Cycloastragenol crystal form D and preparation method thereof

Abstract

The invention belongs to the technical field of organic chemical drug preparation, and provides a cycloastragenol crystal form D and a preparation method and application thereof. The cycloastragenol crystal form D provided by the invention has higher purity and better chemical stability, the crystal form D has better dissolution and release behaviors when being made into a pharmaceutical preparation, and meanwhile, the preparation method of the 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 D and its preparation method and application. 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 neu...

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

Images