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Cefpodoxime proxetil compound as well as preparation method and medicinal composition thereof

A technology of cefpodoxime axetil and a compound, applied in the field of medicine, can solve the problems of poor powder fluidity and poor stability, and achieve the effects of good dispersibility and uniform particle size distribution

Inactive Publication Date: 2013-09-04
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

Destructive experiments show that cefpodoxime axetil has poor stability under light, heat and humidity conditions, is easily degraded to produce decomposition products, and has poor powder fluidity

Method used

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  • Cefpodoxime proxetil compound as well as preparation method and medicinal composition thereof
  • Cefpodoxime proxetil compound as well as preparation method and medicinal composition thereof
  • Cefpodoxime proxetil compound as well as preparation method and medicinal composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] [embodiment 1] the preparation of cefpodoxime axetil compound

[0050] 1) Add 2.1kg of cefpodoxime axetil raw material into 10L of mixed solvent prepared from methanol and dimethylformamide (the volume ratio of methanol to dimethylformamide is 3:1), stir to dissolve For the medicinal liquid, add active carbon with a total volume of 0.1% g / ml of the medicinal liquid to decolorize, filter, and the filtrate is for subsequent use;

[0051] 2) At room temperature, add the filtrate obtained in step 1) to 200L of water at a stirring speed of 900r / min, cool down to 3°C after adding the filtrate, and continue stirring for 10min after obtaining crystals; filter and wash the filter cake with methanol , and dried under reduced pressure to obtain light yellow crystalline powder, which is the cefpodoxime axetil compound. IR (VBr) cm -1 1780 (beta-lactam C=O), 1680 (amide C=O), 1 HNMR1.31 (6H, d, CH (CH 3 ) 2 ), 1.56 (3H,d,CHCH 3 ) 3.30 (3H, S, OCH 3 ) 3.52 (2H, brS, 2-CH 2 ),...

Embodiment 2-8

[0055]

[0056] The X-ray powder diffraction spectrum obtained by measuring the cefpodoxime axetil compound prepared in Examples 2-8 using Cu-Kα rays is consistent with Example 1.

preparation Embodiment 1

[0057] [Preparation Example 1] Cefpodoxime Proxetil Tablet

[0058] In this example, the cefpodoxime axetil compound prepared in Example 1 of the present invention is used to prepare a pharmaceutical composition in tablet form. Oral formulations in the form of tablets are prepared using dry granulation as a processing technique. The pharmaceutical composition is listed in Table 2.

[0059] Table 2

[0060] Element

[0061] Preparation method: Mix cefpodoxime axetil of Example 1 with sodium carboxymethylcellulose and sodium lauryl sulfate, and pass through a sieve (British Standard Sieve (BBS) 25; 600 μm). Pass the mixture through a pulverizer mill fitted with a 1.0 mm screen and impact forward at high speed. Lactose and hydroxypropylcellulose were passed through a 600 μm mesh sieve and mixed with the milled mixture in a non-shear mixer (octagonal mixer). The resulting mixture was dried into granules by extrusion. The extrudate was passed through a 710 μm mesh (...

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to a cefpodoxime proxetil compound as well as a preparation method and a medicinal composition thereof. The cefpodoxime proxetil compound has a chemical structural formula shown in a formula (I); and the cefpodoxime proxetil compound adopts an X-ray powder diffraction pattern which is obtained by Cu-Kalpha ray measurement and shown in a figure 1. The stability test shows that the humidity stability of the cefpodoxime proxetil compound is obviously superior to that of cefpodoxime proxetil in the prior art, the temperature and illumination stability of the cefpodoxime proxetil compound is also superior to that of cefpodoxime proxetil in the prior art, and the purity of the cefpodoxime proxetil compound is obviously higher than that of cefpodoxime proxetil in the prior art; and in addition, surprisingly, the cefpodoxime proxetil compound provided by the invention has good fluidity and is easy to subpackage.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a cefpodoxime axetil compound, a preparation method thereof and a pharmaceutical composition thereof. Background technique [0002] Cefpodoxime axetil, its chemical name is: (6R,7R)-7-[2-(2-amino-4-thiazolyl)-(Z)-2-(methoxyimino)-acetamido]-3 -Methoxymethyl-8-oxo-5-thia-1-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid isopropoxycarbonyloxyethyl ester, molecular formula: C 21 h 27 N 5 o 9 S 2 , molecular weight: 557.61, structural formula: [0003] [0004] It is a third-generation cephalosporin orally administered with a broad antibacterial spectrum. After entering the body, it is hydrolyzed by non-specific esterase into cefpodoxime to exert antibacterial effect. It has a wide range of antibacterial spectrum against Gram-positive bacteria and Gram-negative bacteria. β-lactamase stable. It is clinically applicable to upper respiratory tract infection, lower r...

Claims

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Application Information

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IPC IPC(8): C07D501/34C07D501/12A61K31/546
Inventor 梁宏平
Owner 四川省惠达药业有限公司
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