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Mezlocillin sodium compound and medicine composition thereof

A technology of mezlocillin sodium and mezlocillin acid, which is applied in the field of medicine and can solve problems such as poor stability

Active Publication Date: 2013-04-03
HUNAN KELUN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The hygroscopicity of mezlocillin sodium prepared by prior art is very strong, thus has caused the shortcoming of poor stability

Method used

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  • Mezlocillin sodium compound and medicine composition thereof
  • Mezlocillin sodium compound and medicine composition thereof
  • Mezlocillin sodium compound and medicine composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] 1. At 15-18°C, add 100L of a mixture of water and isopropanol (volume ratio 25:1) into the reaction kettle.

[0061] 2. Add 8Kg of ampicillin to the reaction kettle, add 1mol / L sodium bicarbonate solution dropwise while stirring, and stop the dropwise addition after the solution dissolves.

[0062] 3. Add 5Kg of 1-chloroformyl-3-methanesulfonyl-2-imidazolidinone while stirring for condensation reaction, add 1mol / L sodium bicarbonate dropwise during the reaction to control the pH value to 7.9, and keep the temperature at 15 ℃, the stirring speed is 250 rpm, and the reaction is continued for 45 minutes after the addition is completed, then the solution is filtered, and the filtrate is transferred to a crystallization tank.

[0063] 4. Add 40L of a mixture of ethanol and isopropanol (volume ratio 10:1) to the crystallization kettle, stir to mix it evenly with the feed liquid, keep the temperature at 20°C, and adjust with dilute hydrochloric acid (9.5~10.5% by weight) pH t...

Embodiment 2

[0065] 1. Add 10Kg of mezlocillin acid to 40L of water for injection, stir evenly, and cool down to 8°C.

[0066] 2. Add dropwise the mixed aqueous solution of sodium bicarbonate and sodium hydroxide (sodium bicarbonate 10%w / w, sodium hydroxide 2%w / w), adjust the pH value to 5.5, stir the reaction until the solution is completely clear and continue to stir for 30 minutes , add 5% mezlocillin acid by weight activated carbon, stir for 20 minutes, filter to remove carbon, and filter the filtrate through a 0.22 μm filter membrane to sterilize.

[0067] 3. Put the filtrate in a freeze-drying tray with a thickness of 12mm, pre-freeze at -35°C for 3 hours, then continue to cool down to -45°C, keep it for 1 hour, and then start vacuum drying. The first stage: adjust the vacuum to 35Pa , slowly warm up to -10°C (heating time 6 hours), keep at -10°C for 1 hour; second stage: slowly heat up to 0°C (≤0.1°C / min), keep at 0°C for 1 hour; third stage : 12 hours, the temperature was raised t...

Embodiment 3

[0072] Prescription: (Specification: 0.5g)

[0073] Mezlocillin sodium compound 500g (calculated as mezlocillin)

[0074] Make 1000 pieces

[0075] Process:

[0076] 1. Aseptically pass the mezlocillin sodium compound through an 80-mesh sieve under 100-grade conditions in a sterile room, and weigh the prescription amount for use.

[0077] 2. Calculate the content and fill it according to the specification to get the finished product.

[0078] The preparation of embodiment 4 injection mezlocillin sodium

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Abstract

The invention relates to a mezlocillin sodium compound which is determined by adopting X-ray powder diffraction and has characteristic peaks shown in 2theta of 8.9, 15.7, 16.5, 18.9, 19.8, 24.6, 26.4, 27.8, 29.0, 29.7, 31.8, 33.2, 34.7, 36.8, 37.5, 38.9 and 40.1 in a map. The invention also relates to a mezlocillin sodium compound and a medicine composition with a medicine active component of the mezlocillin sodium compound or the mezlocillin sodium compound and sulbactam sodium or tazobactam sodium. The medicine composition is a powder injection of the mezlocillin sodium compound, or a medicine mixture powder injection of the mezlocillin sodium compound and the sulbactam sodium or tazobactam sodium. The mezlocillin sodium compound has the advantages of difficulty in absorbing mixture, good flowability, high dissolving speed, kept extremely high stability, and greatly improved convenience and safety of the mezlocillin sodium.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a mezlocillin sodium compound and a pharmaceutical composition thereof. Background technique [0002] Mezlocillin sodium chemical name (2S, 5R, 6R)-3,3-dimethyl-6-[(R)-2[3-(methylsulfonyl)-2-oxo-1-imidazolidinecarboyl Amino]-2-phenylacetamido]-7-oxo-4-thia-1-azabicyclo[3.2.0]-heptane-2-carboxylic acid sodium salt, a high-potency benzazole penicillin antibiotic, obtained from gastric Intestinal absorption is difficult, and its sodium salt is often used for parenteral administration. The antibacterial effect of this product is similar to that of carbenicillin, but its scope of action is wider, and its antibacterial spectrum is also wider than that of natural penicillin. Mezlocillin is a penicillin derivative administered parenterally, and it has a bactericidal effect in large doses. The antibacterial spectrum of mezlocillin is basically the same as that of ampicillin...

Claims

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Application Information

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IPC IPC(8): C07D499/68C07D499/16C07D499/12A61K31/431A61K31/43A61P31/04
Inventor 曾艺胡成忠
Owner HUNAN KELUN PHARMA
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