Water-soluble ketoprofen with high skin penetration speed and positive charges and prodrug of related compound

A technology of compounds and active substances, applied in the field of water-soluble prodrugs, which can solve problems such as slow skin penetration

Active Publication Date: 2015-05-13
TECHFIELDS BIOCHEM CO LTD
View PDF14 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the slow skin penetration of these drugs, it is difficult to a

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
  • Water-soluble ketoprofen with high skin penetration speed and positive charges and prodrug of related compound
  • Water-soluble ketoprofen with high skin penetration speed and positive charges and prodrug of related compound
  • Water-soluble ketoprofen with high skin penetration speed and positive charges and prodrug of related compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0062] 1. Synthesis of 2-(3-phenoxyphenyl) dimethylaminoethyl propionate acetate

[0063] 26.1 g (0.1 mol) of 2-(3-phenoxyphenyl)propionyl chloride was dissolved in 100 ml of chloroform. The mixture was cooled to 0°C. 15 ml of triethylamine and 8.9 g (0.1 mol) of dimethylaminoethanol were added to the reaction mixture with stirring. The mixture was stirred at room temperature for 3 hours. The solvent was evaporated to dryness. The residue was dissolved in 300 ml methanol. 200 ml of 5% aqueous sodium bicarbonate solution was added to the reaction mixture. The mixture was stirred for 3 hours. The mixture was evaporated to dryness. 300 ml of methanol were added to the residue with stirring. The solid was removed by filtration and washed with methanol. The solution was evaporated to dryness, and the residue was dissolved in 200 ml of chloroform. 6 g of acetic acid was added to the reaction mixture with stirring. The solids were removed by filtration. An additional 6 g o...

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 water-soluble ketoprofen with a high skin penetration speed and positive charges and a prodrug of a related compound. The invention discloses a compound shown in a structural formula 1, a preparation method of the compound, and application of the compound in preparing a medicine for treating the disease of which the state can be treated through ketoprofen or fenoprofen for people or animals. The invention further discloses a skin penetration treatment application system containing the compound.

Description

technical field [0001] The present invention relates to positively charged water-soluble precursors of 2-(3-benzoylphenyl)propionic acid (ketoprofen) and 2-(3-phenoxyphenyl)propionic acid (phenoprofen). Medicine and its use in the treatment of any ketoprofen and fenoprofen treatable condition in man or animal. Specifically, the present invention is to overcome the side effects caused by using ketoprofen and fenoprofen. These prodrugs can be administered orally or transdermally. technical background [0002] Ketoprofen and fenoprofen are propionate NSAIDs. Ketoprofen was synthesized in 1986 and has since been widely used to relieve the signs and symptoms of rheumatoid arthritis and osteoarthritis, as well as to treat dysmenorrhea. Ketoprofen can be used alone or as an adjunct in the treatment of acute biliary colic, renal colic, pain from oral surgery, severe postpartum pain, and fever (PDR Generics, 1996, second edition, Medical Economics, Montvale, New Jersey, pg 1812) ...

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
IPC IPC(8): C07C219/10C07C213/06C07C327/12C07C235/78C07C231/02A61K9/70A61P11/06A61P29/00A61P35/00A61P1/08A61P3/10A61P25/00A61P19/02A61P19/08A61P27/06A61P17/00A61P25/06A61P17/10A61P27/16
Inventor 于崇曦徐丽娜
Owner TECHFIELDS BIOCHEM CO LTD
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