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Cefixime compound and pharmaceutical composition thereof

A technology of cefixime and compounds, applied in the field of pharmaceutical compounds, can solve problems such as residues, undisclosed crystal purity, hidden dangers of drug safety, etc., and achieve the effect of strong stability and high dissolution rate

Active Publication Date: 2013-01-16
金鸿药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The organic solvent used in the crystal preparation method is tetrahydrofuran. Since tetrahydrofuran is a type of heterocyclic molecule, it is easy to cause certain residues during the crystallization process, and the purity of the crystal is not disclosed in the application. Therefore, the crystal There are still certain risks in drug safety

Method used

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  • Cefixime compound and pharmaceutical composition thereof
  • Cefixime compound and pharmaceutical composition thereof
  • Cefixime compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: the preparation of cefixime crystal

[0042] The preparation method of cefixime crystal of the present invention comprises the following steps:

[0043] (1) Dissolve cefixime solid in a mixed solution of methanol and acetone, heat to 45°C, and the weight ratio of cefixime solid to the mixed solution of methanol and acetone is 1:100; in the mixed solution, methanol, The volume ratio of acetone is 5:3;

[0044] (2) In a 5L reactor, in a sound field with a frequency of 18KHz and an output power of 25W, add a solution of isobutanol with a volume percentage of 1% at 5°C dropwise while stirring, and the stirring speed is 30 rpm; After finishing, stop the sound field, and let the crystal grow for 5 hours; filter after obtaining the crystal, wash with absolute ethanol, and vacuum-dry for 4 hours to obtain the cefixime compound crystal; wherein, the volume of the aqueous solution of isobutanol added is cefixime 5 times that of the organic solution; the speed of t...

Embodiment 2

[0046] Embodiment 2: the preparation of cefixime crystal

[0047] (1) Dissolve cefixime solid in a mixed solution of methanol and acetone and heat to 40°C. The weight ratio of cefixime solid to the mixed solution of methanol and acetone is 1.5:100; in the mixed solution, methanol, The volume ratio of acetone is 5:2;

[0048] (2) In a 10L reactor, in a sound field with a frequency of 30KHz and an output power of 80W, add an aqueous solution of isobutanol with a volume percentage of 2% at 6°C dropwise while stirring, and the stirring speed is 45 rpm; After finishing, stop the sound field, let stand to grow crystals for 6 hours; filter after obtaining the crystals, wash with absolute ethanol, and vacuum-dry for 6 hours to obtain cefixime compound crystals; wherein, the volume of the aqueous solution of isobutanol added is cefixime 4 times that of the organic solution; the speed of the aqueous solution of isobutanol added is 120ml / min.

[0049] The X-ray powder diffraction patte...

Embodiment 3

[0050] Embodiment 3: the preparation of cefixime crystal

[0051] (1) Dissolve cefixime solid in a mixed solution of methanol and acetone, heat to 38°C, and the weight ratio of cefixime solid to the mixed solution of methanol and acetone is 1:50; in the mixed solution, methanol, The volume ratio of acetone is 10:3;

[0052] (2) In a 5L reactor, in a sound field with a frequency of 20KHz and an output power of 30W, add a 3% isobutanol aqueous solution at 7°C dropwise while stirring, and the stirring speed is 60 rpm; After finishing, stop the sound field, and let the crystal grow for 8 hours; filter after obtaining the crystal, wash with absolute ethanol, and vacuum-dry for 8 hours to obtain the cefixime compound crystal; wherein, the volume of the aqueous solution of isobutanol added is cefixime 2 times that of the organic solution; the speed of the aqueous solution of isobutanol added is 90ml / min.

[0053] The X-ray powder diffraction pattern obtained by Cu-Kα ray measuremen...

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Abstract

The invention relates to a pharmaceutical compound and in particular relates to a cefixime crystal compound. The cefixime compound is a crystal, and an X-ray powder diffraction pattern obtained by Cu-Kalpha ray measurement is shown as a figure 1. Main granularity of the cefixime compound crystal disclosed by the invention is 45-80Mum, and the distribution width is 30-100Mum. The cefixime crystal disclosed by the invention has high stability and high purity and is applicable to preparation of the pharmaceutical compound, and preferable dosage forms are dispersible tablets and granules.

Description

technical field [0001] The present invention relates to a medicine compound, in particular to a cefixime compound and a medicine composition thereof. Background technique [0002] Cefixime is the first orally active third-generation cephalosporin. Although compared with the existing orally effective β-lactam antibiotics, the activity against staphylococci is poor, but the activity against streptococci is similar to that of cefaclor, and the activity against gram-negative bacteria is much stronger than that of Existing oral β-lactam antibiotics. The molecular basis for the potent antibacterial activity of cefixime against Gram-negative bacteria has now been elucidated. Cefixime can combine with penicillin-binding protein (PBP) to inhibit the synthesis of peptidoglycan layer on the bacterial cell wall, thereby destroying the division of bacteria. Gram-negative bacteria are surrounded by an outer membrane, and PBP is located in the cytoplasmic membrane (inner membrane). In ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/22C07D501/12A61K31/546A61P31/04
Inventor 黄金秀
Owner 金鸿药业股份有限公司
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