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Resveratrol clathrate and preparation method of resveratrol clathrate preparations

A technology of resveratrol and inclusion compound, applied in the field of medicine, can solve the problems of difficult to achieve therapeutic effect, low bioavailability, easy isomerization, etc., achieves enrichment of preparation varieties, expands application prospects, stability and stability. The effect of improving bioavailability

Inactive Publication Date: 2014-07-30
JILIN INST OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, resveratrol is insoluble in water (solubility in water is 0.03 g / L), oral absorption is poor, bioavailability is low, isomerization is prone to occur under ultraviolet irradiation, and it is difficult to achieve the expected therapeutic effect. The new technology will make it into clathrate first, and then make it into various preparations, which will greatly improve its stability and bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Preparation of resveratrol inclusion compound: Take 10g of β-cyclodextrin to make a saturated aqueous solution, stir it magnetically, weigh 5g of resveratrol, dissolve it in a small amount of absolute ethanol, slowly drop in the above-mentioned β-cyclodextrin to saturate Stir in the aqueous solution for a specified time, refrigerate at 4°C for 24 hours, filter under reduced pressure, wash the filter cake with a small amount of absolute ethanol, and dry the filter cake under vacuum to constant weight to obtain clathrate powder.

Embodiment 2

[0013] Preparation of resveratrol inclusion compound by ultrasonic method: take 30g of β-cyclodextrin to make a saturated aqueous solution, add 10g of resveratrol in ethanol solution, mix and use ultrasonic treatment, wash the precipitated precipitate with solvent, and dry to obtain the inclusion compound compound powder.

Embodiment 3

[0015] Preparation of resveratrol hydroxypropyl-β-cyclodextrin inclusion compound: take 10g of hydroxypropyl-β-cyclodextrin, dissolve it in water, add 10 g of resveratrol ethanol solution, stir and dry , and the resulting solution was dried under reduced pressure to obtain a white powdery hydroxypropyl-β-cyclodextrin inclusion compound.

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PUM

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Abstract

The invention belongs to the technical field of medicines, and relates to a resveratrol clathrate and a preparation method of resveratrol clathrate preparations, and the method mainly includes the following content: (1) selecting a suitable solvent to dissolve resveratrol; (2) using a modern preparation technology, comprising a saturated water solution method, a grinding method, a freeze drying method, an ultrasonic method, a spray drying method and the like, and a new clathrate material, comprising cyclodextrin or its derivatives such as beta cyclodextrin, hydroxypropyl beta cyclodextrin, alpha cyclodextrin, gamma cyclodextrin, glucosyl beta cyclodextrin and the like, to prepare the resveratrol clathrate; (3) using experiments to optimize a best mass ratio of resveratrol to clathrate material molecule; and (4) preparing the resveratrol clathrate into tablets, capsules, oral liquids and other preparations. By preparation of the resveratrol clathrate and the resveratrol clathrate preparations, the problem of poor water solubility and instability and low bioavailability can be solved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of a resveratrol cyclodextrin inclusion compound and a preparation thereof. Background technique [0002] Resveratrol belongs to polyphenolic compounds, also known as stilbene triphenols, mainly derived from grapes (red wine), knotweed, peanuts, mulberries and other plants. Resveratrol is a natural product with multiple biological activities: it is not only a chemopreventive agent for tumors, but also a chemopreventive agent for reducing platelet aggregation, preventing and treating atherosclerosis, and cardiovascular and cerebrovascular diseases. Scholars at home and abroad have confirmed through research that resveratrol not only has preventive and therapeutic effects on cardiovascular diseases, but also has preventive effects on cancer, especially on hormone-dependent tumors; It has preventive effects on loose skin, acne and senile dementia, ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/05A61K47/69
Inventor 王慧竹陈帅薛健飞陈哲
Owner JILIN INST OF CHEM TECH
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