptane-2-carboxylic acid sodium salt. Molecular formula: C20H22N5NaO6S, molecular weight: 483.47, and the structural formula is as follows. [0003] [0004] New penicillin (C20H22N5NaO6S) is a new semi-synthetic ureido penicillin with certain acid resistance. C20H23N5O6S is effective against Gram-positive and negative bacteria, and its effect is similar to that of piperacillin and mezlocillin, while its effect on Pseudomonas aeruginosa is more than 10 times that of ordinary penicillin. Its good antibacterial activity makes it a good choice for treating infectious diseases. One o...

Claims

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Application Information

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IPC IPC(8): C07D499/68C07D499/18A61K31/431A61P31/04
CPCC07B2200/13C07D499/18C07D499/68
Inventor 王建雅克·杜马保罗·埃利希
Owner BAIDE LIXI HEALTH CARE
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