Cefixime compound and pharmaceutical composition thereof

A cefixime and compound technology, which is applied in the field of pharmaceutical compounds, can solve problems such as being unsuitable for large-scale industrial production, collection, and difficulty in filtration, and achieve the effects of good stability, good fluidity, and high dissolution rate.

Inactive Publication Date: 2013-07-10
四川省惠达药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main particle size of the cefixime crystals disclosed in this patent application is very small, and the crystals that are too small are difficult to collect and filter during the preparation process, and are not suitable for large-scale industrial production.

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

[0037] Embodiment 1: the preparation of cefixime compound

[0038] (1) Dissolve cefixime solid in 200ml of mixed organic solvent I, and heat to 50°C to obtain a weight ratio of cefixime solid to mixed organic solvent I of 1:10; said mixed organic solvent I has a volume ratio of 1 : 2 acetonitrile and methanol;

[0039] (2) Add 40ml of mixed organic solvent II at 5°C while stirring, the mixed organic solvent II is ethanol and chloroform with a volume ratio of 1:0.1; after adding, cool down the solution containing cefixime to 1°C, and then stir While adding 400ml of pure water at 10°C, after the addition, let stand to grow crystals for 5 hours, obtain crystals, filter, wash with absolute ethanol, and dry in vacuum at low temperature to obtain cefixime compound crystals. The rate of adding the mixed organic solvent II was 0.4 ml / min, and the rate of adding pure water was 2 ml / min. The stirring speed when adding the mixed organic solvent II is 60 rpm, and the stirring speed when...

Embodiment 2

[0041] Embodiment 2: the preparation of cefixime compound

[0042] . (1) Dissolve cefixime solid in 250ml of mixed organic solvent I and heat to 55°C to obtain a weight ratio of cefixime solid to mixed organic solvent I of 1:15; mixed organic solvent I is 1:4 by volume Acetonitrile and methanol;

[0043] (2) Add 100ml of mixed organic solvent II at 4°C while stirring. The mixed organic solvent II is ethanol and chloroform with a volume ratio of 1:0.2; after adding the mixed solvent, cool down the solution containing cefixime to 2°C, and then 1000ml of pure water at 8°C was added while stirring, and after the addition was completed, the crystals were left standing to grow, and the obtained crystals were filtered, washed with absolute ethanol, and dried in vacuum at low temperature to obtain cefixime compound crystals. The adding speed of mixed organic solvent II is 1 ml / min, and the adding speed of pure water is 5 ml / min; the stirring speed when adding mixed organic solvent I...

Embodiment 3

[0045] Embodiment 3: the preparation of cefixime compound

[0046] (1) Dissolve cefixime solid in 300ml of mixed organic solvent I, and heat to 60°C to obtain a weight ratio of cefixime solid to mixed organic solvent I of 1:12; said mixed organic solvent I has a volume ratio of 1 : 5 acetonitrile and methanol;

[0047] (2) Add 150ml of mixed organic solvent II at 2°C while stirring, the mixed organic solvent II is ethanol and chloroform with a volume ratio of 1:0.1; after adding the mixed solvent, cool down the solution containing cefixime to 1°C, and then 900ml of pure water at 8°C was added while stirring, and after the addition was completed, the crystal was grown by standing still, and the obtained crystal was filtered, washed with absolute ethanol, and dried in vacuum at low temperature to obtain the cefixime compound crystal. The adding speed of mixed organic solvent II is 1 ml / min, and the adding speed of pure water is 3 ml / min; the stirring speed when adding mixed org...

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Abstract

The invention relates to a drug compound, and particularly relates to a cefixime compound. An X-ray powder diffraction pattern of the cefixime compound measured through a Cu-K alpha ray is shown in a figure I. The invention also relates to a pharmaceutical composition containing the cefixime compound. The pharmaceutical composition comprises the cefixime compound and a pharmaceutical adjuvant; the pharmaceutical composition is an oral preparation including an oral normal release preparation and a controlled release preparation; and the oral normal release preparation is selected from a tablet, an enteric-coated tablet, a capsule, a dispersible tablet, dry suspension, a chewable tablet or granules. The cefixime compound disclosed by the invention is high in purity, high in bioavailability and suitable for clinical application.

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 (cefixime, 1) chemical name (6R, 7R)-7-[[(2Z)-(2-aminothiazol-4-yl)[(carboxymethoxy)imino]acetamido]- 3-vinyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid is the third generation of oral cephalosporin antibiotics; it has a broad antibacterial spectrum , long half-life, high efficiency and low toxicity, etc., it is an anti-infective drug widely used in clinical practice. 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. Similar to other third-generation cep...

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 梁宏平
Owner 四川省惠达药业有限公司
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