Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Pharmaceutical application of phenoxy acid derivative

A technology of derivatives and acid compounds, applied in the field of food and pharmacy, can solve the problems of low oral bioavailability, low bioavailability, poor absorption, etc.

Inactive Publication Date: 2016-07-06
HEFEI HUAFANG PHARMA SCI & TECH
View PDF2 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, due to the poor water solubility of fenofibrate, the oral bioavailability is low, which limits its full efficacy.
However, berberine hydrochloride has very little water solubility, even less fat solubility, and poor absorption in the gastrointestinal tract, resulting in low oral bioavailability, which affects its systemic therapeutic effect.
Although, fibrates and berberine have many similar pharmacological activities, they all limit their clinical use to a certain extent due to their low bioavailability. The method of utilizing the degree and exerting the synergistic effect of the two will have very important clinical significance

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
  • Pharmaceutical application of phenoxy acid derivative
  • Pharmaceutical application of phenoxy acid derivative
  • Pharmaceutical application of phenoxy acid derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Synthesis of bezafibrate berberine conjugate

[0021] Take 3.7g of berberine hydrochloride, put it into a 100ml three-necked flask, add 100ml of ethanol, adjust the pH to 7-8 with 3mol / l sodium hydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 3.6g of benzapam Specifically, keep stirring at this temperature for 1-2 hours, filter while hot, concentrate the filtrate to one-third of the original volume, cool and crystallize, filter, and dry to obtain 6.0 g of bezafibrate berberine conjugate with a yield of 85%.

Embodiment 2

[0023] Synthesis of bezafibrate berberine conjugate

[0024] Take 3.7g of berberine hydrochloride, put it into a 100ml three-necked flask, add 150ml of ethanol, adjust the pH to 7-8 with 3mol / l sodium hydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 3.8g of benzapam Specifically, keep stirring at this temperature for 1-2 hours, filter while it is hot, concentrate the filtrate to one-third of the original volume, cool and crystallize, filter, and dry to obtain 6.1 g of bezafibrate berberine conjugate, with a yield of 6.2%.

Embodiment 3

[0026] Synthesis of bezafibrate berberine conjugate

[0027] Take 3.7g of berberine hydrochloride, put it into a 100ml three-necked flask, add 100ml of ethanol, adjust the pH to 7-8 with 3mol / l sodium hydroxide, raise the temperature to 60-70°C, stir to dissolve, then add 4.0g of benzapam Specifically, keep stirring at this temperature for 1-2 hours, filter while hot, concentrate the filtrate to one-third of the original volume, cool and crystallize, filter, and dry to obtain 6.3 g of bezafibrate berberine conjugate, with a yield of 90%. ESI-MS (M + +H)m / zcalcdforC 20 h 16 NO 4 + 337.13found337.12; ESI-MS (M + +H)m / zcalcdforC 19 h 19 ClNO 4 - 360.10 found 360.15.

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 discloses pharmaceutical application of a phenoxy acid derivative and belongs to the field of biomedicine.The phenoxy acid derivative and berberine are chemically synthesized into salt, the problem that phenoxy acid derivative medicine is poor in water solubility and low in oral bioavailability, and consequently full play of the pharmaceutical effect of the medicine is limited is solved, and the problems that berberine hydrochloride is low in water solubility and lower in fat solubility, malabsorption by the gastrointestinal tract is caused, as a result, the oral bioavailability of berberine hydrochloride is low, and the systematic treatment effect of berberine hydrochloride is affected are solved.The derivative shows an excellent effect on regulating the blood glucose and blood fat of a rat with 2-type diabetes in an animal experiment.The derivative has the main effects of improving the oral glucose tolerance, promoting insulin secretion, improving insulin resistance, reducing the amount of triglyceride and the like.

Description

technical field [0001] The invention relates to the technical field of food and pharmaceuticals, in particular to the application of phenoxyacid in the preparation of products for preventing or treating obesity and related diseases or symptoms. Background technique [0002] About 12 million people die of cardiovascular disease and cerebral apoplexy every year in the world, and atherosclerosis caused by hyperlipidemia is the main cause of coronary heart disease, hypertension and cerebrovascular disease. In 2002, the global annual sales of only atorvastatin (a blood lipid-lowering drug) was nearly 8 billion US dollars, becoming the world's best-selling drug that year. It can be seen that the research and development of blood lipid-lowering drugs has significant social benefits and market prospects. Fibrate lipid-lowering drugs are a class of synthetic ligands of peroxisome proliferator-activated receptor α (PPARα), which can effectively delay the development of atherosclerosi...

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): C07D455/03A61K31/4375A61P3/10A61P3/06
CPCC07D455/03
Inventor 何勇高永好吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com