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

A technology for meropenem and APIs, applied in pharmaceutical formulations, drug delivery, antibacterial drugs, etc., can solve the problems of clogging of nanofiltration membranes, difficulty in obtaining organic solvents, and high concentrations

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

Moreover, due to the high concentration of meropenem, the volume cannot be concentrated to a small size, otherwise crystals will precipitate and cause clogging of the nanofiltration m

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

[0112] Add 1 kg of crude meropenem to 20 kg of water for injection at a temperature of 10°C, stir and mix evenly, heat the suspension to 80°C through a heat exchanger to dissolve it, and quickly drop it to room temperature 25°C through a heat exchanger to obtain a solution I.

[0113] The decolorized solution I was filtered in-line through an activated carbon filter to obtain the filtrate II.

[0114] Release 210 g of filtrate II, set the temperature to 10° C., add 1050 ml of acetone, stir for 15 minutes, and then filter to obtain seed crystals. Cool down to 2°C, add the prepared seed crystals to the remaining 20.8 kg of filtrate II, keep the stirring speed at 130 rpm, grow the crystals for 8 hours, and filter to obtain mother liquor 3, which is then concentrated by nanofiltration in the next step.

[0115] The filter cake was rinsed with acetone, dried under vacuum at 30°C for 5 hours, and pulverized to obtain 680 g of meropenem raw material with a yield of 68%.

[0116] Am...

Embodiment 2

[0155] Put 21.0 kg of the refined mother liquor 3 of meropenem obtained in Example 1 into the solution tank of the nanofiltration equipment; control the outlet pressure of the nanofiltration equipment to 18×10 5 Pa began to concentrate, and the temperature of the feed liquid was controlled at 10°C to 25°C during the concentration process. It took 98 minutes, and the concentrate was reduced from 21.0kg to 2.70kg, and 18.30kg of concentrated wastewater was obtained. The concentrated wastewater was sampled to detect the content of meropenem, and the result was undetected. The concentrated solution was taken to detect that the content of meropenem was 10%.

[0156] Add 2.70kg of the concentrated solution to 152L of the filtered mother liquor (mother liquor 2) where the crude product has been precipitated, and stir at a temperature of 10-15°C for 30 minutes; filter, wash crystals, and dry to obtain 186g of crude meropenem; take a sample to detect the crude meropenem Impurities and ...

Embodiment 3

[0159] Add 20kg of crude meropenem to 300kg of water for injection at a temperature of 20°C, stir and mix evenly, heat the suspension to 70°C through a heat exchanger to dissolve, and quickly drop it to 20°C through a heat exchanger to obtain solution I .

[0160] The decolorized solution I was filtered in-line through an activated carbon filter to obtain the filtrate II.

[0161] Release 6.4kg of filtrate II, set the temperature at 5°C, add 25.6L of tetrahydrofuran, stir for 20 minutes, and then filter to obtain seed crystals. Cool down to 0°C, add the prepared seed crystals to the remaining 288 kg of filtrate II, keep the stirring speed at 120 rpm, grow the crystals for 10 hours, and filter to obtain mother liquor 3, which is then concentrated by nanofiltration in the next step.

[0162] The filter cake was rinsed with acetone, dried under vacuum at 25° C. for 6 hours, and pulverized to obtain 14 kg of meropenem raw material with a yield of 70%.

[0163] Among them, the co...

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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 98.5-101.0% 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 400ppm and preferably not greater than 100ppm. 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 (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 ...

Claims

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Application Information

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IPC IPC(8): C07D477/20C07D477/02A61K31/407A61P31/04
CPCC07D477/20C07D477/02C07D477/04A61K9/0019A61K31/407A61P31/04
Inventor 任鹏管曙光谭汉梯唐南湘唐秋停向斌波
Owner SHENZHEN HAIBIN PHARMA
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