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Preparation of resveratrol and preparation method for preparation

A resveratrol 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 improving solubility

Active Publication Date: 2020-05-22
南京大渊医美生物技术有限公司
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  • 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

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  • Preparation of resveratrol and preparation method for preparation
  • Preparation of resveratrol and preparation method for preparation
  • Preparation of resveratrol and preparation method for preparation

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...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a preparation making insoluble compound resveratrol solubilized under the action of synergetic supersaturation and a preparation method for the preparation. The preparation comprises the following components, in parts by weight, 10-25 parts of resveratrol, 65-83 parts of water-soluble high polymer materials, 6-21 parts of cyclodextrin, 0.6-3 parts of phospholipid and 0.4-1 parts of sodium cholate, wherein water-soluble high polymer materials serve as crystallization inhibitors, the cyclodextrin serves as an entrapment agent, and the phospholipid serves as a surface active agent.

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

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Application Information

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Patent Type & Authority Applications(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
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