Methylated heparin compound as well as preparation and application thereof

A technology of methylated heparin and compounds, applied in the field of biomedicine, can solve the problems of poor medication comfort and achieve the effect of increasing the possibility and enriching the way of administration
CN112079942APending Publication Date: 2020-12-15SUZHOU RONGXI BIOTECH CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SUZHOU RONGXI BIOTECH CO LTD
Publication Date
2020-12-15

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Abstract

The invention discloses a methylated heparin compound as well as preparation and application thereof, and a preparation method of the methylated heparin compound comprises the following steps: 1, dissolving heparin, and preparing a heparin solution for reaction; 2, methylating heparin; maintaining the heparin solution for reaction at -5 to 5 DEG C, and slowly dropwise adding an alkali solution anda methylation reagent; after the reaction is finished, treating the reaction liquid to obtain a methylated heparin crude product; and 3, refining and purifying the methylated heparin crude product toobtain a methylated heparin finished product. A lipophilic group, namely methyl, is introduced into a heparin structure, so that non-sulfonated hydroxyl and carboxyl on heparin are partially converted into methoxy and carboxylic acid methyl ester, namely the heparin structure is derivatized, the derivatized heparin has lipophilicity, and the possibility that the heparin enters a blood system through gastrointestinal mucosa is improved; the methylated heparin compound can be applied to heparin oral dosage form medicines or health care products, so that the administration mode of heparin medicines is enriched.
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Description

technical field

[0001] The invention relates to the technical field of biomedicine, in particular to heparin drugs and their preparation. Background technique

[0002] At present, heparin drugs are the most widely used anticoagulant and antithrombotic drugs in clinical practice, and are included in domestic and foreign pharmacopoeias, including Chinese Pharmacopoeia (ChP 2015), European Pharmacopoeia (EP 9.0), and United States Pharmacopoeia (USP 40). Heparin is a sulfated glycosaminoglycan. Its structure is a linear chain structure formed by alternating 1→4 glycosidic bonds between L-iduronic acid or D-glucuronic acid and D-glucosamine sulfate. The structural formula is as follows:

[0003]

[0004] The molecular weight of natural heparin is 3000Da-30000Da, and the average molecular weight is about 15000Da.

[0005] Since sulfated glycosaminoglycans are highly hydrophilic and highly polar substances, the injection form of heparin is the main dosage form. However, the in...

Claims

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