Cefoperazone sodium-sulbactam sodium eutectic crystal and composition, and preparation methods thereof

A technology of cefoperazone sodium and sulbactam sodium, applied in the direction of active ingredients of heterocyclic compounds, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of short validity period and poor stability, and achieve low content of related substances and crystal form Concentrated particle size distribution, reducing the risk of adverse effects

Active Publication Date: 2015-08-19
SHANDONG LUOXIN PHARMA GRP CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] One of the objects of the present invention is to provide a co-crystal of cefoperazone sodium and sulbactam sodium and its preparation method and application thereof. existing problems

Method used

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  • Cefoperazone sodium-sulbactam sodium eutectic crystal and composition, and preparation methods thereof
  • Cefoperazone sodium-sulbactam sodium eutectic crystal and composition, and preparation methods thereof
  • Cefoperazone sodium-sulbactam sodium eutectic crystal and composition, and preparation methods thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0036] Embodiment 1: Preparation of cefoperazone sodium and sulbactam sodium cocrystal:

[0037] Add cefoperazone sodium (13.35g, 0.02mol) and sulbactam sodium (5.10g, 0.02mol) to a volume ratio of 6.5:3:0.5 water:ethanol:acetone solution that is 10 times the weight of cefoperazone sodium and sulbactam sodium During the process, control the temperature at 10-20°C and ultrasonically dissolve it; after the dissolution is clear, add tetrahydrofuran whose volume is 1 times the weight of cefoperazone sodium and sulbactam sodium at a constant speed under stirring at 15-20rmp, and control the dropping time for 10-15 minutes; After finishing, stir and lower the temperature, the stirring and cooling is stirring at a rotating speed of 25-30rmp for 5 minutes to cool down to 0-10°C, then stirring at a rotating speed of 10-12rmp for 5 minutes to cool down to -5-0°C, and standing for 20-30 hours , filtered, washed twice with ethanol:tetrahydrofuran solution with a volume ratio of 5:5, 0.2 t...

Embodiment 2

[0060] Embodiment 2: the preparation of cefoperazone sodium and sulbactam sodium cocrystal:

[0061] Add cefoperazone sodium (26.7g, 0.04mol) and sulbactam sodium (10.2g, 0.04mol) to a volume ratio of 6.5:3:0.5 water:ethanol:acetone solution that is 20 times the weight of cefoperazone sodium and sulbactam sodium In the process, control the temperature at 10-20°C and ultrasonically dissolve it; after the dissolution is clear, add tetrahydrofuran whose volume is twice the weight of cefoperazone sodium and sulbactam sodium at a constant speed under stirring at 15-20rmp, and control the dropping time for 10-15 minutes; After finishing, stir and lower the temperature, the stirring and cooling is stirring at a rotating speed of 25-30rmp for 5 minutes to cool down to 0-10°C, then stirring at a rotating speed of 10-12rmp for 5 minutes to cool down to -5-0°C, and standing for 20-30 hours , filtered, washed 2 times with a volume ratio of 5:5 ethanol: tetrahydrofuran solution, each 0.5 t...

Embodiment 3

[0062] Embodiment 3: Preparation of cefoperazone sodium and sulbactam sodium co-crystal and mixed crystal of sulbactam sodium:

[0063] Add cefoperazone sodium (26.7g, 0.04mol) and sulbactam sodium (12.8g, 0.055mol) to a volume ratio of 6.5:3:0.5 water:ethanol:acetone solution that is 15 times the weight of cefoperazone sodium and sulbactam sodium During the process, control the temperature at 10-20°C and ultrasonically dissolve it; after the dissolution is clear, add tetrahydrofuran whose volume is 1.5 times the weight of cefoperazone sodium and sulbactam sodium at a constant speed under stirring at 15-20rmp, and control the dropping time for 10-15 minutes; Complete, stirring and cooling down, the stirring and cooling is cooling down to 0-10°C for 5 minutes at a rotating speed of 25-30rmp, then cooling down to -5-0°C for 5 minutes under stirring at a rotating speed of 10-12rmp, and standing for 20-30 hours , filtered, washed twice with ethanol:tetrahydrofuran solution with a ...

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Abstract

The invention relates to a cefoperazone sodium-sulbactam sodium eutectic crystal and a pharmaceutical composition containing the eutectic crystal, and preparation methods thereof. The cefoperazone sodium-sulbactam sodium eutectic crystal has the advantages of concentrated distribution of crystal form grain size, good product fluidity, gloss surface, high degree of crystallinity and good stability; the preparation method of the crystal form is simple in process, easy to operate, and suitable for popularization and application in a wide range. In the compound cefoperazone sodium-sulbactam sodium preparation, through introduction of the cefoperazone sodium-sulbactam sodium eutectic crystal and a phosphate buffer to adjust the pH value, the problems that a mixed powder in the preparation is poor in uniformity, liquidity and raw material stability are solved, generation of carbon dioxide gas due to addition of a stabilizer carbonate is avoided, an obtained powder injection is diluted through conventional transfusion, then dissolved rapidly and does not produce crystallization and degradation products, the solution clarity is in accordance with provisions, the solution pH value has no obvious change, and the contents of cefoperazone sodium and sulbactam sodium are stable.

Description

technical field [0001] The invention relates to the field of co-crystals of compound medicines, in particular to a co-crystal of cefoperazone sodium and sulbactam sodium, a pharmaceutical composition comprising the co-crystal of cefoperazone sodium and sulbactam sodium and a preparation method thereof. Background technique [0002] Cefoperazone sodium mainly inhibits the synthesis of bacterial cell walls. Sulbactam sodium itself has weak antibacterial effect and is a competitive and irreversible β-lactamase inhibitor. After combined application with cefoperazone sodium, it can increase the ability of cefoperazone sodium to resist the degradation of various β-lactamases. produce obvious synergistic effect. The compound preparation of cefoperazone sodium and sulbactam sodium is a broad-spectrum antibacterial drug developed and marketed by Pfizer (trade name: Supushen), which has antagonistic effects on Gram-positive bacteria, negative bacteria and some anaerobic bacteria, esp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/12C07D499/86C07D499/18A61K9/14A61K31/43A61K31/546A61P31/04
CPCA61K9/14A61K31/43A61K31/546C07D499/18C07D499/86C07D501/12C07D501/36A61K2300/00
Inventor 刘明霞李华杨磊祥蒋燕杰
Owner SHANDONG LUOXIN PHARMA GRP CO LTD
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