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Preparation method of amorphous cefditoren pivoxil

A cefditoren axetil and amorphous technology, applied in the field of preparation of amorphous cefditoren axetil, can solve problems such as unreported cefditoren axetil, and achieve the effects of stable and feasible process, good product quality and high solubility

Inactive Publication Date: 2018-12-21
SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In summary, patents or literature have not reported that pure amorphous cefditoren axetil is prepared by solvent method

Method used

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  • Preparation method of amorphous cefditoren pivoxil
  • Preparation method of amorphous cefditoren pivoxil

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Suspend 50 grams of cefditoren axetil in 500 milliliters of dichloromethane, add 5 grams of activated carbon, heat up and stir for 30 minutes, filter, and wash the activated carbon with a small amount of dichloromethane. The filtrate and washing liquid were combined, concentrated to dryness under reduced pressure at 35°C, and the obtained solid was detected by XPRD as amorphous.

Embodiment 2

[0023] Suspend 50 grams of cefditoren axetil in 200 milliliters of dichloromethane, add 300 milliliters of acetone, then add 5 grams of activated carbon, heat up and stir for 30 minutes, filter, and wash the activated carbon with a small amount of dichloromethane. The filtrate and washing liquid were combined, concentrated under reduced pressure at 35°C to about 100 ml, added dropwise into 1000 ml of ether, precipitated, cooled in an ice bath at 0-5°C, stirred for 1 hour, filtered, washed with ether, and dried in vacuo. The resulting solid was detected by XPRD and was amorphous.

Embodiment 3

[0025] Suspend 50 grams of cefditoren axetil in 500 milliliters of dichloromethane, add 5 grams of activated carbon, heat up and stir for 30 minutes, filter, and wash the activated carbon with a small amount of dichloromethane. The filtrate and washing liquid were combined, concentrated under reduced pressure at 35°C to 100 ml, added dropwise into 1000 ml of ether, precipitated, cooled in an ice bath at 0-5°C, stirred for 1 hour, filtered, washed with ether, and dried in vacuo. Gained solid is detected by XPRD, such as figure 1 Shown is amorphous.

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Abstract

The invention discloses a preparation method of amorphous cefditoren pivoxil. The preparation method comprises the following steps: dissolving cefditoren pivoxil crystals in an organic solvent, rapidly concentrating, obtaining a cefditoren pivoxil amorphous form, or concentrating to a small volume, dropwise adding to a second organic solvent, and precipitating the cefditoren pivoxil amorphous form. A target product is detected by an XPRD manner and is an amorphous peak type. By adopting the cefditoren pivoxil amorphous form prepared in the invention, the solubility of the cefditoren pivoxil can be improved, and the bioavailability of a drug preparation can be improved. The preparation method disclosed in the invention is mild in conditions, stable in process, easy in operation.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and in particular relates to a preparation method of amorphous cefditoren axetil. Background technique [0002] Cefditoren pivoxil (cefditorenpivoxil), registration number: 117467-9-4, is the third generation of oral cephalosporin antibiotics, developed by Japan Meiji Seika Co., Ltd. in 1994, for the treatment of Gram-positive bacteria and Gram-positive bacteria Infections caused by negative bacteria, especially Staphylococcus, Gram-positive bacteria of the genus Streptococcus including Streptococcus pneumoniae, Escherichia coli, Branhamella catarrhalis, Klebsiella spp, Proteus spp, Gram-negative bacteria such as Haemophilus influenzae and anaerobic bacteria such as Peptostreptococcus, Propionibacterium acnes, and Bacteroides have shown strong antibacterial power. Because of its broad antibacterial spectrum, cefditoren axetil is widely used in clinical practice. Structural formula: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/24C07D501/02
Inventor 李江红陈林石克金任凤英杨晨苟小军颜军梁立
Owner SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP
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