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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
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  • 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

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  • 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%.

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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

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Application Information

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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
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