Preparation method of amorphous cefuroxime axetil oral antibacterial composition and its prepared composition and compound preparation

A technology of cefuroxime axetil and antibacterial composition, which is applied in the field of medicine, can solve the problems of poor bioavailability, high preparation cost, unfavorable acceptance, etc., and achieve the effects of strong antibacterial effect, good bioavailability, and reduced dosage

Active Publication Date: 2016-04-06
GUANGDONG LIGUO PHARMACY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, in the above-mentioned application, only cefuroxime axetil and sulbactam pivoxil are simply mixed, and the bioavailability of crystalline cefuroxime axetil and sulbactam pivoxil after mixing is poor
In addition, due to the high price of sulbactam pivoxil and its large dosage, the cost of the preparation is relatively high, which is not conducive to its acceptance by patients in economically backward areas.

Method used

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  • Preparation method of amorphous cefuroxime axetil oral antibacterial composition and its prepared composition and compound preparation
  • Preparation method of amorphous cefuroxime axetil oral antibacterial composition and its prepared composition and compound preparation
  • Preparation method of amorphous cefuroxime axetil oral antibacterial composition and its prepared composition and compound preparation

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preparation example Construction

[0023] The process procedures such as preparing capsules and tablets used in the present invention are all well-known technologies in the art, and those skilled in the art can refer to relevant reference books to learn.

[0024] In the preparation method of amorphous cefuroxime axetil oral antibacterial composition, organic solvent can be lower aliphatic ketone, saturated lower alcohol, C 2 -C 6 Lower alkanes, C 2 -C 6 Nitriles, ethers, lower carboxylic acid esters or their mixtures. For example, preferably, lower aliphatic ketone is acetone, methyl ethyl ketone or their mixture, saturated lower alcohol is methanol, ethanol, isopropanol or their mixture, C 2 -C 6 The lower alkanes are dichloromethane, chloroform, carbon tetrachloride, dichloroethane, trichloroethane or their mixtures, C 2 -C 6 The nitriles are acetonitrile, C 2 -C 6 The ethers are n-propyl ether, isopropyl ether, and tetrahydrofuran, and the lower carboxylic acid esters are ethyl formate, propyl format...

Embodiment 1

[0027] Example 1 Amorphous Cefuroxime Axetil Oral Antibacterial Compound Capsule A

[0028] Dissolve crystalline cefuroxime axetil and crystalline sulbactam pivoxil in 3 times (W / V) acetone, add activated carbon for decolorization, and spray dry to obtain uniform spherical particles, that is, amorphous cefuroxime axetil oral antibacterial composition , and then made into capsules, the weight ratio of cefuroxime axetil (in cefuroxime) and sulbactam pivoxil (in sulbactam) is 1:1.

Embodiment 2

[0029] Example 2 Amorphous Cefuroxime Axetil Oral Antibacterial Compound Tablet B

[0030] Dissolve crystalline cefuroxime axetil and crystalline sulbactam pivoxil in 5 times (W / V) acetone, add activated carbon for decolorization, and spray dry to obtain uniform spherical particles, that is, amorphous cefuroxime axetil oral antibacterial composition , Then make tablet, wherein, the weight ratio of cefuroxime axetil (in cefuroxime) and sulbactam pivoxil (in sulbactam) is 2:1.

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Abstract

The invention discloses a preparation method of an oral amorphous cefuroxime axetil antibacterial composition, and a composition and compound preparation prepared by the same. The preparation method comprises the steps of: dissolving crystalline cefuroxime axetil and crystalline sulbactam pivoxil in an organic solvent, decoloring, and spray drying to obtain the oral amorphous cefuroxime axetil antibacterial composition. By the preparation method disclosed by the invention, the oral amorphous cefuroxime axetil antibacterial composition with uniform spherical shapes, large specific area, good bioavailability and a smaller dose of sulbactam pivoxil can be obtained, and the compound preparation prepared by the preparation method has low cost and good antibacterial effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of an oral oral antibacterial composition of amorphous cefuroxime axetil and the prepared oral antibacterial composition of amorphous cefuroxime axetil and a compound preparation. Background technique [0002] Cefuroxime Axetil is a second-generation cephalosporin. As a broad-spectrum bactericidal antibiotic, it has a strong antibacterial effect on Gram-positive bacteria and most Gram-negative bacteria. Nephrotoxicity is low. With the wide application of cefuroxime axetil in clinical practice, some originally sensitive strains have developed resistance to cefuroxime, making its antibacterial effect decline. Studies have found that the main mechanism of bacterial resistance to cephalosporins is to produce specific β-lactamase to decompose drugs. [0003] In order to overcome the above problems, Chinese patent application CN1742735A discloses a cefuroxime ax...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/546A61K31/43A61P31/04
Inventor 潘行远曾建江楼秋霞
Owner GUANGDONG LIGUO PHARMACY
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