Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A preparation of resveratrol and its preparation method

A resveratrol and preparation technology, applied in the field of resveratrol preparation and its preparation based on synergistic supersaturation, can solve the problems of not being clear, not higher than 10%, enhancing the stability of insoluble drug solutions, etc. Achieve the effect of improving surface charge and easy realization

Active Publication Date: 2021-10-26
南京大渊医美生物技术有限公司
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, limited to the principle of cyclodextrin inclusion, RES molecules and cyclodextrin can only theoretically exist in a molar ratio of 1:1, but in practice, because the inclusion efficiency of cyclodextrin is generally lower than 100 %, so the molar content of cyclodextrin is generally higher than that of RES
This has brought about an obvious problem: since the molecular weight of cyclodextrin is much higher than that of RES, the solid content of RES in the final RES clathrate is limited to a low level, generally not higher than 10%. That is to say, in order to promote the solubilization of RES, nearly 90% of substances without any physiological activity have to be added, which is not an efficient loading method
However, according to our research, in the existing research on the three-phase material formed by drug + solid dispersion + cyclodextrin, there is no clear effective means to enhance the solution stability of poorly soluble drugs

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A preparation of resveratrol and its preparation method
  • A preparation of resveratrol and its preparation method
  • A preparation of resveratrol and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The problem to be solved is that we hope to increase the water solubility of RES in order to improve its solubility in water and increase the killing effect on coronaviruses. Therefore, we tried the solubility after using several auxiliary materials and RES to form complexes alone, and found that several auxiliary materials were better for increasing the solubility of RES. This step is actually used to screen which material is better for solubilizing RES and maintaining solution stability.

[0038] For the comparison of single-factor solubilization techniques (percentages are mass fractions), the prescriptions are shown in Table 1.

[0039] Table 1 Comparison of single-factor solubilization technology prescriptions

[0040]

[0041]

[0042] According to the prescription, weigh each substance in proportion to obtain a mixture with a total mass of M. The mass concentration of weighing 30 times that of M is 98% ethanol, the mixture is dissolved in the ethanol, hea...

Embodiment 2

[0050] We use the two materials with better solubilization effect screened in Example 1, namely HP-β-CD or HPMCAS-M to make a binary complex, that is, to form RES-HP-β-CD or RES-HPMCAS -M, the main purpose of this step is to judge which material has a better RES "capacity" by increasing the RES content, that is, which material can hold more RES, which is mainly used to consider the preparation of high solid content RES is set. The method is: according to the prescription listed in Table 3, in the mode of A+B or A+C, each substance is weighed in proportion to obtain a mixture with a total mass of M. The mass concentration of weighing 30 times that of M is 98% ethanol, the mixture is dissolved in the ethanol, heated to 50° C. and stirred to dissolve to form a clear and transparent solution, and the organic solvent is quickly volatilized and removed by a vacuum rotary evaporator to obtain White powdery solid product. RES solid content climbing test (percentage is mass fraction)...

Embodiment 3

[0062] Through Example 2, we confirmed that HPMCAS-M has a larger RES capacity than HP-β-CD, that is, it can still maintain a clear solution after containing more RES. In Example 3, we further found that when HPMCAS-M and HP-β-CD are used in combination, the dissolution rate of RES can be further increased than that of HPMCAS-M or HP-β-CD alone, confirming the preparation of three The elemental complex (RES-HP-β-CD-HPMCAS-M) is superior to the binary complex (RES-HP-β-CD or RES-HPMCAS-M) in enhancing the dissolution rate, in other words, Has a better immediate release effect. The method is: according to the prescription listed in Table 5, each substance is weighed in proportion to obtain a mixture with a total mass of M. The mass concentration of weighing 30 times that of M is 98% ethanol, the mixture is dissolved in the ethanol, heated to 50° C. and stirred to dissolve to form a clear and transparent solution, and the organic solvent is quickly volatilized and removed by a v...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention belongs to the field of pharmaceutical preparations, and specifically relates to a preparation based on synergistic supersaturation that solubilizes the poorly soluble compound resveratrol and its preparation method. This preparation includes: resveratrol, a water-soluble polymer material as a crystallization inhibitor, cyclodextrin as a carrier, phospholipids and sodium cholate as a surfactant. The preparation includes the following components by weight: : 10 to 25 parts of resveratrol, 65 to 83 parts of water-soluble polymer materials, 6 to 21 parts of cyclodextrin, 0.6 to 3 parts of phosphorus ester, and 0.4 to 1 part of sodium cholate.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a resveratrol preparation based on synergistic supersaturation and a preparation method thereof. Background technique [0002] Resveratrol (Resveratrol, RES) is a natural polyphenolic substance with strong biological activity, mainly derived from grapes, knotweed, peanuts, mulberries and other plants. Existing findings show that RES has a variety of pharmacological effects, including anti-tumor, cardiovascular protection, blood lipid lowering, anti-bacterial and anti-inflammatory, anti-aging, anti-oxidation, anti-platelet aggregation, prevention of atherosclerosis, and regulation of lipid metabolism. Studies in recent years have also found that RES has a strong inhibitory effect on a variety of viruses. [0003] The chemical name of resveratrol (RES) is 3,4',5-trihydroxy-1,2-diphenylethylene (3,4',5-stilbene triol), and the CAS number is 501-36-0. RES is white needle ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/05A61K47/69A61K47/24A61K47/28A61K47/38A61P31/14
CPCA61K9/145A61K9/146A61K31/05A61K47/6951A61P31/14
Inventor 王台虎黄和赵万洲
Owner 南京大渊医美生物技术有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com