Preparation method of meropenem trihydrate crystal

A technology for meropenem trihydrate and meropenem, which is applied in the field of preparation of meropenem trihydrate crystals, can solve problems such as uninvolved solubility properties, and achieve the effects of good solubility, high purity, and rapid solubility properties

Active Publication Date: 2010-11-24
JIANKANGYUAN PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] None of the above reported preparation methods of meropenem trihydrate crystals involved its solubility properties, but in clinical applications, solubility properties are an indicator of concern

Method used

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  • Preparation method of meropenem trihydrate crystal

Examples

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Effect test

Embodiment 1

[0025] Under nitrogen atmosphere, distilled water (200ml) was heated to 45°C-50°C. The crude meropenem product (5.0 g, test = 93%) was added to distilled water, stirred at 45°C-50°C for 2 minutes, 1.0 g of activated carbon was added, and then rapidly cooled to 5°C-10°C. The carbon was filtered. Acetone (100ml) was added to the filtrate, the temperature was lowered to -20°C to -5°C, and the system was frozen. Vigorous stirring was maintained at this temperature for 30 minutes. Then the temperature of the system was raised to 5°C-20°C, at which temperature acetone (300ml) was added. Then lower the temperature to 0°C to 5°C and stir for 3 to 4 hours. The crystalline solid was filtered, washed with acetone, and dried under reduced pressure at 40° C. for 3-4 hours to obtain white meropenem trihydrate crystals (4.03 g, 99.5% assay). In the clarity test, the time for no turbidity is 30 seconds, the time for less than 5 particles is 45 seconds, and the time for complete dissolutio...

Embodiment 2

[0031] The method of Example 1 was repeated using crude meropenem (5.0 g, test=80%) to obtain white meropenem trihydrate crystals (3.52 g, test 98.2%). In the clarity test, the time for no turbidity is 30 seconds, the time for less than 5 particles is 60 seconds, and the time for complete dissolution is 75 seconds.

Embodiment 3

[0033] Distilled water (100 ml) was heated to 65°C under nitrogen atmosphere. The crude meropenem product (5.0 g, inspection = 93%) was added to distilled water, stirred at 65°C for 2 minutes, 1.0 g of activated carbon was added, and then rapidly cooled to 5°C-10°C. The carbon was filtered. Acetone (50ml) was added to the filtrate, the temperature was lowered to -20°C to -5°C, and the system was frozen. Vigorous stirring was maintained at this temperature for 30 minutes. Then the temperature of the system was raised to 5°C-20°C, at which temperature acetone (150ml) was added. Then lower the temperature to 0°C to 5°C and stir for 3 to 4 hours. The crystalline solid was filtered, washed with acetone, and dried under reduced pressure at 40° C. for 3-4 hours to obtain white meropenem trihydrate crystals (4.15 g, 99.3% assay). In the clarity test, the time for no turbidity is 30 seconds, the time for less than 5 particles is 45 seconds, and the time for complete dissolution is ...

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Abstract

The invention discloses a preparation method of a meropenem trihydrate crystal, comprising the following steps: dissolving a crude meropenem product in water at 30-70 DEG C to obtain solution I; treating the solution I with active carbon and then filtering the treated solution at 5-30 DEG C to obtain solution II; adding an organic solvent to the solution II and then cooling to -20-0 DEG C to form a crystal nucleus; and melting the crystal nucleus, adding an organic solvent, and then crystallizing to obtain the meropenem trihydrate crystal. The preparation method is simple and feasible; and the obtained meropenem trihydrate crystal has uniform crystallinity, high purity and fast dissolving performance, and the crystal can be used for preparing a meropenem medicinal preparation with good dissolubility.

Description

technical field [0001] The invention relates to a method for preparing a compound, in particular to a method for preparing meropenem trihydrate crystals with good solubility properties. Background technique [0002] Carbapenem antibiotics are a new type of fully synthetic β-lactam antibiotics, which have strong antibacterial activity against Gram-positive and negative bacteria, aerobic bacteria, and anaerobic bacteria. Since the discovery of thiamycin in 1976, the research on carbapenem antibiotics has made great progress. In particular, 1β-methyl carbapenem antibiotics have good chemical stability and are stable to β-lactamase and renal dehydropeptide-I enzymes. They are currently one of the first-choice drugs for the treatment of severe and multidrug-resistant bacterial infections. It has been more and more widely used in clinical practice. [0003] Currently commercialized 1β-methyl carbapenem antibiotics include meropenem, biapenem, doripenem, and ertapenem. Meropenem...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D477/20C07D477/06
Inventor 朱喜宗任鹏汪小华
Owner JIANKANGYUAN PHARMA GROUP
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