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Children sulbenicillin sodium compound entity and pharmaceutical preparation thereof

A technology of sulbenicillin sodium and compounds, which is applied in the field of pharmaceutical compounds, can solve the problems of poor stability of sulbenicillin sodium, occurrence of degradation products, easy discoloration of appearance, etc., and achieve good clarity, improved solubility, and less toxic and side effects

Inactive Publication Date: 2015-09-30
ZHEJIANG CHANGDIAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the sulfbenicillin sodium prepared by the above method has poor performance stability, and is unstable to heat, acidic environment, and alkaline environment. It is manifested in problems such as easy discoloration of the appearance, reduction of content, and occurrence of degradation products. The reasons for the occurrence may be The impact of some impurities in the finished product of sulbenicillin sodium that cannot be removed by crystallization

Method used

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  • Children sulbenicillin sodium compound entity and pharmaceutical preparation thereof
  • Children sulbenicillin sodium compound entity and pharmaceutical preparation thereof
  • Children sulbenicillin sodium compound entity and pharmaceutical preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 100 g of the crude product of sulfbenicillin sodium, add 1000 ml of purified water, heat up to 30°C until completely dissolved, add 10 g of activated carbon, stir to decolorize, and filter to obtain the filtrate.

[0027] Add 5ml of ethyl acetate to the above filtrate under stirring, transfer to a 1000ml pressure-resistant container, make sure it is full and the air bubbles are removed, seal the container, oscillate, freeze at -20°C for 2 hours, and take it out.

[0028] Separate the liquid from the solid, discard the ethyl acetate solution, transfer to a crystallization tank after the ice melts, add 5000ml of acetone dropwise at 5°C for about 1 hour, stir at a slow speed for 30 minutes, continue to grow crystals for 1 hour, filter with suction, wash with acetone, After vacuum drying at 40°C, the finished product of sulbenicillin sodium was obtained with a purity of 99.4%.

Embodiment 2

[0030] Weigh 100 g of the crude product of sulfbenicillin sodium, add 500 ml of purified water, heat up to 30°C until completely dissolved, add 7 g of activated carbon, stir to decolorize, and filter to obtain the filtrate.

[0031] Add 5ml of chloroform to the above filtrate under stirring, transfer it to a 500ml pressure-resistant container, make sure it is full and the air bubbles are removed, seal the container, oscillate, freeze at -15°C for 5 hours, and take it out.

[0032] Separate the liquid from the solid, discard the chloroform solution, transfer to the crystallization tank after the ice melts, add 2000ml of acetone dropwise at 5°C for about 1 hour, stir at a slow speed for 30min, continue to grow crystals for 1h, filter with suction, wash with acetone, 45°C After vacuum drying, the finished product of sulbenicillin sodium was obtained with a purity of 99.5%.

Embodiment 3

[0034] Weigh 100 g of the crude product of sulfbenicillin sodium, add 350 ml of purified water, heat up to 30°C until completely dissolved, add 3 g of activated carbon, stir to decolorize, and filter to obtain the filtrate.

[0035] Add 2.3ml of ethyl acetate and 2.3ml of chloroform mixed solvent to the above filtrate under stirring, transfer to a 350ml pressure-resistant container, make sure it is full and air bubbles are removed, seal the container, oscillate, freeze at -10°C for 8 hours, and then take it out.

[0036] Separate the liquid from the solid, and discard the mixed solution of ethyl acetate and chloroform. After the ice melts, transfer it to a crystallization tank, add 1050ml of acetone dropwise at 5°C for about 1 hour, stir at a slow speed for 30 minutes, continue to grow crystals for 1 hour, and filter with suction. After washing with acetone and vacuum drying at 50°C, the finished product of sulbenicillin sodium was obtained with a purity of 99.4%.

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Abstract

The present invention discloses a children sulbenicillin sodium compound entity, wherein the original research tradename is Lilacillin, and the chemical structural formula of the compound entity is defined in the specification. The preparation steps comprise: (1) dissolving a sulbenicillin sodium crude product in purified water, adding active carbon, carrying out stirring decolorizing, and filtering; (2) adding an extractant to the filtrate under the stirring, transferring and filling into a pressure resistance container, removing air bubbles, carrying out sealing oscillation, carrying out temperature control freezing, and taking out; and (3) carrying out liquid-solid separation, discarding the extractant, adding acetone in a dropwise manner at a temperature of 5 DEG C after the solid melts, stirring at a slow speed, growing the grain, filtering, washing, and carrying out vacuum drying to obtain the sulbenicillin sodium finished product. The children sulbenicillin sodium compound entity of the present invention has advantages of good solubility, good clarity, low related substance content, good stability, low toxic-side effect, and the like.

Description

technical field [0001] The invention relates to a compound entity of sulfbenicillin sodium for children and a pharmaceutical preparation thereof, belonging to the field of pharmaceutical compounds. Background technique [0002] Sulbenicillin sodium, English name: Sulbenicillin Sodium, original product name: Lilacillin, its chemical name is (2S, 5R, 6R)-3,3-dimethyl-6-(2-phenyl-2- Sulfoacetylamino)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid disodium salt. Molecular formula: C 16 h 16 N 2 Na 2 o 7 S 2 , molecular weight: 458.42. [0003] Sulbenicillin sodium belongs to semi-synthetic penicillin antibiotics, which are effective against Enterobacteriaceae such as Escherichia coli, Proteus, Enterobacter, Citrobacter, Salmonella and Shigella, as well as Pseudomonas aeruginosa , Haemophilus influenzae, Neisseria and other Gram-negative bacteria have antibacterial effect. This product also has antibacterial activity against hemolytic Streptococcus, Streptococ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/62C07D499/18A61K31/43A61P31/04
CPCC07D499/62C07D499/18
Inventor 陈宇东厉达中
Owner ZHEJIANG CHANGDIAN PHARMA
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