Supramolecular composite of isosteviol or derivative thereof and preparation method thereof

A technology of isosteviol and its derivatives, applied in the field of supramolecularized compositions, can solve the problems of difficult absorption and low bioavailability, and achieve the effects of easy absorption, high preparation efficiency and easy storage

Active Publication Date: 2012-11-28
JIANGSU STEVEN BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0027] In order to solve the problems that isosteviol and its derivatives are only slightly soluble in water, difficult to absorb when taken orally, and have low bioavailability, the present invention discloses a supramolecular composition of isosteviol or its derivatives and β-cyclodextrin, and the preparation method of the composition

Method used

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  • Supramolecular composite of isosteviol or derivative thereof and preparation method thereof
  • Supramolecular composite of isosteviol or derivative thereof and preparation method thereof
  • Supramolecular composite of isosteviol or derivative thereof and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0051] Preparation of isosteviol: 0.6% stevioside aqueous solution, add sulfuric acid to make the concentration 4% (W / W), mix well, heat at reflux for 20 minutes, filter the white precipitate, and dry to get crude isosteviol (content is about 40%), isosteviol can also be purified by column chromatography.

[0052] Preparation of β-cyclodextrin supramolecularization composition of isosteviol: Mix 500 grams of β-cyclodextrin with 2500 ml of pure water, keep warm at 60°C and stir to form a solution, add 150 grams of isosteviol, keep stirring for more than 12 hours , cooled slowly, left overnight, filtered, and vacuum-dried to obtain a white clathrate, which contained 1.3% isosteviol in the solid.

Embodiment 2

[0054] Mix 100g of β-cyclodextrin with 300ml of pure water at room temperature, stir to make a suspension, add 20g of solid isosteviol (content 70%-95%), mix well, and grind (about 5-8 hours) , cooled, filtered, and dried at 40°C to obtain a white clathrate.

Embodiment 3

[0056] Weigh 5 grams of β-cyclodextrin and add 30 milliliters of water to make a suspension, add one-fifth of its mass (ie 1 gram) isosteviol powder, mix, and grind for 2 hours at 25°C to form a paste. Cool, filter, and dry at 60°C until it becomes powdery to obtain a white clathrate.

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Abstract

The invention relates to a supramolecular composite of isosteviol or a derivative thereof and a preparation method thereof, and the form thereof is a white solid inclusion compound. The mass ratio of the isosteviol or the derivative thereof in the composite to beta-cyclodextrin (or the derivative thereof) is 1:3.57-1:107.1, namely the content of the isosteviol or the derivative thereof of the composite is 0.925%-21.88%; and the solid inclusion composite is the white solid composite prepared by mixing the isosteviol or the derivative thereof with the beta-cyclodextrin in the presence of water.The preparation method of the composite comprises the steps of adding the isosteviol or the derivative thereof with the mass (dry mass) of 1 / 3.57-1 / 107.1 into water solution or suspensoid of beta-cyclodextrin, mixing, grinding or carrying out ultrasonic treatment, cooling, filtering, obtaining a solid matter and vacuum drying for preparation to obtain the product in the invention, and the preparation method does not need to add any organic solvent during the preparation process. The composite features good solubility and easy processing, thereby being a good health care food or drug raw material.

Description

technical field [0001] The invention relates to a supramolecularized composition of isosteviol or its derivatives, and a preparation method of the composition. Background technique [0002] Isosteviol is a tetracyclic diterpenoid compound, which is the aglycon of stevioside, that is, the isomer of steviol. It contains a carboxyl group and a carbonyl group in its molecule, and its molecular weight is 318. A large number of studies have shown that isosteviol and its derivatives play an important role in lowering blood sugar, antihypertensive, protecting myocardium, and as DNA synthetase inhibitors and anticancer agents. The structure of isosteviol is shown in formula 1. [0003] [0004] Isosteviol derivatives, as structural analogs of isosteviol, also have similar or stronger biological activities. For example, Dihydroisosteviol (Dihydroisosteviol, formula 2) can hinder the secretion of intestinal juice induced by cholera toxin, and is expected to become a new class of C...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A23L1/30A61K31/19A61K47/40A61P3/10A61P9/12A61P9/00A61P43/00A61P35/00A23L33/10
Inventor 陈育如刘虎姜中玉曹阳
Owner JIANGSU STEVEN BIOTECHNOLOGY CO LTD
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