Cycloastragenol crystal form D and preparation method thereof
A technology of cycloastragenol and crystal form, which is applied in the field of organic chemical drug preparation, and can solve problems such as complex process, unstable three-membered ring structure, and multiple by-products
Pending Publication Date: 2020-07-07
LUNAN PHARMA GROUP CORPORATION
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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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Embodiment 1
[0037] Add 250mg of cycloastragenol into 1.ml of methanol and 5ml of acetonitrile mixed solvent to prepare a 41.67mg / ml solution of cycloastragenol in methanol and acetonitrile, heat to 50°C and stir for 2-4 hours to completely dissolve cycloastragenol. Heat filtration, seal with a parafilm, put in an explosion-proof refrigerator for crystallization for 2 to 4 days, filter, collect the solid, and dry under reduced pressure at 50°C. Yield: 98.1%, HPLC purity: 99.95%.
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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...
Claims
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Patent Type & Authority Applications(China)
IPC IPC(8): C07J53/00A61K31/58A61P39/06
CPCC07J53/004A61P39/06C07B2200/13
Inventor 刘忠方克忠翟立海
Owner LUNAN PHARMA GROUP CORPORATION
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