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Chondroitin sulfate derivative of nano-methotrexate and preparation method and application of chondroitin sulfate derivative

A technology of chondroitin sulfate and methotrexate, which is applied in the field of methotrexate derivatives, can solve the problems of inability to mass-produce, complicated process production, and complicated operation requirements, and achieves improvement of rehabilitation treatment level, low process requirements, The effect of improving safety quality

Active Publication Date: 2016-08-17
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, these existing technologies have problems such as high cost of raw materials, complex manufacturing process, and cumbersome operation requirements, so they cannot be mass-produced

Method used

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  • Chondroitin sulfate derivative of nano-methotrexate and preparation method and application of chondroitin sulfate derivative
  • Chondroitin sulfate derivative of nano-methotrexate and preparation method and application of chondroitin sulfate derivative
  • Chondroitin sulfate derivative of nano-methotrexate and preparation method and application of chondroitin sulfate derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1. Dissolve 1.0g chondroitin sulfate in 20mL ultrapure water.

[0039] Dissolve 0.769 g of 4-(4,6-dimethoxytriazin-2-yl)-4-methylmorpholine hydrochloride in the solution obtained in step (1) and activate for 30 minutes.

[0040] 2. Dissolve 1.2g of methotrexate in 10mL of ultrapure water, adjust the pH to be acidic until completely dissolved.

[0041] 3. Add the solution obtained in step (3) into the activated solution in step (2), and place it on a magnetic stirrer to stir for 5 hours.

[0042] 4. After 5 hours, pour the reaction solution into a dialysis bag, dialyze in ultrapure water for 48 hours, and change the water every 4 hours.

[0043] 5. After 48 hours, freeze-dry the solution in the dialysis bag obtained in step (5) to obtain the desired target product.

[0044] 6. Analysis of the target product, its structural formula is as follows:

[0045]

[0046] In the above formula, m is an integer of 20-300; n is an integer of 22-150.

Embodiment 2

[0048] 1. Dissolve 53.2mg of chondroitin sulfate in 5mL of ultrapure water.

[0049] 2. Dissolve 40.91 mg of 4-(4,6-dimethoxytriazin-2-yl)-4-methylmorpholine hydrochloride in the solution obtained in step (1), and activate it for 30 minutes.

[0050] 3. Dissolve 63.84mg of methotrexate in 5mL of ultrapure water, adjust the pH to acidic until completely dissolved.

[0051] 4. Add the solution obtained in step (3) into the activated solution in step (2), and place it on a magnetic stirrer to stir for 6 hours.

[0052] 5. After 6 hours, pour the reaction solution into a dialysis bag, dialyze in ultrapure water for 48 hours, and change the water every 4 hours.

[0053] 6. After 48 hours, freeze-dry the solution in the dialysis bag obtained in step (5) to obtain the desired target product.

[0054] 7. Analyze the target product, and analyze its structural formula as follows:

[0055]

[0056] In the above formula, m is an integer of 20-300; n is an integer of 22-150.

[0057...

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Abstract

The invention discloses a chondroitin sulfate derivative of nano-methotrexate and a preparation method and application of the chondroitin sulfate derivative and relates to the technical field of synthesis methods and application of methotrexate derivatives. According to the method, 4-(4,6-dimethoxytriazine-2-yl)-4-methylmorpholine hydrochloride is dissolved in a chondroitin sulfate water solution to obtain an activated solution, an acidic methotrexate water solution and the activated solution are mixed to obtain a reactivated mixed solution, and lastly the reactivated mixed solution is put in ultrapure water for dialysis and freeze-drying to obtain the chondroitin sulfate derivative of nano-methotrexate. The preparation method is simple, cost is low, the product can be used for preparing an injection for preventing, treating and stopping osteolytic bone lesions caused by malignant tumors, treating hypercalcemia and reducing bone resorption.

Description

technical field [0001] The invention relates to methotrexate derivatives, in particular to a chondroitin sulfate derivative of methotrexate and its synthesis method and application. Background technique [0002] Malignant tumors have become a class of diseases that seriously endanger human physical and mental health, and have brought a heavy economic burden to society. The incidence rate in my country has increased by 69% in the past 20 years, with 2.2 million new cancer cases every year, and one out of every five deaths is due to cancer. With the problems of diet, lifestyle, working style, population aging and other issues brought about by the improvement of my country's material living standards, the incidence of cancer has increased year by year. Researching new anticancer drugs and reducing the toxicity of existing anticancer drugs is a hot spot in current medical research. [0003] The replication and repair of DNA and RNA require the use of tetrahydrofolate as a subs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/08A61K47/48A61K9/14A61K31/519A61P35/00A61P19/08A61P3/14
CPCA61K31/519C08B37/0069
Inventor 朱沛志王进宇刘冠雄张文静
Owner YANGZHOU UNIV
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