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A composition containing resveratrol and its preparation method

A technology of resveratrol and absolute ethanol, which is applied in the direction of medical preparations of non-active ingredients, drug combinations, active ingredients of hydroxyl compounds, etc., can solve the problems of decreased cumulative dissolution rate, decreased bioavailability, and increased hardness of drugs , to improve the apparent solubility, prevent recrystallization, and improve the stability of the formulation

Active Publication Date: 2019-06-25
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after long-term storage of resveratrol solid dispersion, hardness will increase, crystals will precipitate or crystals will coarsen, resulting in a decrease in the cumulative dissolution rate of the drug and a decrease in bioavailability

Method used

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  • A composition containing resveratrol and its preparation method
  • A composition containing resveratrol and its preparation method
  • A composition containing resveratrol and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Prepare a kind of resveratrol solid dispersion as follows:

[0045] (1) take by weight resveratrol 1g, carboxymethyl chitosan 9g, ethanol 25g;

[0046] (2) 1g of resveratrol is added to 25g of absolute ethanol and fully dissolved;

[0047] (3) 9g carboxymethyl chitosan is added to step (2) in the dissolved resveratrol dehydrated alcohol solution;

[0048] (4) Ethanol was removed by rotary evaporation of the mixture obtained in (3) at 40°C;

[0049] (5) vacuum drying removes residual ethanol;

[0050] (6) The granules obtained by vacuum drying and pulverization are classified with an 80-mesh sieve, and particles with a particle size of <180 μm are collected to obtain a resveratrol solid dispersion.

Embodiment 2

[0052] Solubility experiment:

[0053] According to the "Solubility Test Method" on page XIV of "Pharmacopoeia of the People's Republic of China" Part Two (2010 Edition) "General Cases", it is determined according to law. Grind 1 g of the resveratrol bulk drug and 10 g of the product of Example 1 of the present invention (approximately equivalent to 1 g of the bulk drug) into fine powder (through 80 mesh sieves), and place them in 25°C, 30mL, 100mL, 1000mL, 10000mL containers respectively. Shake vigorously for 30 seconds every 5 minutes in deionized water; observe the dissolution within 30 minutes. If there are no visible solute particles or droplets, it is considered completely dissolved. The results are shown in Table 1.

[0054] Table 1 Resveratrol and the solubility test result of Example 1

[0055]

[0056]According to the judgment standard of page XIV "solubility" in "Pharmacopoeia of the People's Republic of China" Part Two (2010 Edition) "General Cases". As can b...

Embodiment 3

[0058] Interaction Characterization:

[0059] The product of Example 1 of the present invention was compressed into tablets using potassium bromide, and analyzed by infrared spectroscopy. see results figure 1 . Depend on figure 1 It can be seen that the infrared spectrogram of the product of Example 1 presents the superimposed peak shape characteristics of resveratrol and carboxymethyl chitosan, and the -OH peak position of the product of Example 1 is 3260cm -1 ,-C=O peak position 1589cm -1 , the -OH peak position of resveratrol is 3330cm -1 ,-C=O peak position 1602cm -1 , the -OH peak position of carboxymethyl chitosan is 3450cm -1 ,-C=O peak position 1650cm -1 , it can be seen that the -OH peak position and -C=O peak position of the product of Example 1 are all shifted to the low wave number, and the -OH peak position of the product of Example 1 is broadened, indicating that resveratrol and carboxychitosan have been formed Interactions (formation of hydrogen bonds) o...

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Abstract

The invention relates to a composition containing resveratrol and a preparation method thereof. The composition comprises 100 parts by weight of resveratrol and 20-500 parts by weight of a pharmaceutically acceptable water-soluble amorphous carrier, wherein the amorphous carrier is selected from polyvinylpyrrolidone K29 / 32, carboxymethyl chitosan or a combination thereof The method is as follows: adding 100 parts by weight of resveratrol into absolute ethanol to dissolve; adding 20-500 parts by weight of a water-soluble amorphous carrier; removing ethanol; pulverizing and sieving; pressing into tablets or preparing into capsules. The composition of the invention can significantly improve the stability of the resveratrol solid preparation while maintaining good dissolution rate.

Description

technical field [0001] The invention belongs to the technical field of medicine and health care, and in particular relates to a composition containing resveratrol and a preparation method thereof. Background technique [0002] Resveratrol widely exists in plants in nature. Generally, it is extracted and separated from Polycum cuspidatum (Polycum.p.) and grapes, and can also be obtained by synthesis. This has been described in detail in previous literature and patents. Resveratrol has a wide range of physiological effects. It is an antioxidant that regulates blood lipids, antithrombotic, and anticancer effects. It has become a hot spot in medical and pharmaceutical research and is widely used in health foods and medicines. [0003] Resveratrol mainly contains stilbene core structure, including cis- and trans-isomers, and is usually insoluble or slightly soluble in water, with low bioavailability and insufficient stability, which affects its popularization and use . Theref...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K31/05A61P39/06A61P3/06A61P9/10A61P35/00
Inventor 马小军王冰吕国军于炜婷赵姗张建斌吕岩
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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