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Hesperetin and betaine eutectic substance B, and preparation method, composition and application thereof

A technology of betaine and hesperetin, which is applied in the field of medicine, can solve the problems of no similar or conflicting research content, no co-crystal formation of hesperetin-betaine, etc., and achieve significant solubility and dissolution rate advantages. The effect of good safety drug advantage

Pending Publication Date: 2021-08-06
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In summary, so far, there has been no research report on the formation of co-crystals of hesperetin-betaine, and there is no similar or conflicting research content with the present invention in terms of material form, combination ratio, preparation method and use.

Method used

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  • Hesperetin and betaine eutectic substance B, and preparation method, composition and application thereof
  • Hesperetin and betaine eutectic substance B, and preparation method, composition and application thereof
  • Hesperetin and betaine eutectic substance B, and preparation method, composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Hesperetin and Betaine Cocrystal B Preparation Method 1

[0061] Take an appropriate amount of hesperetin and betaine, the molar ratio of the two is 1:1, add the sample into a suitable container by solvent suspension method at room temperature, add an appropriate amount of organic solvent, stir for an appropriate time at room temperature, and dissolve the obtained suspension Evaporation and drying of liquid solvent, natural drying by filtration or vacuum drying by filtration, see Table 3 for the condition parameters. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and figure 1 Consistent, indicating that the obtained sample is cocrystal B of hesperetin and betaine.

[0062] Table 3 hesperetin and betaine cocrystal B preparation method 1 specific example

[0063]

Embodiment 2

[0065] Dissolution and release characteristics of hesperetin-betaine in vitro

[0066] The solubility characteristics of hesperetin-betaine cocrystal B and hesperetin API in aqueous systems were investigated. The experiment was carried out with reference to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations", and the percentage of dissolution was calculated by the high performance liquid phase method and the external standard method. Take time as the abscissa, and the dissolution percentage as the ordinate to draw the dissolution curve respectively ( Figure 6 ). The data are shown in Table 4.

[0067] Detection conditions: detection system: Aligent 1200, chromatographic column: Agilent Eclipse XDB-C18 (4.6 × 150mm, 5μm); mobile phase: methanol-water (70:30, v / v); flow rate: 1mL min -1 ; Column temperature: 30°C; Detection wavelength: Hesperetin: 280nm; Injection volume: 10 μl.

[0068] Table 4 Dissolution Profile Data

[0069]

[0070] ...

Embodiment 3

[0072] Stability advantage of hesperetin and betaine cocrystal B

[0073] High temperature test: put the sample of hesperetin and betaine eutectic B into an open clean watch glass, place it at 60°C for 10 days, and take samples on the 0th day, the 5th day and the 10th day. Powder X-ray diffraction analysis was performed on the samples obtained at the above sampling points, and the results showed that the cocrystal B of hesperetin and betaine was stable under the test of high temperature influencing factors.

[0074] Illumination test: Put the hesperetin-betaine eutectic B sample in an open clean watch glass, put it in a light box equipped with a fluorescent lamp, and place it under the condition of 4500lx±500lx for 10 days, and then put it on the 0th day, the 1st day Samples were taken on days 5 and 10. Powder X-ray diffraction analysis was performed on the samples obtained at the above sampling points, and the results showed that the cocrystal B of hesperetin and betaine was...

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Abstract

The invention discloses a hesperetin and betaine eutectic B, and a preparation method, a composition and application thereof, and belongs to the technical field of medicines. Specifically, the invention discloses the eutectic B formed by hesperetin and betaine, and the molecular formula of the eutectic is (C16H14O6).(C5H11NO2). The invention also discloses the preparation method of a hesperetin and betaine eutectic B, and the application of the hesperetin and betaine eutectic B as an active ingredient of a medicine in the preparation of medicines for resisting oxidation, resisting inflammation, treating cardiovascular and cerebrovascular diseases, treating epilepsy, treating liver and kidney injury, resisting tumors, treating nerve diseases and treating Alzheimer's disease and complications.

Description

technical field [0001] The invention relates to a cocrystal B formed by hesperetin and betaine; a preparation method for the cocrystal B of hesperetin and betaine; the cocrystal B of hesperetin and betaine is used as an active ingredient of a medicine, and is used in the preparation of anti-inflammatory drugs. Oxidation, anti-inflammation, cardiovascular and cerebrovascular diseases, epilepsy, liver and kidney damage, anti-tumor, neurological diseases and the application of drugs for the treatment of Alzheimer's disease and complications; it belongs to the field of medical technology. Background technique [0002] Hesperetin (English name: Hesperetin) is a dihydroflavonoid compound widely present in citrus fruits. It is a hydrolyzed product of hesperidin. Its structural formula is shown in a. , the role of preventing atherosclerosis [1-3] . [0003] Betaine (English name: Betaine) is a quaternary ammonium water-soluble alkaloid extracted from Lycium barbarum. It has a vari...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/32C07C229/12C07C227/42A61P29/00A61P9/00A61P25/08A61P1/16A61P13/12A61P35/00A61P25/00A61P25/28A61P39/06A61K31/353A61K31/205
CPCC07D311/32C07C229/12C07C227/42A61P29/00A61P9/00A61P25/08A61P1/16A61P13/12A61P35/00A61P25/00A61P25/28A61P39/06A61K31/353A61K31/205C07B2200/13A61K2300/00
Inventor 吕扬杜冠华谢逸菲杨世颖邢逞
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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