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Ticarcillin disodium hydrate and preparation method as well as application thereof

A technology of ticarcillin disodium and hydrate, which is applied in the directions of active ingredients of heterocyclic compounds, pharmaceutical formulations, medical preparations containing active ingredients, etc., and can solve the unpublished literature report on the preparation method of ticarcillin disodium hydrate. and uses, etc., to achieve the effect of improving bioavailability, improving operability, and good dissolution performance

Inactive Publication Date: 2012-01-11
胡梨芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the published literature only reports Ticarcillin disodium (Ticarcillin disodium) (C 15 h 14 N 2 Na 2 o 6 S 2 , Molecular Weight: 428.39, CAS No.: 4697-14-7), so far, there is no published literature at home and abroad to report ticarcillin disodium hydrate of the present invention and its preparation method and use

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Preparation of ticarcillin disodium monohydrate Add 10 g of ticarcillin acid and 100 ml of water in a reaction flask, stir, add triethylamine dropwise at 5°C, stir, make the pH to about 8.1, stir, 5 Add dropwise an ethanol solution of 28% sodium isooctanoate (8.83g) at ℃, stir for about 1 hour, slowly add 250ml of acetone and 250ml of ethanol dropwise, place below -5℃ to fully separate out the solid, filter with suction, wash with a small amount of ethanol and chloroform 3 times, filter with suction, dissolve the obtained solid with a small amount of water, add 200ml of acetone, 100ml of ethanol, and 30ml of chloroform as the crystallization solvent for recrystallization, place it below -5°C to fully separate the crystals, filter with suction, and vacuum at about 40°C After drying for about 5 hours, 6.1 g of off-white crystals were obtained. Specific rotation: +182°. Karl Fischer’s method determined that the water content was 4.1%. Thermal analysis: the weight ...

Embodiment 2

[0031]Example 2 Preparation of ticarcillin disodium monohydrate Add 10 g of ticarcillin monosodium monohydrate and 80 ml of water to the reaction flask, stir, add saturated sodium carbonate aqueous solution dropwise at 5°C to bring the pH to 8.0, stir for 30 Minutes, add 0.2g of activated carbon, stir for 30 minutes, filter with suction, wash with water, filter with suction, slowly add 300ml of acetone, 200ml of acetonitrile, and 40ml of chloroform to the filtrate dropwise, and place it below -10°C to fully separate out the solid, filter with suction, and wash with chloroform for 3 times , suction filtration, the obtained solid was just dissolved with a small amount of water, added 300ml of acetone, 200ml of acetonitrile, 10ml of ether, and 50ml of chloroform as crystallization solvents for recrystallization, and placed below -10°C overnight to allow the crystals to be fully analyzed. Suction filtration, 40°C After vacuum drying for about 5 hours, 5.9 g of off-white crystals we...

Embodiment 3

[0032] Example 3 Preparation of ticarcillin disodium 0.5 hydrate Add 20 g of ticarcillin acid and 130 ml of water into the reaction flask, stir, add saturated sodium bicarbonate solution dropwise to the filtrate at 5°C to bring the pH to 7.9, and stir for 30 minutes , add 0.2g of activated carbon, stir for 30 minutes, filter with suction, wash with water, and filter with suction, slowly add 500ml of acetone, 150ml of ether, and 30ml of chloroform to the filtrate, and place it below -5°C to allow the solid to fully separate out, filter with suction, wash with acetone and chloroform 3 times, suction filtration, the obtained solid was just dissolved with a small amount of water, recrystallized with 300ml of acetone, 300ml of isopropanol, and 30ml of chloroform as the crystallization solvent, and placed overnight at -5°C to allow the crystals to be fully analyzed. Suction filtration, 45 After vacuum drying at ℃ for about 24 hours, 12.1 g of off-white crystals were obtained, specifi...

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PUM

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Abstract

The invention relates to a ticarcillin disodium hydrate and a preparation method as well as application thereof. The ticarcillin disodium hydrate has high storage stability and is applied to preparing medicaments for treating or preventing diseases caused by grampositive or gramnegative sensitive bacteria, for example, superficial secondary infection such as diseases of human or animal respiratory system, hepatobiliary system and five sense organs, urinary tract infection, abdominal infection, pelvic infection, blood poisoning, skin soft tissue infection, bone and joint infection, gynecological infection, blood poisoning, burn, surgical incision and the like, typhoid, leucocythemia, secondary infection of malignancy patients and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides an antibacterial drug-ticarcillin disodium hydrate, a preparation method and application thereof. Background technique [0002] Ticarcillin disodium (2S, 5R, 6R)-6-[[(2R)-carboxy-3-thienylacetyl]amino]-3,3-dimethyl-7-oxo-4 -Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid disodium salt, a semi-synthetic penicillin, highly effective against Pseudomonas aeruginosa, 2 to 4 times stronger than carbenicillin. It is stable to the β-lactamase produced by clinically isolated drug-resistant Pseudomonas aeruginosa, but it is easily destroyed by the β-lactamase produced by Escherichia coli, Proteus mirabilis and individual strains of Pseudomonas aeruginosa. The role of ampicillin is small, 1 / 20 to 1 / 10 of ampicillin. Combined with gentamicin and polymyxin, it has a synergistic effect on Pseudomonas aeruginosa. It is not absorbed orally, and the blood concentration reaches its ...

Claims

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Application Information

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IPC IPC(8): C07D499/72C07D499/16A61K31/431A61K31/43A61K31/424A61P31/04
CPCY02A50/30
Inventor 刘力
Owner 胡梨芳
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