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Meropenem raw medicine, preparation method thereof and pharmaceutical composition containing same

A technology of meropenem and raw materials, which is applied in the fields of pharmaceutical formulations, antibacterial drugs, medical preparations containing active ingredients, etc.

Active Publication Date: 2014-02-12
SHENZHEN HAIBIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, there is no report on a high-yield preparation of high-purity, clear impurity status, and low solvent residue meropenem API involving the entire crystallization process of dissolution, crystallization, and crystal growth.

Method used

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  • Meropenem raw medicine, preparation method thereof and pharmaceutical composition containing same
  • Meropenem raw medicine, preparation method thereof and pharmaceutical composition containing same
  • Meropenem raw medicine, preparation method thereof and pharmaceutical composition containing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Add 2600g of pure water into a 5L flask, stir and heat up to 65°C, add 200g of crude meropenem into the flask, dissolve within 2 minutes, then cool down to 20°C within 3 minutes, add 20g of medical activated carbon for 2-3 minutes to decolorize , filter at 20°C, add the filtrate to a 10L three-necked flask, add 0.2g of seed crystals, keep the stirring speed at about 120 rpm, cool down to 5°C, start to calculate the crystal growth time, keep the temperature at 2-3°C, 10 Hours later, add 5200ml of acetone pre-cooled to 0-5°C dropwise, grow crystals at 2-3°C for 30 minutes after dripping, filter, rinse the filter cake with acetone, and dry the filter cake under vacuum at 30°C for 6 hours to obtain the meropenem raw material drug 176 grams, yield 88%.

[0095] Among them, the content of meropenem is 99.04% (calculated as anhydrous matter); impurity A in related substances is 0.10%; impurity B is 0.11%; any unknown single impurity is 0.02%; the sum of other impurities except...

Embodiment 2

[0134] Add 320g of pure water into a 500ml flask, stir and heat up to 50°C, add 20g of crude meropenem into the flask, dissolve within 2 minutes, then cool down to 10°C within 2 minutes, add 0.2g of medical activated carbon for 2-3 minutes to decolorize , filter at 10°C, add the filtrate to a 1000ml three-neck flask, add 0.4g seed crystals, then cool down to 5°C, start to calculate the crystal growth time, keep the stirring speed at 110 rpm, and the temperature at 3-5°C, and grow the crystals 8 hours, then add dropwise 480ml of acetone pre-cooled to 0-5°C, control the temperature of the filtrate II at 0°C-5°C, grow the crystal for 1 hour after dropping, filter, rinse the filter cake with acetone, and vacuum the filter cake at 20°C After drying for 5 hours, 17.2 g of meropenem bulk drug was obtained with a yield of 86%.

[0135] Among them, the content of meropenem is 100.04% (calculated as anhydrous matter); impurity A in related substances is 0.08%; impurity B is 0.09%; any u...

Embodiment 3

[0139] Add 200g of pure water into a 500ml flask, stir and raise the temperature to 70°C, quickly add 20g of crude meropenem into the flask, dissolve it within 2 minutes, then quickly cool down to 30°C within 2 minutes, add 4g of medical activated carbon for decolorization 5 Minutes, filter at 30°C, add the filtrate to a 1000ml three-necked flask, cool down to 20°C, add 2g of seed crystals, then cool down to 5°C, start to calculate the crystal growth time, keep the stirring speed at 150 rpm, and the temperature at 3-5 After growing the crystal for 2.1 hours at ℃, add 100ml of acetone dropwise, grow the crystal for 30 minutes after dropping, filter, rinse the filter cake with acetone, and dry the filter cake in vacuum at 40°C for more than 2 hours to obtain 16.6 g of meropenem raw material drug, yield 83%.

[0140] Among them, the content of meropenem is 99.7% (calculated as anhydrous matter); impurity A in related substances is 0.08%; impurity B is 0.13%; any unknown single im...

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Abstract

The invention discloses a meropenem raw medicine which is characterized in that the content of meropenem in the raw medicine is 98.0-101.0% by weight based on anhydride; the content of the impurity A and impurity B in the related substances of the raw medicine is not greater than 0.25% respectively; the content of any unknown single impurity is not greater than 0.05%; the total content of other impurities except the A and B is not greater than 0.2%; the acetone residue is not greater than 500ppm. The invention also discloses a meropenem pharmaceutical composition for injection, and the pharmaceutical composition takes the meropenem raw medicine provided by the invention as an active ingredient and has excellent stability. The meropenem raw medicine provided by the invention has the advantages of high purity, clear impurity condition, low solvent residue, good solubility and good long-term storage stability, and can guarantee the effectiveness and safety of the medicine. In the invention, the process is simple and compact, the cost is remarkably low, and the control is simple. The invention is suitable for industrial large-scale aseptic production of the meropenem raw medicine and pharmaceutical preparation.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular, the invention relates to a meropenem bulk drug, a preparation method thereof, and a pharmaceutical composition containing the meropenem bulk drug. Background technique [0002] Meropenem, the chemical name is (-)-(4R,5S,6S)-3-[(3S,5S)-5-(dimethylaminoacyl)-3-pyrrolidine]thio-6-[ (1R)-1-Hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]-hept-2-ene-2-carboxylic acid trihydrate, is a β- Methyl carbapenem antibiotics, broad-spectrum antibacterial and available for injection, used to treat a variety of infections, including meningitis and pneumonia, which normally exist in the form of trihydrate, CAS registered The number is [119478~56~7], and the specific structural formula is shown in formula (I). [0003] [0004] API (Active Pharmaceutical Ingredient) is the English name for API (Active Pharmaceutical Ingredient), which refers to the API used in the production of various preparations ...

Claims

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Application Information

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IPC IPC(8): C07D477/20C07D477/02A61K31/407A61P31/04
CPCA61K31/407C07D477/02C07D477/20
Inventor 任鹏陈与华赵鹏孙万鹏郑君
Owner SHENZHEN HAIBIN PHARMA
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