Heparin bisphosphonate derivative and synthetic method and application thereof

A technology of bisphosphonates and a synthesis method, which can be used in drug combinations, bone diseases and other directions, can solve problems such as inability to mass-produce, high preparation costs, and complex processes, and achieves improved rehabilitation treatment levels, simple preparation methods, and low process requirements. Effect

Inactive Publication Date: 2015-11-25
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] However, these existing technologies have problems such as high preparation cost, complicated process, and cumbersome operation, so they cannot be mass-produced

Method used

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  • Heparin bisphosphonate derivative and synthetic method and application thereof
  • Heparin bisphosphonate derivative and synthetic method and application thereof
  • Heparin bisphosphonate derivative and synthetic method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Example 1: Preparation of heparin alendronate sodium derivatives

[0041] 1. Dissolve 1g of heparin in 20ml of ultrapure water;

[0042] 2. Add 1.2331g of 2-morpholineethanesulfonic acid (EMS), 0.7269g of N-hydroxysuccinimide (HOSU), 1.2165g of 1-(3-dimethylamino)-3-ethyl carbon Diimine hydrochloride (EDC) was dissolved in 30ml of ultrapure water;

[0043] 3. Dissolve 2.0534g of alendronate sodium in 100ml of ultrapure water;

[0044] 4. Add the solution obtained in (2) into the solution of (1), place it on a magnetic stirrer, and stir for activation for 5 hours;

[0045] 5. After 5 hours, add the solution obtained in (3) into the solution obtained in (4), and stir for 24 hours;

[0046] 6. After 24 hours, pour the solution obtained in (5) into a dialysis bag, dialyze in ultrapure water for 48 hours, and change the water every 4 hours;

[0047] 7. After 48 hours, freeze-dry the solution in the dialysis bag in (6) to obtain the desired target product.

[0048] 8. Th...

Embodiment 2

[0049] Example 2: Preparation of heparin alendronate sodium derivatives

[0050] (1) Dissolve 53.2mg heparin in 5ml ultrapure water;

[0051] (2) Dissolve 73.6 mg of EMS, 42.3 mg of HoSu, and 61.2 mg of EDC in 15 ml of ultrapure water.

[0052] (3) Dissolve 410.68mg of alendronate sodium in 5ml of ultrapure water

[0053] (4) Add the solution obtained in (2) into the solution of (1), and place it on a magnetic stirrer to stir and activate for 5 hours;

[0054](5) After 5h, the solution obtained in (3) was added to the solution obtained in (4), and the reaction was stirred for 24h;

[0055] (6) After 24 hours, pour the solution obtained in (5) into a dialysis bag, dialyze in ultrapure water for 48 hours, and change the water every 4 hours;

[0056] (7) After 48 hours, freeze-dry the solution in the dialysis bag in (6) to obtain the desired target product.

[0057] The present invention applies the product:

[0058] It is used for preventing and preventing osteolytic lesion...

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Abstract

The present invention relates to a heparin bisphosphonate derivative and a synthetic method and application thereof. The modification material for alendronate sodium is heparin; the heparin and alendronate sodium are coupled through an amide bond for drug modification of alendronate sodium. The present invention overcomes the defects of high preparation cost, complex process, complicated operation and incapability of mass production in the conventional method. The invention directly employs a chemical method for modification of alendronate sodium. The alendronate sodium improved drug is simple for preparation, low in cost, and uses readily available raw materials; besides, the improved drug can improve the permeability of alendronate sodium in the body, reduce irritation of drug on mucous membranes, increase the effective concentration of the alendronate sodium drug in targets, reduce the side effects of alendronate sodium in the body, improve the body's level of rehabilitation therapy, and improve medication safety and quality of patients.

Description

technical field [0001] The present invention relates to bisphosphonate derivatives, in particular to a heparin bisphosphonate derivative and its synthesis method and application. Background technique [0002] Osteoporosis has become a disease that seriously affects human health. According to the statistics of the World Health Organization, there are more than 200 million patients suffering from osteoporosis worldwide. Men over 50 to 60 years old and women over 40 to 50 years old are likely to suffer from varying degrees of osteoporosis. In recent years, some surveys have shown that there are 40 to 80 million people suffering from OP in my country, and the total incidence of OP among people over 60 years old is 22.6%, and it has a tendency to increase year by year. At present, the medical community has put the prevention and treatment of OP and the prevention of hypertension and hyperlipidemia in an equally important position. Osteoporosis is a group of bone diseases cause...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/10A61K31/727A61P19/08A61P19/10
Inventor 朱沛志王静成颜连启王进宇
Owner YANGZHOU UNIV
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