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Cycloastragenol crystal form B and preparation method thereof

A technology of cycloastragalus and crystal form, which is applied in the field of organic chemical drug preparation, can solve the problems of unstable three-membered ring structure, complicated process, complicated purification steps of the final product and the like

Pending Publication Date: 2020-07-07
LUNAN PHARMA GROUP CORPORATION
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  • Abstract
  • Description
  • Claims
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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 B and preparation method thereof
  • Cycloastragenol crystal form B and preparation method thereof
  • Cycloastragenol crystal form B and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Add 250 mg cycloastragenol crystal form A into 6 ml of a mixed solution of methanol and methyl tert-butyl ether (volume ratio 1:5), heat to reflux, and after reflux for 2 to 4 hours, filter while hot to collect the filtrate, seal with a parafilm, tie Well, stand for crystallization for 2-4 days, filter, collect the solid, and dry under reduced pressure at 50°C to obtain a crystalline solid, yield: 96.3%, HPLC purity: 99.95%.

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Abstract

The invention provides a cycloastragenol crystal form B as well as a preparation method and application thereof. The cycloastragenol crystal form B provided by the invention has higher purity and better chemical stability, and a better dissolution and release effect can be achieved when the crystal form B is prepared into a pharmaceutical preparation, and meanwhile, the preparation method of cycloastragenol is simple, convenient and easy to industrialize.

Description

technical field [0001] The invention belongs to the technical field of organic chemical drug preparation, and in particular relates to cycloastragenol crystal form B, 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): C07J53/00A61K31/58A61P39/06
CPCC07J53/004A61P39/06C07B2200/13
Inventor 张朝花翟立海郭立红胡长恺
Owner LUNAN PHARMA GROUP CORPORATION
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