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Ginsenoside cyclodextrin inclusion compound and preparation method thereof

A technology of cyclodextrin inclusion compound and ginsenoside, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of application limitations and poor water solubility, and achieve The preparation method is simple and easy, and the effect of mild conditions

Inactive Publication Date: 2016-07-20
KUNMING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] β-cyclodextrin is the most widely used cyclodextrin family, but its application is limited due to its poor water solubility

Method used

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  • Ginsenoside cyclodextrin inclusion compound and preparation method thereof
  • Ginsenoside cyclodextrin inclusion compound and preparation method thereof
  • Ginsenoside cyclodextrin inclusion compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Preparation of inclusion compound of ginsenoside F1 and hydroxypropyl-β-cyclodextrin

[0028] Add hydroxypropyl-β-cyclodextrin (161.8mg, 0.1mmol) into a 25mL reaction bottle, add 20mL of distilled water and stir until dissolved, then add ginsenoside F1 (63.87mg, 0.1mmol), and protect from light at 25°C Stir for 72 hours, filter to remove insoluble matter, then filter with a 0.45 μm microporous membrane, evaporate the filtrate to dryness to obtain a white powder, and dry in a vacuum oven for 24 hours to obtain the mixture of ginsenoside F1 and hydroxypropyl-β-cyclodextrin Solid clathrates, the clathrates of prepared ginsenosides and cyclodextrins were all characterized by X-ray powder diffraction ( image 3 ), the water solubility comparison before and after inclusion is shown in Table 1.

Embodiment 2

[0029] Example 2: Preparation of inclusion compound of ginsenoside F1 and sulfobutyl ether-β-cyclodextrin

[0030] Add sulfobutyl ether-β-cyclodextrin (700mg, 0.5mmol) into a 25mL reaction bottle and add 20mL of distilled water and stir until dissolved, then add ginsenoside F1 (63.87mg, 0.1mmol), and protect from light at 25°C Ultrasound for 10 hours, filter to remove insoluble matter, then filter with a 0.45 μm microporous membrane, evaporate the filtrate to dryness to obtain a white powder, dry in a vacuum oven for 24 hours, and obtain ginsenoside F1 and sulfobutyl ether-β-cyclodextrin The solid clathrate of the obtained ginsenoside and the clathrate of cyclodextrin are all characterized by X-ray powder diffraction ( Figure 4 ), the water solubility comparison before and after inclusion is shown in Table 1.

Embodiment 3

[0031] Example 3: Preparation of inclusion compound of ginsenoside Re and hydroxypropyl-β-cyclodextrin

[0032]Add hydroxypropyl-β-cyclodextrin (1132.6mg, 0.7mmol) into a 25mL reaction bottle, add 20mL of distilled water and stir until dissolved, then add ginsenoside Re (94.72mg, 0.1mmol), and protect from light at 60°C Sonicate for 1 hour, filter to remove insoluble matter, then filter with a 0.45 μm microporous membrane, evaporate the filtrate to dryness to obtain a white powder, and dry it in a vacuum oven for 24 hours to obtain the mixture of ginsenoside Re and hydroxypropyl-β-cyclodextrin Solid clathrates, the clathrates of prepared ginsenosides and cyclodextrins were all characterized by X-ray powder diffraction ( Figure 7 ), the water solubility comparison before and after inclusion is shown in Table 1.

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Abstract

The invention discloses a ginsenoside cyclodextrin inclusion compound and a preparation method thereof.The compound comprises ginsenoside and cyclodextrin, wherein the molar ratio of ginsenoside to cyclodextrin is (1:2)-(1:20), the ginsenoside is ginsenoside F1 or ginsenoside Re or ginsenoside Rd or ginsenoside Rb2 or ginsenoside Rc, and the cyclodextrin is hydroxypropyl-beta-cyclodextrin or sulfobutyl ether-beta-cyclodextrin; the compound is prepared through a saturated solution method or an ultrasonic method; after ginsenoside and cyclodextrin form the compound, the solubility of the compound in water is greatly improved. The preparation method is simple and convenient to implement, mild in condition, easy to implement and capable of being used for developing novel prepartions of ginsenoside.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and specifically relates to a cyclodextrin inclusion compound of five ginsenosides and a preparation method thereof. Background technique [0002] Ginsenosides are a class of triterpenoid saponins, which mainly exist in the precious Chinese medicinal materials ginseng and American ginseng, and are their active ingredients, and have good pharmacological effects such as anti-tumor, anti-Alzheimer's disease, and anti-cardiovascular disease. However, ginsenosides generally have poor water solubility and are unstable, resulting in low bioavailability in vivo, unable to exert their medicinal effects well, and even produce some toxic and side effects. Therefore, it is necessary to take necessary technical means to improve it to improve its water solubility and other properties, so that it is more suitable for medicinal use. [0003] Cyclodextrin (CD for short) is a cyclic oligosaccharide produced by a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/704A61P35/00A61P25/28A61P9/00
CPCA61K31/704
Inventor 廖霞俐任玉峰王智苏艳芳杨波
Owner KUNMING UNIV OF SCI & TECH
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