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Children ampicillin sodium compound entity and pharmaceutical preparation thereof

A technology of ampicillin sodium and ampicillin, applied in the field of pharmaceutical compounds, can solve the problems of poor stability of ampicillin sodium, occurrence of degradation products, easy discoloration of appearance, etc., and achieve the effects of less allergy, less impurities and good clarity

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 prepared ampicillin sodium still exhibits poor stability, and is unstable to heat, partial acid environment, and partial alkali environment, and shows problems such as easy discoloration of the appearance, reduction of content, and occurrence of degradation products. The reason for occurrence may be ampicillin sodium Some impurities in the finished product cannot be removed by crystallization

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Add 527ml of dichloromethane and 123ml of triethylamine into the reactor, stir evenly, cool down to 0°C, add 200g of ampicillin, and stir until completely dissolved. After the solution was sterilized by membrane filtration, the pipeline through which ampicillin passed during the filtration was rinsed with a mixture of 260ml of dichloromethane and 16ml of triethylamine, and the filtrate and washing solution were combined.

[0030] Add 140 grams of sodium isooctanoate to 609 ml of methyl acetate, and stir until completely dissolved. After the solution is sterilized by membrane filtration, the pipeline through which sodium isooctanoate passes through is rinsed with 200 ml of methyl acetate, and the filtrate and washing liquid are combined.

[0031] Cool the ampicillin solution to -5°C, add 1% sodium isooctanoate solution under rapid stirring, and after stirring for 10 minutes, slowly raise the temperature of the solution to 15°C while stirring, stir for 30 minutes, keep wa...

Embodiment 2

[0036] Add 527ml of dichloromethane and 123ml of triethylamine into the reactor, stir evenly, cool down to 0°C, add 200g of ampicillin, and stir until completely dissolved. After the solution was sterilized by membrane filtration, the pipeline through which ampicillin passed during the filtration was rinsed with a mixture of 260ml of dichloromethane and 16ml of triethylamine, and the filtrate and washing solution were combined.

[0037] Add 140 grams of sodium isooctanoate to 609 ml of methyl acetate, and stir until completely dissolved. After the solution is sterilized by membrane filtration, the pipeline through which sodium isooctanoate passes through is rinsed with 200 ml of methyl acetate, and the filtrate and washing liquid are combined.

[0038] Cool the ampicillin solution to -8°C, add 2% sodium isooctanoate solution under rapid stirring, stir for 10 minutes, slowly increase the solution temperature to 12°C while stirring, stir for 30 minutes, keep warm at 12°C, and th...

Embodiment 3

[0043]Add 527ml of dichloromethane and 123ml of triethylamine into the reactor, stir evenly, cool down to 0°C, add 200g of ampicillin, and stir until completely dissolved. After the solution was sterilized by membrane filtration, the pipeline through which ampicillin passed during the filtration was rinsed with a mixture of 260ml of dichloromethane and 16ml of triethylamine, and the filtrate and washing solution were combined.

[0044] Add 140 grams of sodium isooctanoate to 609 ml of methyl acetate, and stir until completely dissolved. After the solution is sterilized by membrane filtration, the pipeline through which sodium isooctanoate passes through is rinsed with 200 ml of methyl acetate, and the filtrate and washing liquid are combined.

[0045] Cool the ampicillin solution to -10°C, add 3% sodium isooctanoate solution under rapid stirring, stir for 10 minutes, slowly increase the solution temperature to 10°C while stirring, stir for 30 minutes, keep warm at 10°C, and th...

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Abstract

The present invention discloses a children ampicillin sodium compound entity, wherein the preparation method comprises: (1) adding ampicillin to a mixed solution of dichloromethane and triethylamine, cooling, adding a small amount of a sodium 2-ethylhexanoate solution, increasing the solution temperature, adding the remaining sodium 2-ethylhexanoate solution, carrying out suction filtration, washing, and carrying out vacuum drying to obtain an ampicillin sodium crude product; (2) dissolving the ampicillin sodium crude product in purified water, adding active carbon, carrying out stirring decolorizing, and filtering; (3) 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 (4) 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 ampicillin sodium finished product. The children ampicillin 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 an ampicillin sodium compound entity for children and a pharmaceutical preparation thereof, belonging to the field of pharmaceutical compounds. Background technique [0002] Ampicillin sodium, chemical name: (2S, 5R, 6R)-3,3-dimethyl-6[(R)-2-amino-2-phenylacetamido]-7-oxo-4-sulfur Generation-1-amobicyclo[3.2.0]heptane-2-potassium acid sodium salt. Molecular formula: C 16 h 18 N 3 NaO 4 S, molecular weight: 371.39. Ampicillin sodium is one of the earliest semi-synthetic penicillin antibiotics, suitable for the treatment of infections caused by sensitive bacteria. Typical indications include: sinusitis, otitis media, epiglottitis, bacterial pneumonia and other upper and lower respiratory tract infections; urinary tract infection, pyelonephritis; peritonitis, cholecystitis, endometritis, pelvic cellulitis and other intra-abdominal infections; Bacterial bacteremia; skin, soft tissue, bone, joint infection; gonococcal infecti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/68C07D499/16A61K31/43A61P31/04
CPCC07D499/68C07D499/16
Inventor 陈宇东厉达中
Owner ZHEJIANG CHANGDIAN PHARMA
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