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

A technology of meropenem and API, which is applied in pharmaceutical formulations, antibacterial drugs, medical preparations containing active ingredients, etc. The effect of stability

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

AI Technical Summary

Problems solved by technology

Therefore, this method of recrystallizing crude meropenem by dissolving it in strongly alkaline 10% sodium hydroxide water will not only fail to achieve the purpose of purifying meropenem but will also increase the impurities of meropenem
Therefore, the meropenem claimed in the examples has been tested by related substances of meropenem in the second part of the Chinese Pharmacopoeia in 2010, and the single largest impurity is 0.03%, and the total impurities are 0.13%. Regarding the detection standard of the substance, it does not mention the content of "the largest impurity before and after the main peak". We cannot determine whether the "single largest impurity" and "total impurities" include "the largest impurity before and after the main peak", so that it is not clear Know the status of the meropenem impurity in it
[0009] Impurities in meropenem or any active pharmaceutical ingredient (API) are unwanted and, in extreme cases, may even be harmful to patients being treated with API-containing dosage forms

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

[0084] Add 12 kg of crude meropenem to 120 kg of water, stir to form a suspension, raise the temperature of the material to 50°C to dissolve it, and then lower the temperature to 10°C.

[0085] Add 100 g of activated carbon for decolorization, and filter.

[0086] Add 480 L of crystallization solvent acetonitrile to the filtrate, and stir and grow the crystal for 2 hours after the addition is complete.

[0087] Filter, wash the crystals with acetonitrile, and dry to obtain 10.6 kg of the first refined meropenem.

[0088] The quality of the first refined meropenem: the total amount of impurities is 0.75%; the residual organic solvent is 0.23%.

Embodiment 2

[0090] Add 10 kg of the first refined meropenem product prepared in Example 1 into 150 kg of water, stir, use a heat exchanger to raise the temperature of the feed solution to 50°C, then cool it down to 0°C, and grow the crystal with stirring for 15 hours.

[0091] Filter, wash the crystals with acetonitrile, and dry to obtain 8.1 kg of high-purity meropenem bulk drug.

[0092] Among them, the content of meropenem is 99.6% (calculated as anhydrous matter); impurity A in related substances is 0.04%; impurity B is 0.03%; any unknown single impurity is 0.01%; the sum of other impurities except A and B is 0.02% ; Acetone residue is 100ppm, and acetonitrile is not detected.

[0093] 1. Determination of the structure of meropenem:

[0094] The test results of the physical properties of the meropenem raw material are as follows:

[0095] Elemental Analysis: C 17 h 25 N 3 o 5 S·3H 2 o

[0096] Calculated: C, 46.67%; H, 7.14%; N, 9.60%; S, 7.33%;

[0097] Found: C, 46.46%; H, ...

Embodiment 3

[0131] Add 12kg of crude meropenem to 180kg of water, stir to form a suspension, raise the temperature of the feed solution to 80°C to dissolve it, and then lower the temperature to 20°C.

[0132] Add 240g of activated carbon for decolorization, and filter.

[0133] Add 360 L of crystallization solvent acetone to the filtrate, and continue to stir and grow the crystal for 3 hours after the addition is complete.

[0134] Filter, wash the crystals with acetone, and dry to obtain 10.44 kg of the first refined meropenem.

[0135] The quality of the first refined meropenem: the total amount of impurities is 0.62%; the residual organic solvent is 0.25%.

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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 0.25%; the acetone residue is not greater than 300ppm. 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.

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 carbocyanine Mycelene antibiotics, which have broad-spectrum antibacterial properties and are available for injection, are used to treat a variety of infections, including meningitis and pneumonia. It exists in the form of trihydrate under normal conditions. The CAS registration number is [119478 ~56~7], the specific structural formula is shown in formula (I). [0003] [0004] API (Active Pharmaceutical Ingredient) is an API (Active Pharmaceutical Ingredient) in English, which refers to the raw material dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D477/20C07D477/02A61K31/407A61P31/04
CPCA61K31/407C07D477/02C07D477/20
Inventor 任鹏赵鹏孙万鹏
Owner XINXIANG HAIBIN PHARMA
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