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

Hesperetin and carbamazepine eutectic, and preparation method, composition and application thereof

A technology of hesperetin and co-crystals, applied in the field of co-crystals formed by hesperetin and carbamazepine, which can solve the problem of no research reports, similarities or conflicts on the formation of co-crystals between hesperetin and carbamazepine and other issues, to achieve the advantages of good safety and drug advantages, significant solubility and dissolution rate advantages

Pending Publication Date: 2021-08-06
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
View PDF0 Cites 1 Cited by
  • 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 between hesperetin and carbamazepine, 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

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
  • Hesperetin and carbamazepine eutectic, and preparation method, composition and application thereof
  • Hesperetin and carbamazepine eutectic, and preparation method, composition and application thereof
  • Hesperetin and carbamazepine eutectic, and preparation method, composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Hesperetin and carbamazepine co-crystal preparation method 1

[0060] Take an appropriate amount of hesperetin and carbamazepine, 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 mix the obtained mixture The suspension solvent was evaporated to dryness, filtered to dry naturally or filtered to vacuum-dried, and the conditions and parameters were shown in Table 3. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and figure 1 Consistent, indicating that the obtained sample is a co-crystal of hesperetin and carbamazepine.

[0061] Table 3 hesperetin and carbamazepine co-crystal preparation method 1 specific example

[0062]

Embodiment 2

[0064] Dissolution and release characteristics of hesperetin and carbamazepine co-crystal in vitro

[0065] The solubility characteristics of hesperetin and carbamazepine co-crystal and hesperetin API in pure water, pH value 1.2, pH value 4.5, pH value 6.8 were investigated. The experiment was carried out with reference to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations". Dissolution percentage adopts high performance liquid phase method, and external standard method calculates its dissolution percentage content. Take time as the abscissa, and the dissolution percentage as the ordinate to draw the dissolution curve respectively ( Image 6 ). The data are shown in Table 4.

[0066] 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; Injectio...

Embodiment 3

[0071] Stability advantage of hesperetin and carbamazepine co-crystal

[0072] High temperature test: put the samples of hesperetin and carbamazepine eutectic into an open clean watch glass, place them 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 carried out on the samples obtained at the above sampling points, and the results showed that the hesperetin and carbamazepine eutectic was stable under the high temperature influence factor test.

[0073] High humidity test: put the hesperetin and carbamazepine eutectic sample in an open clean watch glass, place it at 25°C for 10 days at a relative humidity of 90%±5%, and test it on the 0th day, the 5th day and Samples were taken on day 10. Powder X-ray diffraction analysis was performed on the samples obtained at the above sampling points, and the results showed that the cocrystal of hesperetin and carbamazepine was stable under high humidity conditions. ...

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

No PUM Login to View More

Abstract

The invention discloses a hesperetin and carbamazepine eutectic, and a preparation method, a composition and application thereof, and belongs to the technical field of medicines. Specifically, the invention discloses the eutectic formed by hesperetin and carbamazepine, with the molecular formula of (C16H14O6).(C15H12N2O), the preparation method of the hesperetin and carbamazepine eutectic, and the application of the hesperetin and carbamazepine eutectic as an effective pharmaceutical ingredient in the preparation of drugs for resisting tumors, oxidation, inflammation, epilepsy, trigeminal neuralgia and manic depression and preventing atherosclerosis, arrhythmia diseases and complications.

Description

technical field [0001] The invention relates to a cocrystal formed by hesperetin and carbamazepine; a preparation method for the cocrystal of hesperetin and carbamazepine; the cocrystal of hesperetin and carbamazepine is used as an active ingredient of a medicine, and is used in the preparation of anti-inflammatory drugs. Tumor, anti-oxidation, anti-inflammation, epilepsy, trigeminal neuralgia, manic depression, prevention of atherosclerosis, arrhythmia diseases 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] Carbamazepine (English name: Carbamazepine) is a common fat-soluble calcium channel blocker and is the drug of choice for the clinical treatment of epilepsy. It is often used to treat ...

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
IPC IPC(8): C07D311/32C07D223/22A61K31/352A61K31/55A61P35/00A61P39/06A61P29/00A61P25/08A61P25/04A61P25/24A61P9/10A61P9/06
CPCC07D311/32C07D223/22A61P35/00A61P39/06A61P29/00A61P25/08A61P25/04A61P25/24A61P9/10A61P9/06C07B2200/13
Inventor 吕扬杜冠华谢逸菲杨世颖张丽
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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