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Injection-use pharmaceutical composition comprising cefathiamidine and tazobactam sodium

A technology of tazobactam sodium and cefathiamidine, which is applied to the active ingredients of heterocyclic compounds, antibacterial drugs, pharmaceutical formulations, etc., can solve the differences in inhibition enzyme spectrum and stability, and the degree of optimization of antibacterial activity cannot be accurately predicted. Antibacterial activity is greatly affected, and the effect of excellent stability, wide range of storage conditions and high antibacterial activity is achieved.

Active Publication Date: 2014-09-03
FUAN PHARM (GRP) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The pharmaceutical composition of some β-lactam antibiotics and β-lactamase inhibitors has been disclosed in the prior art, but because different β-lactam antibiotics have specific antibacterial spectrum, different β-lactamase The inhibitory spectrum and stability of the inhibitors are also different, resulting in the pharmaceutical composition including β-lactam antibiotics and β-lactamase inhibitors, the degree of optimization of the antibacterial activity cannot be accurately predicted
Moreover, different dosage ratios have a great impact on the antibacterial activity of the composition of β-lactam antibiotics and β-lactamase inhibitors, and there is no fixed rule to follow in the many teachings given by the prior art.

Method used

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  • Injection-use pharmaceutical composition comprising cefathiamidine and tazobactam sodium
  • Injection-use pharmaceutical composition comprising cefathiamidine and tazobactam sodium
  • Injection-use pharmaceutical composition comprising cefathiamidine and tazobactam sodium

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]

[0030] Add cefathiamidine, L-arginine and tazobactam sodium to 800ml water for injection in sequence, stir and dissolve to obtain the inner water phase W1; mix PLGA (molecular weight about 6000, LA:GA polymerization ratio 50:50), Tween Dissolve in 1200 methylene chloride / acetone with a volume ratio of 3:1 to obtain the oil phase; add PVP, mannitol and glycine to 800 water for injection and stir until completely dissolved to obtain the external water phase W2; slowly add W1 under stirring In the oil phase, ultrasonically treat for 20s under ice bath to obtain colostrum; slowly add colostrum into W2 and stir for 10 minutes to obtain double emulsion, pour the double emulsion into 1500ml of sodium chloride aqueous solution for injection, stir in ice bath for 4 hours to evaporate residual organic solvent , the microspheres were collected by filtration through a 0.45 μm microporous membrane, washed three times with water for injection, and vacuum freeze-dried.

Embodiment 2

[0032]

[0033] Add cefathiamidine, L-arginine and tazobactam sodium to 800ml water for injection in turn, stir and dissolve to obtain the inner water phase W1; mix PLGA (molecular weight about 5500, LA:GA polymerization ratio 50:50), Tween Dissolve in 1200ml of dichloromethane / acetone with a volume ratio of 3:1 to obtain the oil phase; add PVP, mannitol and glycine to 800ml of water for injection and stir until completely dissolved to obtain the external water phase W2; slowly add W1 under stirring In the oil phase, ultrasonically treat for 20s under ice bath to obtain colostrum; slowly add colostrum into W2 and stir for 10 minutes to obtain double emulsion, pour the double emulsion into 1500ml of sodium chloride aqueous solution for injection, stir in ice bath for 4 hours to evaporate residual organic solvent , the microspheres were collected by filtration through a 0.45 μm microporous membrane, washed three times with water for injection, and vacuum freeze-dried.

Embodiment 3

[0035]

[0036] Add cefathiamidine, L-arginine and tazobactam sodium to 1000% water for injection in turn, stir and dissolve to obtain the inner water phase W1; PLGA (molecular weight is about 5000, LA:GA polymerization ratio 50:50), Tween Dissolve in 1200ml of dichloromethane / acetone with a volume ratio of 3:1 to obtain the oil phase; add PVP, mannitol and glycine to 800ml of water for injection and stir until completely dissolved to obtain the external water phase W2; slowly add W1 under stirring In the oil phase, ultrasonically treat for 20s under ice bath to obtain colostrum; slowly add colostrum into W2 and stir for 10 minutes to obtain double emulsion, pour the double emulsion into 1500ml of sodium chloride aqueous solution for injection, stir in ice bath for 4 hours to evaporate residual organic solvent , the microspheres were collected by filtration through a 0.45 μm microporous membrane, washed three times with water for injection, and vacuum freeze-dried.

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Abstract

The invention provides an injection-use pharmaceutical composition comprising cefathiamidine and tazobactam sodium, and the pharmaceutical composition has a cooperatively antibacterial effect. The pharmaceutical composition comprises the following ingredients: by weight, 1-4 parts of the cefathiamidine, 1-2 parts of the tazobactam sodium, 2-6 parts of PLGA; 0.2-0.5 parts of L-arginine; 0.5-1 parts of PVP; 0.5-1 parts of mannitol; 0.5-1 parts of glycine; and 1-2 parts of tween. The pharmaceutical composition has the advantages of high stability, good redissolubility, simple preparation processes, a good inhibitory effect on staphylococcus aureus, staphylococcus epidermidis and staphylococcus epidermidis, and a definite curative effect, can reduce the dosage of a single prescription preparation and shorten the treatment period, and has broad market prospects.

Description

technical field [0001] The invention relates to a compound preparation of β-lactam antibiotics and β-lactamase inhibitors, in particular to a pharmaceutical composition of cefathiamidine for injection and tazobactam sodium. Background technique [0002] β-lactam antibiotics (β-lactams) refer to a large class of antibiotics with a β-lactam ring in their chemical structure, including the most commonly used penicillins and cephalosporins in clinical practice, as well as the newly developed cephamycins and thiomycetes. Other atypical β-lactam antibiotics such as steroids and monocyclic β-lactams. Such antibiotics have the advantages of strong bactericidal activity, low toxicity, wide indications and good clinical curative effect. The chemical structure of this class of drugs, especially the change of the side chain, has formed many antibiotics with different antibacterial spectrum and antibacterial effect and various clinical pharmacological properties. [0003] Cefathiamidine...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/545A61K9/19A61P31/04A61K31/431
Inventor 洪荣川郭子维张静芳徐霞陈小勇
Owner FUAN PHARM (GRP) CO LTD
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