Preparation method of amorphous cefditoren pivoxil composition

A technology for cefditoren pivoxil and cefditoren axetil, which is applied in the field of pharmaceutical chemical synthesis, can solve problems such as poor crystal stability, difficult solvent drying, influence on preparation preparation, etc., and achieves shortening drying time, enhancing bioavailability, avoiding The effect of mixed crystal results

Inactive Publication Date: 2019-09-20
BEIJING JIMEITANG MEDICINE RES CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been verified that the process is poorly feasible and there are major problems: 1. Due to the poor stability of this product, the related substances dissolved in the aqueous solution grow rapidly; 2. It is difficult to dry water as a solvent, the drying temperature is high and the drying time is long. The crystal form stability of the amorphous cefditoren pivoxil composition is poor under high temperature and high humidity conditions, and it is easy to transition from a high-energy state (amorphous form) to a low-energy state (crystalline state), and mixed crystals occur, resulting in impure crystal forms. Affect the preparation of subsequent preparations

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Suspend 50g of cefditoren axetil in 500ml of dichloromethane and acetone (volume ratio: 1:1), raise the temperature to 40°C and stir for 0.5h until completely dissolved, add 0.5g of hypromellose, stir for 5min until the hypromellose The powder is evenly dispersed, spray-dried, the air inlet temperature is 50-60°C, the atomization frequency is 35HZ-40HZ, and the outlet air temperature is 30-35°C. Collect the solid powder and send it to XRD for inspection. The spectrum is as follows figure 1 (no diffraction angle), confirmed to be amorphous.

Embodiment 2

[0030] Suspend 20g of cefditoren axetil in 300ml of chloroform, acetonitrile, and ethanol (2:1:1), raise the temperature to 35°C and stir for about 0.5h-1h until completely dissolved, add 0.5g of hypromellose, and stir for 5min to The hypromellose is uniformly dispersed, spray-dried, the air inlet temperature is 65-70°C, the atomization frequency is 40-50HZ, and the outlet air temperature is 30-40°C. Collect the solid powder and submit it for XRD inspection. The spectrum is as follows figure 2 (no diffraction angle), confirmed to be amorphous.

Embodiment 3

[0032] Suspend 50g of cefditoren axetil in 500ml of dichloromethane and acetone (volume ratio: 1:1), heat up to 40°C and stir for 0.5h until completely dissolved, add 0.25g of povidone k30, stir for 5min until it is uniformly dispersed, spray Drying, the inlet air temperature is 50-60°C, the atomization frequency is 30HZ-40HZ, the outlet air temperature is 30-35°C, collect the solid powder and submit it for XRD inspection, the spectrum is as follows image 3 (no diffraction angle), confirmed to be amorphous.

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Abstract

The invention relates to the field of medicinal chemistry synthesis and provides a preparation method of an amorphous cefditoren pivoxil composition. The preparation method is characterized by including: dissolving crystalline cefditoren pivoxil into a mixed organic solvent heated to certain temperature, suspending a water-soluble polymer material of a certain proportion into the mixed organic solvent, and drying through a spraying dryer to obtain the amorphous cefditoren pivoxil composition (with the water-soluble polymer material of a certain proportion wrapped inside).

Description

technical field [0001] The invention relates to the field of pharmaceutical chemical synthesis, relates to cefditoren pivoxil, in particular to a preparation method of an amorphous cefditoren pivoxil composition. Background technique [0002] Cefditoren pivoxil (cefditoren pivoxil) is a third-generation oral cephalosporin antibiotic developed by the Japanese Meiji Seika Company in 1994 for the treatment of infections caused by Gram-positive and Gram-negative bacteria, especially Gram-positive bacteria of the genus Staphylococcus, Streptococcus including Streptococcus pneumoniae, Escherichia coli, Branham catarrhalis, Klebsiella, Proteus, Haemophilus influenzae, etc. Negative bacteria and anaerobic bacteria such as Peptostreptococcus, Propionibacterium acnes, and Bacteroides have shown strong antibacterial activity. Because cefditoren pivoxil has a wide antibacterial spectrum, it is widely used in clinical practice, and its chemical structural formula is: [0003] [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/546A61K47/38A61K47/32A61P31/04C07D501/24C07D501/12
CPCA61K9/146A61K31/546A61K47/32A61K47/38A61P31/04C07D501/12C07D501/24
Inventor 张龙杰赵德千李利芳
Owner BEIJING JIMEITANG MEDICINE RES CO LTD
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