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Anticoagulation-resistant heparin derivative

A technology of heparin derivatives and products, applied in anti-inflammatory agents, drug combinations, digestive system, etc., can solve problems such as disappointing experimental results

Active Publication Date: 2018-08-21
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the results of safety evaluation data are very good, the results of clinical phase II and III trials are very disappointing (Korzenik, J., et al., Multicenter, randomized, double-blind, placebo-controlledtrial of deligoparin (ultra low molecular weight heparin) for active ulcerative colitis. Gastroenterology, 2003.124(4):p.A67.)

Method used

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  • Anticoagulation-resistant heparin derivative
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  • Anticoagulation-resistant heparin derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Dissolve 20g of high-quality heparin (purchased from Changshan Biochemical Pharmaceutical Co., Ltd., product name: heparin sodium) in 0.6L deionized water, and add an equal volume of 0.2M sodium periodate to 0.6L of high-quality heparin (33g / L) Solution (prepared now), react at 300 rpm, 4°C and protect from light for 22 hours. Add 80mL of ethylene glycol to neutralize excess sodium periodate, then add 28g of sodium borohydride and react at 4°C for 16 hours. The pH was adjusted to 7.0 with HCl. Filter through a 0.22 μm filter membrane to collect filtered samples. Then use a dialysis bag to desalinate or use a Millipore ultrafiltration device with a 1K filter membrane for ultrafiltration concentration and desalination until the filtrate is passed through 0.1M AgNO 3 Desalination is considered complete when no color change is detected. The samples were frozen at -80°C and then placed in a lyophilizer to freeze-dry, and then crushed into powder with a mortar or a small p...

Embodiment 2

[0108] Dissolve the anticoagulant heparin prepared in Example 1 in the reaction buffer, add heparinase I prepared according to the method of ZL200410038098.6 to the solution every 0.5 to 1 h, add 20 IU heparinase I each time, and use the optical path difference Use a 1cm quartz cuvette and an ultraviolet spectrophotometer to monitor the light absorption A231 of the solution at 231nm (use a pH7.4 buffer to calibrate and zero the instrument. For the accuracy of the test results, when the ultraviolet spectrophotometer reading A231 is greater than 0.6 , dilute the solution by a certain number of times, so that the reading is measured at 0.2-0.6). When it is detected that A231 reaches 46, the reaction is terminated, and the enzyme activity of the added total heparanase I reaches about 220-250IU. The final method is to inactivate the enzyme in the reaction solution in a boiling water bath at 100°C for 5-10 minutes, then take out the reaction system and cool it to room temperature, a...

Embodiment 3

[0110] Dissolve the anticoagulant heparin prepared in Example 1 in the reaction buffer, add heparinase I prepared according to the method of ZL200410038098.6 to the solution every 0.5 to 1 h, add 20 IU heparinase I each time, and use the optical path difference Use a 1cm quartz cuvette and an ultraviolet spectrophotometer to monitor the light absorption A231 of the solution at 231nm (use a pH7.4 buffer to calibrate and zero the instrument. For the accuracy of the test results, when the ultraviolet spectrophotometer reading A231 is greater than 0.6 , dilute the solution by a certain number of times, so that the reading is measured at 0.2-0.6). When it is detected that A231 reaches 106, the reaction is terminated, and the enzyme activity of the added total heparanase I reaches about 340-380 IU at this time. The final method is to inactivate the enzyme in the reaction solution in a boiling water bath at 100°C for 5-10 minutes, then take out the reaction system and cool it to room...

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Abstract

The invention relates to an anticoagulation-resistant heparin derivative. The anti-Xa factor of the anticoagulation-resistant heparin derivative is lower than or equals to 70IU / mg, preferably the anti-Xa factor is lower than or equals to 60IU / mg, preferably is lower than or equals to 50IU / mg, preferably is lower than or equals to 40IU / mg, preferably is lower than or equals to 30IU / mg, preferably is lower than or equals to 20IU / mg, preferably is lower than or equals to 10IU / mg, the anti-IIa factor is lower than or equals to 175IU / mg, preferably is lower than or equals to 170IU / mg, preferably islower than or equals to 160IU / mg, preferably is lower than or equals to 150IU / mg, preferably is lower than or equals to 140IU / mg, preferably is lower than or equals to 130IU / mg, preferably is lower than or equals to 120IU / mg, preferably is lower than or equals to 110IU / mg, preferably is lower than or equals to 100IU / mg, preferably is lower than or equals to 90IU / mg, preferably is lower than or equals to 80IU / mg, preferably is lower than or equals to 70IU / mg, preferably is lower than or equals to 60IU / mg, preferably is lower than or equals to 50IU / mg, preferably is lower than or equals to 40IU / mg, preferably is lower than or equals to 30IU / mg, preferably is lower than or equals to 20IU / mg, and preferably is lower than or equals to 10IU / mg.

Description

technical field [0001] The present invention relates to the preparation of deanticoagulated heparin derivatives and their use for preventing and / or treating inflammatory bowel disease. Background technique [0002] Inflammatory bowel disease (Inflammatory Bowel Disease, IBD) is a group of very widespread and incurable chronic inflammatory diseases, including ulcerative colitis (Ulcerative Colitis, UC) and Crohn's disease (Crohn's disease, CD). According to reports, the highest prevalence of IBD in western countries reaches 0.8%, and the incidence and prevalence of IBD in Asia show a continuous and rapid growth trend, becoming a disease of global concern. Prevalence increases of more than 40% are projected in many countries over the next decade. The demand for IBD-related drugs will increase significantly (Bernstein CN, et al. World Gastroenterology Organization Global Guidelines Inflammatory Bowel Disease: Update August 2015. Journal of Clinical Gastroenterology, 2016, 50(1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/10C12P19/26A61K31/727A61P1/00A61P29/00A61P19/02A61P17/00A61P27/02A61P1/16
CPCA61K31/727C12P19/26C08B37/0075A61P1/00A61P1/16A61P17/00A61P19/02A61P27/02A61P29/00
Inventor 邢新会王怡季洋张翀常智杰
Owner TSINGHUA UNIV
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