Cefathiamidine composition

A cefathiamidine and composition technology, which is applied in the directions of inactive components of polymer compounds, antibacterial drugs, organic active components, etc., can solve the problems of long-term storage, easy oxidative deterioration, short antibacterial time, etc., and achieves hard oxidative deterioration. , long antibacterial time, good stability

Active Publication Date: 2018-11-09
YOUCARE PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Existing cefathiamidine preparations have disadvantages such as poor stability, easy oxidation and deterioration, inability to store for a long time, short antibacterial time, etc.

Method used

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  • Cefathiamidine composition
  • Cefathiamidine composition
  • Cefathiamidine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] First, 250 grams of hydroxypropyl-β-cyclodextrin is dissolved in 1500 grams of water for injection to obtain a hydroxypropyl-β-cyclodextrin solution. Then add 50 grams of cefathiamidine into the hydroxypropyl-β-cyclodextrin solution, heat to 40°C, and heat and stir at 40°C for 4 hours for inclusion, after the inclusion is completed, the mixture is cooled to room temperature and filtered After obtaining the filtrate.

[0026] 15 grams of low-molecular-weight dextran was heated and dissolved with 45 grams of water for injection to obtain a low-molecular-weight dextran solution, cooled to room temperature, and filtered. Add the low-molecular-weight dextran solution into the inclusion solution of hydroxypropyl-β-cyclodextrin and cefathiamidine, stir to dissolve, then add 5 grams of vitamin C, stir to dissolve, and adjust the pH value with a 5% citric acid solution to 5.0, finally add water for injection to 2000ml, stir evenly, and then filter and sterilize with a 0.22μm mi...

Embodiment 2

[0028] Firstly, 450 grams of hydroxypropyl-β-cyclodextrin is dissolved with 2600 grams of water for injection to obtain a hydroxypropyl-β-cyclodextrin solution. Then add 100 grams of cefathiamidine into the hydroxypropyl-β-cyclodextrin solution, heat to 45°C, heat and stir at 45°C for 3.5 hours for inclusion, after the inclusion, cool the mixture to room temperature, filter After obtaining the filtrate.

[0029] Heat and dissolve 25 grams of low-molecular-weight dextran with 80 grams of water for injection to obtain a low-molecular-weight dextran solution, cool to room temperature, and filter. Add the low-molecular-weight dextran solution into the inclusion solution of hydroxypropyl-β-cyclodextrin and cefathiamidine, stir to dissolve, then add 8 grams of vitamin C, stir to dissolve, and adjust the pH value with a 6% citric acid solution To 4.8, finally add water for injection to 3500ml, stir evenly, and then filter and sterilize with a 0.22μm microporous membrane, and fill it...

Embodiment 3

[0031] First, 800 grams of hydroxypropyl-β-cyclodextrin is dissolved with 4400 grams of water for injection to obtain a hydroxypropyl-β-cyclodextrin solution. Then add 200 grams of cefathiamidine into the hydroxypropyl-β-cyclodextrin solution, heat to 50°C, and heat and stir at 50°C for 3 hours to carry out inclusion. After the inclusion is completed, the mixture is cooled to room temperature and filtered. After obtaining the filtrate.

[0032] 40 grams of low-molecular-weight dextran was heated and dissolved with 160 grams of water for injection to obtain a low-molecular-weight dextran solution, cooled to room temperature, and filtered. Add the low-molecular-weight dextran solution into the inclusion solution of hydroxypropyl-β-cyclodextrin and cefathiamidine, stir to dissolve, then add 12 grams of vitamin C, stir to dissolve, and adjust the pH value with a 7% citric acid solution To 4.7, finally add water for injection to 6000ml, stir evenly, and then filter and sterilize w...

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Abstract

The invention discloses a cefathiamidine composition. The cefathiamidine composition comprises cefathiamidine, hydroxypropyl-beta-cyclodextrin, low molecular dextran, vitamin C and citric acid. Cefathiamidine is coated with hydroxypropyl-beta-cyclodextrin. A preparation method of the cefathiamidine composition comprises the following steps of 1, dissolving hydroxypropyl-beta-cyclodextrin by injection water to obtain a hydroxypropyl-beta-cyclodextrin solution, 2, adding cefathiamidine into the hydroxypropyl-beta-cyclodextrin solution, carrying out clathration under the condition of heating stirring, carrying out cooling to a room temperature, and carrying out filtration to obtain a filtrate, and 3, heating and dissolving low molecular dextran in injection water, cooling the solution to a room temperature, carrying out filtration, adding the filtrate into an inclusion solution of hydroxypropyl-beta-cyclodextrin and cefathiamidine, carrying out stirring dissolution, adding vitamin C into the solution, carrying out stirring dissolution, adjusting a pH value by a citric acid solution, adding injection water into the solution, carrying out degerming filtration, carrying out loading, carrying out freeze-drying and carrying out packaging to obtain the cefathiamidine composition.

Description

technical field [0001] The invention relates to cefathiamidine, in particular to a cefathiamidine composition, and belongs to the technical field of medicine. Background technique [0002] Cefathiamidine, chemical name: (6R,7R)-3[(acetoxy)methyl]-7-[α-(N,N'-diisopropylamidinothio)-acetamido]8- Oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid betaine. Molecular formula: C 19 h 28 N 4 o 6 S 2 , molecular weight: 472.59. [0003] Cefathiamidine is white or off-white crystalline powder; almost odorless, hygroscopic. [0004] Cefathiamidine is the first-generation cephalosporin, which was first used clinically in China. The antibacterial spectrum is similar to that of cephalothin, and it has a stronger effect on Staphylococcus aureus, Streptococcus viridans, and Pneumococcus, and has unique antibacterial activity against Enterococcus, and is mainly used for respiratory tract infections caused by Staphylococcus aureus, Pneumococcus, and Streptococcus, Biliary tra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/40A61K31/545A61K9/19A61K47/22A61K47/26A61P31/04
Inventor 李琦杨磊
Owner YOUCARE PHARMA GROUP
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