Pharmaceutical application of phenoxy acid derivative
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
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
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
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 i
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
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
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
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
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to view more 
Login to view more