Cefotiam hydrochloride medicament composition sterile powder injection and preparation method thereof

A technology of cefotiam hydrochloride and sterile powder injection, which is applied in the field of drug synthesis and preparation, can solve the problems of low yield, low product yield and high solvent residue, and achieves low content of related substances, high purity and stability Good results

Active Publication Date: 2009-11-25
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the production of cefotiam aseptic powder, sodium thiosulfate reagent is added to the reaction system for the appearance color of the finished cephalosporin to make the appearance color better, but the yield of the product is low and the solvent residue is high
[0009] In summary, although the prior art has disclosed multiple synthetic methods of cefotiam hydrochloride, existing synthetic methods exist the obtained cefotiam hydrochloride purity is low, the steps are numerous, and the defects such as low yield, so , researchers start from the existing technology, by choosing a good synthesis method, and strictly controlling the process conditions of each step, so as to achieve the purpose of solving the defects of the existing technology, in view of this, this invention is proposed

Method used

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  • Cefotiam hydrochloride medicament composition sterile powder injection and preparation method thereof
  • Cefotiam hydrochloride medicament composition sterile powder injection and preparation method thereof
  • Cefotiam hydrochloride medicament composition sterile powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] (1) Weigh 27.2 grams of 7-ACA and add it to 140 mL of anhydrous acetonitrile to form a suspension; add 17.3 grams of 5-mercapto-1-dimethylamino-ethyl-1H to the formed suspension -tetrazolium to form a mixed solution, and when the temperature of the mixed solution was kept at -5 to 5°C, 160 mL of boron trifluoride-diethyl ether complex (containing 20 grams of boron trifluoride, 0.3 mol, mixed at 30 React at ℃ for 2.5 hours, then cool to 5℃, add 30mL of 37% hydrochloric acid dropwise, adjust the pH value to 3.0 with 28% ammonia water in an ice bath, grow crystals for 1 hour, filter, wash the filter cake with 50ml of acetone, and set at 45℃ After drying, 33.1 g of intermediate 1 were obtained.

[0057] (2) Dissolve 18.6 grams of 2-formylamino-thiazolyl-4-acetic acid in 250 mL of dichloromethane, cool to -20 ° C, add PCl in batches, stir while adding, the stirring speed is 130 rpm Minutes, after the addition was complete, continue to stir for 2 hours at a stirring speed of...

Embodiment 2

[0062] (1) Weigh 27.2 grams of 7-ACA and add it to 140 mL of anhydrous acetonitrile to form a suspension; add 25.95 grams of 5-mercapto-1-dimethylamino-ethyl-1H to the formed suspension -tetrazolium to form a mixed solution. When the temperature of the mixed solution was kept at 0-5°C, 170 mL of boron trifluoride-diethyl ether complex (containing 23 grams of boron trifluoride, 0.35 mol) was added, and the mixture was mixed uniformly at 38 React at ℃ for 2 hours, then cool to 5℃, add 28mL of 37% hydrochloric acid dropwise, adjust the pH value to 3.0 with 25% ammonia water in an ice bath, grow crystals for 1.5 hours, filter, wash the filter cake with 50ml of acetone, and store at 40℃ After drying, 32.8 g of intermediate 1 were obtained.

[0063] (2) Dissolve 18.6 grams of 2-formylamino-thiazolyl-4-acetic acid in 250 mL of dichloromethane, cool to -20°C, add PCl in batches, stir while adding, the stirring speed is 120 rpm minutes, after the addition was complete, the stirring wa...

Embodiment 3

[0068] (1) Weigh 27.2 grams of 7-ACA and add it to 140 mL of anhydrous acetonitrile to form a suspension; add 13.84 grams of 5-mercapto-1-dimethylamino-ethyl-1H to the formed suspension -tetrazolium to form a mixed solution. When the temperature of the mixed solution was kept at -2 to 2°C, 160 mL of boron trifluoride-diethyl ether complex (containing 20 grams of boron trifluoride, 0.3 mol, mixed at 30 React at -38°C for 2-2.5 hours, then cool to 2°C, add 37% hydrochloric acid dropwise, adjust the pH value to 3.0 with 27% ammonia water in an ice bath, grow crystals for 1 hour, filter, and wash the filter cake with 50ml acetone , 33.1 g of Intermediate 1 were obtained after drying at 45 °C.

[0069] (2) Dissolve 18.6 grams of 2-formylamino-thiazolyl-4-acetic acid in 250 mL of dichloromethane, cool to -20 ° C, add PCl in batches, stir while adding, the stirring speed is 110 rpm Minutes, after the addition was complete, continue to stir for 3 hours at a stirring speed of 60 rpm, ...

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PUM

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Abstract

The present invention discloses a cefotiam hydrochloride medicament composition sterile powder injection, including 500 to 600 weight shares of cefotiam hydrochloride and 110 to 150 weight shares of anhydrous sodium carbonate. The cefotiam hydrochloride medicament composition sterile powder injection has advantages of a good stability and a high purity. The invention also discloses a method for preparing the cefotiam hydrochloride medicament composition sterile powder injection, including steps of weighing the cefotiam hydrochloride and the anhydrous sodium carbonate according to the formula amount separately and mixing them in a sterile container uniformly. The method is simple, and the cefotiam hydrochloride prepared by the above method has a good stability.

Description

technical field [0001] The invention belongs to the field of drug synthesis and preparation, and more specifically, the invention relates to a cefotiam hydrochloride pharmaceutical composition aseptic powder injection and a preparation method thereof. Background technique [0002] Cefotiam is a second-generation semi-synthetic cephalosporin developed by Takeda Corporation of Japan and first launched in Japan in 1981. The effect of this product on Gram-positive bacteria is close to that of cefazolin, and it has better effect on Gram-negative bacteria, such as Haemophilus, Escherichia coli, Klebsiella, and Proteus mirabilis. , Citrobacter, and indole-positive Proteus also have antibacterial effects. Clinical use of stable dihydrochloride for intravenous administration is used to treat infections caused by sensitive bacteria, such as pneumonia, bronchitis, biliary tract infection, peritonitis, urinary tract infection, infection and sepsis caused by surgery and trauma, etc. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/546A61K47/02A61P31/04C07D501/36C07D501/06C07D501/12
Inventor 李明华宋良伟朱全明
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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