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Linarin inclusion compound as well as preparation method and application thereof

A technology for cymenoside and clathrate, applied in the field of cymenoside clathrate and preparation thereof, can solve the problems of low drug bioavailability, poor lipid solubility, etc., achieve excellent anti-inflammatory and anti-allergic effects, and improve stability the effect of improving bioavailability

Pending Publication Date: 2019-11-08
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, Menghuaside is a heat-sensitive compound, which is easily degraded by heat, insoluble in water, and poor in fat solubility.
Therefore, its application in medicine is limited, and the bioavailability of the medicine prepared by it is low

Method used

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  • Linarin inclusion compound as well as preparation method and application thereof
  • Linarin inclusion compound as well as preparation method and application thereof
  • Linarin inclusion compound as well as preparation method and application thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0035] A preparation method of clathrate, comprising the following steps:

[0036] a) dissolving the fenugreek in an organic solvent to make a montinalin solution;

[0037] b) dissolving the clathrate material in water to make clathrate material solution;

[0038] c) heating and stirring the mongoside solution and the clathrate material solution for clathrate;

[0039] Steps a) and b) are in no sequence;

[0040] The clathrate material is selected from at least one of cyclodextrin and cyclodextrin derivatives;

[0041] The mass ratio of the montanoside to the clathrate material is 0.5-1.6:8-32;

[0042] The heating temperature is 40-60°C;

[0043] The stirring time is 2-9 hours, and the stirring speed is 300-600 rpm.

[0044] In order to improve the problem of the poor solubility of fenugreek glycosides, the present invention adopts clathrate technology, which means that one molecule is occluded in the hole structure of another molecule to form an clathrate. This kind of...

Embodiment 1

[0085] A preparation method for clathrate inclusion compound, comprising the steps of:

[0086] (a) dissolving fenugreek in ethanol to obtain a montanoside solution;

[0087] (b) dissolving hydroxypropyl-β-cyclodextrin in water to obtain an aqueous solution of hydroxypropyl-β-cyclodextrin;

[0088] (c) Add the fenugreek solution in step (a) dropwise into the aqueous solution of hydroxypropyl-β-cyclodextrin in step (b), and stir for 4 hours at a temperature of 60°C at a stirring speed of 400rpm at room temperature Stand still for 12 hours, remove the solvent by rotary steaming, let stand for 1.5 hours to cool to room temperature, and freeze at -80°C for 24 hours to obtain the inclusion compound of pergoside;

[0089] The mass ratio of the saponin, ethanol, hydroxypropyl-β-cyclodextrin and water is 0.5:10:24:10.

Embodiment 2

[0091] A preparation method of the clathrate, comprising the steps of:

[0092] (a) dissolving hydroxypropyl-β-cyclodextrin in water to obtain an aqueous solution of hydroxypropyl-β-cyclodextrin;

[0093] (b) dissolving fenugreek in ethanol to obtain a montanoside solution;

[0094] (c) Add the fenugreek solution in step (a) dropwise into the aqueous solution of hydroxypropyl-β-cyclodextrin in step (b), and stir for 6 hours at a temperature of 50°C at a stirring speed of 500rpm at room temperature Stand still at low temperature for 12 hours, remove the solvent by rotary evaporation, let stand for 1 hour to cool to room temperature, and freeze at -80°C for 24 hours to obtain the inclusion compound of pergoside;

[0095] The mass ratio of the saponin, ethanol, hydroxypropyl-β-cyclodextrin and water is 0.5:10:15.5:20.

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Abstract

The invention relates to the technical field of inclusion, in particular to a linarin inclusion compound as well as a preparation method and application thereof. The preparation method of the linarininclusion compound comprises the steps as follows: a) dissolving linarin in an organic solvent to prepare a linarin solution; b) dissolving an inclusion material in water to prepare an inclusion material insulation; and c) heating and stirring the linarin solution and the inclusion material solution for inclusion, wherein the steps a) and b) have no sequence; the inclusion material is selected from at least one of cyclodextrin and cyclodextrin derivatives; the mass ratio of linarin to the inclusion material is (0.5-1.6):(8-32); the heating temperature is 40-60 DEG C; the stirring time is 2-9 hand the stirring speed is 300-600 rpm. By use of specific feed ratio, specific heating time, stirring speed and stirring time, the inclusion compound with higher drug loading capacity can be obtained, and the inclusion compound has excellent anti-inflammatory and anti-allergic effects.

Description

technical field [0001] The present invention relates to the field of clathrate technology, in particular, to a clathrate clathrate and its preparation method and application. Background technique [0002] Menghuaside is a natural flavonoid glycoside widely present in plants such as Asteraceae wild chrysanthemum and Budisma. It has a wide range of physiological and pharmacological activities, can prevent diabetes and improve diabetes, and also has the effect of inhibiting aldose reductase, phosphodiesterase, Staphylococcus aureus, beta hemolytic streptococcus, etc., can protect the liver, and protect the liver Chronic bronchitis has a certain effect. It also has anti-aging, anti-hypoxia effect, anti-adverse stimulation effect, two-way regulation effect on the body, and anti-fatigue effect. [0003] However, Menghuaside is a heat-sensitive compound, which is easily degraded by heat, insoluble in water, and poor in fat solubility. Therefore, its application in medicine is li...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K9/19A61K31/7048A61P29/00A61P37/08A61P27/02
CPCA61K47/6951A61K9/19A61K9/0048A61K31/7048A61P29/00A61P37/08A61P27/02
Inventor 刘洋张启蒙王童
Owner ZHENGZHOU UNIV
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