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Method for preparing isoquercetin inclusion compound

A technology of isoquercetin and inclusion complex is applied in the field of drug carrier preparation, can solve problems such as application limitation, and achieve the effects of improving water solubility, stable structure and good water solubility

Active Publication Date: 2016-12-07
PROYA COSMETICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the low water solubility of hydroxypropyl β-cyclodextrin itself (18.5 g / L, 25 ℃), the application of a single hydroxypropyl β-cyclodextrin inclusion compound is greatly limited

Method used

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  • Method for preparing isoquercetin inclusion compound
  • Method for preparing isoquercetin inclusion compound
  • Method for preparing isoquercetin inclusion compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A kind of preparation method of isoquercetin clathrate, adopts following steps:

[0028] A. In a 100 mL round bottom flask, add 8.04 g of poloxamer 188 (poloxamer 188) dissolved in 30 mL of absolute ethanol, add 0.12 g of triethylamine, and slowly add 0.078 g of acetyl chloride under magnetic stirring conditions , stirred and reacted in an ice-water bath for 3 h, then suction filtered, and the solvent was removed by a rotary evaporator to obtain 6.1 g of a white liquid product, acetylated poloxamer (MPoloxamer, product 1), with a yield of 75.80%.

[0029] B. In a 100 mL round bottom flask, add 0.20 g of succinic anhydride (SA) and 0.12 g of 4-dimethylaminopyridine (DMAP) dissolved in 50 mL of absolute ethanol, and slowly add 8.30 g of MPoloxamer anhydrous weak. React at 25°C for 4 h, spin off the solvent with a rotary evaporator, add diethyl ether to precipitate, filter with suction, wash the precipitate with diethyl ether 3 times, and obtain the white powdery solid pr...

Embodiment 2

[0033] A kind of preparation method of isoquercetin clathrate, adopts following steps:

[0034] A. In a 100 mL round bottom flask, add 4.82 g of poloxamer 188 (poloxamer 188) dissolved in 30 mL of absolute ethanol, add 0.07 g of triethylamine, and slowly add 0.049 g of acetyl chloride under magnetic stirring conditions , stirred and reacted in an ice-water bath for 4 h, then suction filtered, and the solvent was removed by a rotary evaporator to obtain 4.18 g of a white liquid product, acetylated poloxamer (MPoloxamer, product 1), with a yield of 86.72%.

[0035] B. In a 100 mL round bottom flask, add 0.10 g of succinic anhydride (SA) and 0.08 g of 4-dimethylaminopyridine (DMAP) dissolved in 30 mL of absolute ethanol, and slowly add 4.09 g of MPoloxamer anhydrous weak. React at 30°C for 5 h, spin off the solvent with a rotary evaporator, add diethyl ether to precipitate, filter with suction, and wash the precipitate with diethyl ether 3 times to obtain a white powdery solid pro...

Embodiment 3

[0039] A kind of preparation method of isoquercetin clathrate, adopts following steps:

[0040] A. In a 100 mL round bottom flask, add 9.98 g of poloxamer 188 (poloxamer 188) dissolved in 30 mL of absolute ethanol, add 0.15 g of triethylamine, and slowly add 0.098 g of acetyl chloride under magnetic stirring conditions , stirred and reacted in an ice-water bath for 5 h, then suction filtered, and the solvent was removed by a rotary evaporator to obtain 8.01 g of a white liquid product, acetylated poloxamer (MPoloxamer, product 1), with a yield of 88.91%.

[0041] B. In a 100 mL round bottom flask, add 0.40 g of succinic anhydride (SA) and 0.20 g of 4-dimethylaminopyridine (DMAP) dissolved in 65 mL of absolute ethanol, and slowly add 16.04 g of MPoloxamer anhydrous weak. React at 35°C for 7 h, spin off the solvent with a rotary evaporator, add diethyl ether to precipitate, filter with suction, wash the precipitate with diethyl ether 4 times, and obtain the white powdery solid ...

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Abstract

The invention relates to a method for preparing an isoquercetin inclusion compound. The method is characterized by comprising the following steps: A, preparing acetylated poloxamer from poloxamer, acetyl chloride and triethylamine in a molar ratio of 1:1:1.2; B, preparing poloxamer-succinate from poloxamer and succinate; C, preparing poloxamer-hydroxypropyl beta-cyclodextrin polymer from hydroxypropyl beta-cyclodextrin and the poloxamer-succinate in a molar ratio of 1:1-1.5; and D, slowly adding an isoquercetin saturated solution into the poloxamer-hydroxypropyl beta-cyclodextrin polymer saturated solution in a volume ratio of 1:1, sufficiently stirring to react for 12-24 hours, adding diethyl ether to separate solid, performing pump-filtering, washing and drying to obtain the isoquercetin inclusion compound. The isoquercetin inclusion compound has the advantages of good water solubility, high encapulation rate and stable product.

Description

technical field [0001] The invention relates to the field of preparation of drug carriers, in particular to a preparation method of isoquercetin inclusion compound. Background technique [0002] Isoquercitrin is a representative compound of flavonols, with a melting point of 225-227 °C, almost insoluble in cold water and slightly soluble in boiling water. It exists widely in various tissues such as fruits, leaves, stems and roots of various plants in the form of sugar anhydride. Isoquercetin has a variety of biological activities and pharmacological effects such as dilating coronary vessels, lowering blood lipids, anti-platelet aggregation, anti-inflammation, anti-oxygen free radicals, anti-allergy, etc. Therefore, isoquercetin and its derivatives are used in medicine, food, Cosmetics and other fields have broad application prospects. Hydroxypropyl β-cyclodextrin (HP-β-CD) has a special structure of ring-shaped hollow cylinder, hydrophilic outside the ring and hydrophobic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/14A61K31/7048A61P9/10A61P3/06A61P7/02A61P29/00A61P39/06A61P37/08
CPCA61K9/146A61K31/7048
Inventor 周浩淼陈玉燕金激吕旭阳毕永贤蒋丽刚
Owner PROYA COSMETICS
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