Mezlocillin sodium trihydrate and preparation method thereof

A technology of mezlocillin sodium trihydrate and mezlocillin sodium is applied in the directions of active ingredients of heterocyclic compounds, organic chemistry, antibacterial drugs, etc. Good fluidity and stability

Inactive Publication Date: 2010-10-20
湖北美林药业有限公司
View PDF1 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The products are all amorphous mezlocillin sodium without crystal water. This kind of amorphous mezlocillin sodium has the disadvantage of strong hygroscopicity, which leads to low clarity and poor product stability.

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
  • Mezlocillin sodium trihydrate and preparation method thereof
  • Mezlocillin sodium trihydrate and preparation method thereof
  • Mezlocillin sodium trihydrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0036] The preparation method of mezlocillin sodium trihydrate: comprise the steps:

[0037] (1), with 5-10 parts of mezlocillin sodium raw material drug, dissolve with the water of 10-20 parts, consumption is weight part;

[0038] (2) Put the dissolving liquid into the crystallizer, slowly (1-10mL / min) add 60-90 parts by weight of eluting agent, cool to 2-8°C, keep the temperature for 2-5 hours, and wait for the solid matter to precipitate, Filter to get solids;

[0039] (3), the solid matter is rinsed with 3-5 parts of dissolving agent, and dried under ventilated or vacuum condition, drying time 3~5 hours, drying temperature 10~50 ℃, get mezlocillin sodium trihydrate ( Its function is to remove volatile impurities and moisture).

[0040] The solvent is one or more of acetone, dichloromethane, chloroform, ethanol, isopropanol, n-propanol, ether, methyl acetate, ethyl acetate, and butyl acetate.

[0041] The cooling temperature in the (2) step is 8° C. (preferred temperatur...

Embodiment 1

[0043] Weigh 10 g of mezlocillin sodium raw material, place in a 200 ml beaker, add 20 g of water to dissolve. Slowly add (8 mL / min) 90 g of isopropanol, stir while adding, control the temperature to 8° C., and keep the temperature constant for 2 hours.

[0044] Filter with suction, wash the filter cake with 5 g of isopropanol, and dry in vacuum at 10° C. for 5 hours to obtain mezlocillin sodium trihydrate.

Embodiment 2

[0046] Weigh 5 g of mezlocillin sodium raw material, place in a 200 ml beaker, add 10 g of water to dissolve. Slowly add (2 mL / min) 60 g of eluting agent, stir while adding, eluting agent is 25 g of acetone, 35 g of ethyl acetate, control the temperature to 2°C, and keep the temperature constant for 5 hours.

[0047] Suction filtration, wash the filter cake with 3 g of acetone, and vacuum-dry at 50° C. for 3 hours to obtain mezlocillin sodium trihydrate.

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

No PUM Login to view more

Abstract

The invention relates to a mezlocillin sodium trihydrate, wherein the molecular formula thereof is C21H24N5NaO8S2.3H2O. The preparation method of the mezlocillin sodium trihydrate comprises the following steps: dissolving 5-10 parts of a mezlocillin sodium bulk drug with 10-20 parts of water according to parts by weight; placing the obtained dissolving solution into a crystallizer and then adding 60-90 parts of an elution agent by weight to cool to 2-8 DEG C; keeping a constant temperature for 2-5 hours; separating out a solid and then filtering to obtain the solid; and finally washing the solid with 3-5 parts of the elution agent, and then drying under a ventilating or vacuum condition for 3-5 hours at the temperature of 10-50 DEG C to obtain the mezlocillin sodium trihydrate. The invention further provides mezlocillin sodium for medicine injection which is prepared by crushing the mezlocillin sodium trihydrate, sieving the crushed mezlocillin sodium trihydrate with a 100 mesh sieve and then carrying out aseptic-packaging. The mezlocillin sodium trihydrate and the mezlocillin sodium for medicine injection which are obtained by the invention have clean surface, good product mobility, good stability and fast dissolution velocity.

Description

technical field [0001] The invention relates to a mezlocillin sodium trihydrate, and also relates to a preparation method of the hydrate. Background technique [0002] Mezlocillin Sodium (Mezlocillin Sodium) is a semi-synthetic penicillin antibiotic, its full name is (2S, 5R, 6R)-3,3-dimethyl-6-[(2R)-[3-(methylsulfonyl)-2 -Oxo-1-imidazolidinecarboxamido]-2-phenylacetamido]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid sodium salt. [0003] Mezlocillin sodium is effective against Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Proteus, Enterobacter, Citrobacter, Serratia, Acinetobacter and penicillin-sensitive Gram-positive cocci. It has antibacterial effect and large dose has bactericidal effect. The antibacterial activity against Escherichia coli, Enterobacter, Klebsiella pneumoniae, Citrobacter, Serratia, and Acinetobacter is stronger than that of carbenicillin and ampicillin; against indole-positive Proteus, Pseudomonas aeruginosa The antib...

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): C07D499/68C07D499/16A61K31/431A61P31/04
Inventor 曾艺林刚
Owner 湖北美林药业有限公司
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