A kind of cefepime hydrochloride compound

A technology for cefepime hydrochloride and compounds, which is applied in the field of cefepime hydrochloride compounds, can solve the problems of biological activity that needs to be further tested, and achieve the effects of safe and reliable clinical application, easy separation and collection, and good bioavailability

Active Publication Date: 2016-01-27
YOUCARE PHARMA GROUP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] A cefepime hydrochloride compound is disclosed in the patent application 201310229537.0. The X-ray powder diffraction spectrum obtained by Cu-Kα ray measurement is as follows: figure 1 As shown, in the crystallization process of the crystal, the organic solution containing cefepime hydrochloride is heated to 130-150°C and maintained for 1-1.5 hours. Since the decomposition temperature of cefepime is 150°C, this method is used to prepare The biological activity of the crystals needs to be further tested

Method used

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  • A kind of cefepime hydrochloride compound
  • A kind of cefepime hydrochloride compound
  • A kind of cefepime hydrochloride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1. Prepare 2L of aqueous solution of crude cefepime hydrochloride 0.6g / ml;

[0034] 2. In a sound field with a frequency of 30KHz and an output power of 30W, under the condition of nitrogen filling, add tetrahydrofuran at 5°C while stirring. The volume of tetrahydrofuran added is 4L, and the addition speed is 20ml / min;

[0035] 3. After adding tetrahydrofuran, adjust the frequency of the sound field to 25KHz, and continue to add 5L of a mixed solution of isopropanol and cyclohexane at 3°C ​​at a speed of 100ml / min; remove the sound field after adding the mixed solvent, and cool down to 0°C , the cooling rate is 0.25° C. / hour; the crystal is grown for 6 hours, washed and dried to obtain the cefepime hydrochloride compound.

[0036] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.96%, and the yield is 96.8%; the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement is as follows: figure 2 As shown; thro...

Embodiment 2

[0038] 1. Prepare 2 L of an aqueous solution of 0.5 g / ml crude product of cefepime hydrochloride;

[0039] 2. In a sound field with a frequency of 28KHz and an output power of 30W, under nitrogen filling conditions, add tetrahydrofuran at 8°C while stirring; the volume of tetrahydrofuran added is 3L; the addition speed is 20ml / min;

[0040]3. After adding tetrahydrofuran, adjust the frequency of the sound field to 22KHz, and continue to add 4L of a mixed solution of isopropanol and cyclohexane at 1°C at a speed of 40ml / min. After adding the mixed solvent, remove the sound field and cool down to 0°C , the cooling rate was 0.2° C. / hour, the crystal was grown for 4 hours, washed and dried to obtain the cefepime hydrochloride compound.

[0041] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.96%, and the yield is 96.8%; the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement is as follows: figure 2 As shown; t...

Embodiment 3

[0043] 1. Prepare 2L of aqueous solution of crude cefepime hydrochloride 0.6g / ml;

[0044] 2. In a sound field with a frequency of 26KHz and an output power of 40W, under the condition of nitrogen filling, add tetrahydrofuran at 6°C while stirring. The volume of tetrahydrofuran added is 4L, and the addition speed is 20ml / min;

[0045] 3. After adding tetrahydrofuran, adjust the frequency of the sound field to 21KHz, and continue to add 5L of a mixed solution of isopropanol and cyclohexane at 1°C at a speed of 50ml / min; remove the sound field after adding the mixed solvent, and cool down to 0°C , the cooling rate is 0.25° C. / hour, the crystal is grown for 6 hours, washed and dried to obtain the cefepime hydrochloride compound.

[0046] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.96%, and the yield is 96.8%; the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement is as follows: figure 2 As shown; through...

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Abstract

The invention relates to the field of pharmacy, and particularly relates to a cefepime dihydrochloride compound. The cefepime dihydrochloride is crystal, and an X-ray powder diffraction diagram measured by using a Cu-K alpha ray is shown in a figure 2. The purity of the cefepime dihydrochloride compound disclosed by the invention can be up to 99.95-99.98%; the molecular formula of the cefepime dihydrochloride obtained by elemental analysis and differential thermal analysis is C19H25ClN6O5S2.2HCl.H2O. The solvent used in the crystallization method disclosed by the invention is low in content, andthe cefepime dihydrochloride compound is safe and reliable in clinical application. A stability experiment proves that the cefepime dihydrochloride crystal compound provided by the invention is good in stability, and the prepared cefepime dihydrochloride compound is lower than that in the prior art in hygroscopicity, better than that in the prior art in bioavailability, and more applicable to clinical application.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a cefepime hydrochloride compound. Background technique [0002] Cefepime is a broad-spectrum fourth-generation cephalosporin that achieves bactericidal effect by inhibiting the biosynthesis of bacterial cell walls. In vitro tests have shown that it has effects on both Gram-positive and Gram-negative bacteria. This product has a low affinity to the β-lactamase encoded by the bacterial chromosome, can be highly resistant to the hydrolysis of most β-lactamases, and can quickly penetrate into the cells of Gram-negative bacteria. In bacterial cells, its target molecule is penicillin-binding protein (PBP). Molecular formula: C 19 h 25 ClN 6 o 5 S 2 ·HCl·H 2 O Properties: This product is white or off-white powder; slightly smelly, tasteless. [0003] The synthesis of cefepime hydrochloride (Gong Pingping, Chinese Journal of Medicinal Chemistry, 2002, December) discloses a synthetic met...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/46C07D501/12
CPCC07D501/12C07D501/46
Inventor 李琦杨磊
Owner YOUCARE PHARMA GROUP
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