Cycloastragenol crystal form C and preparation method thereof

A technology of cycloastragaliol and crystal form is applied in the field of organic chemical drug preparation, and can solve the problems of complicated purification steps, complicated process, multiple by-products and the like of the final product

Pending Publication Date: 2020-07-07
LUNAN PHARMA GROUP CORPORATION
View PDF6 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, cycloastragenol is usually prepared by chemically hydrolyzing astragaloside IV. However, the three-membered ring structure on astragaloside IV is extremely unstable, and many by-products are easily formed.
Chinese patent CN104817610A uses sulfuric acid to hydrolyze astragaloside IV to prepare cycloastragenol, but the reaction requires a high-temperature and high-pressure reactor, and the purification steps of the final product are complicated; Chinese patent CN103880910A reports the preparation of cycloastragenol by a redox method, But its process is relatively complicated; in addition, patent CN105734109A and patent CN105566434A both use a variety of hydrolytic enzymes to hydrolyze astragaloside IV to prepare cycloastragenol
However, the existing literature has not yet reported the research on the related crystal forms of cycloastragenol

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
  • Cycloastragenol crystal form C and preparation method thereof
  • Cycloastragenol crystal form C and preparation method thereof
  • Cycloastragenol crystal form C and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Add 250mg of cycloastragenol crystal form A to 33ml of acetonitrile, heat to 40°C, beat at a speed of 400r / min for 2-4 hours, cool down to room temperature naturally after beating, filter, collect solids, and dry under reduced pressure at 50°C to obtain crystals like solid, yield: 98.1%, HPLC purity: 99.94%.

Embodiment 2

[0036] Add 250mg of cycloastragenol crystal form A to 33ml of acetonitrile, heat to 30°C, beat at a speed of 500r / min for 2-4 hours, cool down to room temperature naturally after beating, filter, collect solids, and dry under reduced pressure at 50°C to obtain crystals like solid, yield: 96.9%, HPLC purity: 99.92%.

Embodiment 3

[0038] Add 250mg of cycloastragenol crystal form A to 33ml of acetonitrile, heat to 60°C, beat at a speed of 200r / min for 2-4 hours, cool down to room temperature naturally after beating, filter, collect solids, and dry under reduced pressure at 50°C to obtain crystals like solid, yield: 95.1%, HPLC purity: 99.92%.

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 belongs to the technical field of organic chemical drug preparation, and provides a cycloastragenol crystal form C as well as a preparation method and application thereof. The cycloastragenol crystal form C provided by the invention has higher purity and better chemical stability, the crystal form C has better dissolution and release effects when being prepared into a pharmaceuticalpreparation, and meanwhile, the preparation method of cycloastragenol is simple, convenient, easy to industrialize and high in production adaptability.

Description

technical field [0001] The invention belongs to the technical field of organic chemical drug preparation, and in particular relates to cycloastragenol crystal form C, a preparation method and application thereof. Background technique [0002] Astragaloside IV (astragaloside IV) is a representative saponin component of the traditional Chinese medicine Astragalus membranaceus, and cycloastragenol (CAG) is a saponin of astragaloside IV. Cycloastragenol is the main hydrolysis metabolite of astragaloside in the intestinal tract and the component absorbed into the blood. It has a relatively small molecular weight and strong lipophilicity, which is conducive to biofilm penetration and gastrointestinal absorption to achieve better bioavailability. A large number of modern medical studies have proved that astragaloside IV can reduce the damage of ischemia-reperfusion brain tissue by enhancing the body's ability to scavenge oxygen free radicals, inhibiting peroxidation, and reducing ...

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 Applications(China)
IPC IPC(8): C07J53/00A61K31/58A61P39/06A61P9/10
CPCC07J53/004A61P39/06A61P9/10C07B2200/13
Inventor 翟立海张朝花余军厚马庆文
Owner LUNAN PHARMA GROUP CORPORATION
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap