Cefoxitin sodium superfine-powder preparation and preparation method thereof

A technology of cefoxitin sodium and ultrafine powder, which is applied in the field of medicine, can solve the problems of obvious side effects and low purity of active ingredients, and achieve the effect of improving purity, less impurities and good solubility

Inactive Publication Date: 2014-09-17
杭州长典老一元健康管理有限公司
View PDF4 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, some methods of cefoxitin sodium preparations have been disclosed at home and abroad, but the cefoxitin sodium preparations made by these methods have problems such as low purity of active ingredients and obvious side effects caused thereby

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cefoxitin sodium superfine-powder preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Add 120 g of 7-α-methoxy-3-deacetyl cephalothin benzathine salt into 1.44 L of acetone, cool to -70 ° C ~ -80 ° C, add 80 g of chlorosulfonyl acetocyanate, and wait for the reaction to When 7-α-methoxy-3-deacetyl cephalothin benzathine salt ≤ 1.5%, it ends; the resulting reaction solution is poured into deionized water, and the hydrolysis reaction is carried out under stirring at a temperature of 0~25°C. In the hydrolyzate Add 1.92L of ethyl acetate, stir for 15 minutes and then filter. After the filtrate is allowed to stand and separate phases, collect the organic phase. Add activated carbon to the above organic phase, stir for 40 minutes and then filter. Concentrate the above filtrate under reduced pressure. When the concentrated juice has crystals Stop concentrating, then raise the temperature to 40°C, add dichloromethane to the concentrated solution at the same time, stir for 40 minutes, and filter until the wet product of cefoxitin acid is obtained.

[0029] Dissol...

Embodiment 2

[0033] Add 120 g of 7-α-methoxy-3-deacetyl cephalothin benzathine salt into 1.44 L of acetone, cool to -70 ° C ~ -80 ° C, add 80 g of chlorosulfonyl acetocyanate, and wait for the reaction to When 7-α-methoxy-3-deacetyl cephalothin benzathine salt ≤ 1.5%, it ends; the resulting reaction solution is poured into deionized water, and the hydrolysis reaction is carried out under stirring at a temperature of 0~25°C. In the hydrolyzate Add 1.92L of ethyl acetate, stir for 15 minutes and then filter. After the filtrate is allowed to stand and separate phases, collect the organic phase. Add activated carbon to the above organic phase, stir for 40 minutes and then filter. Concentrate the above filtrate under reduced pressure. When the concentrated juice has crystals Stop concentrating, then raise the temperature to 40°C, add dichloromethane to the concentrated solution at the same time, stir for 40 minutes, and filter until the wet product of cefoxitin acid is obtained.

[0034] Dissol...

Embodiment 3

[0039] Example 3 - Safety Test (Allergy Test)

[0040] Take 20 white guinea pigs, weighing 280g~350g, male and female. Divided into 4 groups, 5 Meizu, cefoxitin sodium for injection (100mg / mL), ovalbumin solution positive group (30mg / mL), normal saline control group.

[0041]Each group first injected the corresponding solution 0.5mL intraperitoneally every other day, for a total of 3 times, and then divided the animals in the above groups into two groups. One group received cefoxime for injection respectively on the 14th day after the first administration. Butyrate sodium, ovalbumin solution and normal saline 2mL / rat were challenged, and the allergic reaction of the animals after injection was observed, and graded according to the grade standard of allergic reaction. Group 2 was attacked in the same way 21 days after the first injection, and observed. If the grade of allergic reaction is more than 2 grades, the allergic reaction is judged to be positive.

[0042] The resu...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
diameteraaaaaaaaaa
Login to view more

Abstract

The invention discloses a preparation method of cefoxitin sodium superfine-powder preparations. The method comprises the following steps: 1, at room temperature, adding 7-alpha-methoxy-3-deacetyl cefalotin benzathine to acetone; 2, pouring reaction liquid obtained after reaction into ionized water, stirring the obtained mixture to carry out a hydrolysis reaction at 0-25 DEG C; 3, adding ethyl acetate to the obtained hydrolysis liquid; 4, adding activated carbon into an organic phase, stirring for 40 minutes, filtering the obtained product; 5, dissolving sodium iso-octoate into an ethanol solution; and 6, crushing dried cefoxitin sodium into superfine powder by using an air flow. The invention also discloses a cefoxitin sodium superfine-powder preparation which comprises special cefoxitin sodium superfine powder. According to the preparation method, the purity of cefoxitin sodium is greatly improved, so that the cefoxitin sodium has the advantages of high purity, less impurities, small particles, large specific surface area, good solubility, good activity and the like.

Description

technical field [0001] The invention provides a superfine powder preparation of cefoxitin sodium and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cefoxitin sodium, the chemical name is 3-carbamoyloxymethyl-7-methoxy-8-oxo-7-(2-thiopheneacetamido)-5-thio-1-azabicyclo (4.2 .0) Oct-2-ene-2-carboxylic acid sodium salt, English name Cefoxitin, molecular formula C 16 h 16 N 3 NaO 7 S 2 , molecular weight: 449.43, the chemical structural formula is as follows: [0003] [0004] Cefoxitin sodium is a cephamycin antibiotic, which is produced by Streptomyceslactamdurans, a class of antibiotics produced by semi-synthesis. Its mother nucleus is similar to cephalosporins, and it is listed as into second-generation cephalosporins. Cefoxitin sodium has weak antibacterial ability against Gram-positive bacteria and strong effect against Gram-negative bacteria. It is mainly used clinically for respiratory tract infection, ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/57C07D501/04A61K9/14A61K31/546A61P31/04
CPCC07D501/57A61K9/14A61K31/546C07D501/04
Inventor 傅苗青李凤生陈宗东
Owner 杭州长典老一元健康管理有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap