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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

Pending Publication Date: 2020-12-15
SUZHOU RONGXI BIOTECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Since sulfated glycosaminoglycans are highly hydrophilic and highly polar substances, the injection form of heparin is the main dosage form. However, the injection form has defects such as potential infection risk of multiple injections and poor medication comfort. Oral medication can avoid the above two disadvantages

Method used

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  • Methylated heparin compound as well as preparation and application thereof
  • Methylated heparin compound as well as preparation and application thereof
  • Methylated heparin compound as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 1. Dissolve the heparin and prepare the heparin solution for the reaction. Specific steps are as follows:

[0027] Dissolution of heparin substrate: choose a 250mL three-neck round-bottom flask equipped with a thermometer and a nitrogen balloon, place the three-neck round-bottom flask in an ice-salt bath, add 1.5g heparin and 135mL purified water into the reaction flask, and start stirring to dissolve. After the heparin solution was completely dissolved, 15 mL of dichloromethane was added and the stirring was continued to prepare a heparin solution for reaction. The internal temperature of the heparin solution for reaction was -0.5°C.

[0028] 2. Heparin methylation:

[0029] Preparation of 30% sodium hydroxide aqueous solution: put 30mL of purified water in a 150mL plastic beaker, place the plastic beaker in an ice-salt bath, cool the purified water to ≤5°C, and slowly add 12.8g of sodium hydroxide solid Stir in purified water until the sodium hydroxide is completely...

Embodiment 2

[0039] 1. Dissolve the heparin and prepare the heparin solution for the reaction. Specific steps are as follows:

[0040] Dissolution of heparin substrate: prepare a 1000mL round-bottomed flask, configure one thermometer, one nitrogen balloon, and two 100mL constant-pressure dropping funnels, place the round-bottomed flask in an ice-salt bath, and mix 4.0g heparin with 360mL purified Add water into the reaction bottle, start stirring and dissolving, after the heparin solution is completely dissolved, add 40mL of chloroform, and continue stirring to prepare a heparin solution for reaction, the inner temperature of the heparin solution for reaction is -0.1°C.

[0041] 2. Heparin methylation:

[0042] Preparation of 30% sodium hydroxide aqueous solution by mass fraction: Put 100mL of purified water in a 500mL plastic beaker, place the plastic beaker in an ice-salt bath, cool down the purified water, and after the temperature stabilizes at 0.5-2.5°C, add 42.9g of hydrogen Slowly...

Embodiment 3

[0048] 1. Dissolve the heparin and prepare the heparin solution for the reaction. Specific steps are as follows:

[0049] Dissolution of heparin substrate: prepare a 10L round bottom flask, respectively configure one thermometer, one nitrogen balloon, one 800mL constant pressure dropping funnel, one 500mL constant pressure dropping funnel, place the round bottom flask in an ice-salt bath, Add 50.0g of heparin and 4500mL of purified water into the reaction bottle, and start stirring to dissolve. After the heparin solution is completely dissolved, add 500mL of chloroform and continue stirring to prepare a heparin solution for reaction. The internal temperature of the heparin solution for reaction is - 1.0°C.

[0050] 2. Heparin methylation:

[0051] Preparation of 30% sodium hydroxide solution by mass fraction: Put 1000mL purified water in a 5L plastic beaker, place the plastic beaker in an ice-salt bath, cool down the purified water to 2.0-3.5°C, and slowly dissolve 429g of s...

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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.

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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Application Information

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IPC IPC(8): C08B37/10A61K31/727A61P7/02A23L33/00
CPCC08B37/0075A61K31/727A61P7/02A23L33/00A23V2002/00A23V2200/30
Inventor 陆晓华金永生周巧云靳彩娟姚亦明
Owner SUZHOU RONGXI BIOTECH CO LTD
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