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Treatment of postpartum haemorrhage with chemically modified heparin or heparan sulphate and a uterotonic agent

A technology of heparan sulfate and chemical modification, which can be used in blood diseases, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., and can solve problems such as no prompts

Inactive Publication Date: 2015-01-14
DILAFOR
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the literature also does not suggest that low molecular weight heparins can be used for direct intervention when complications arise requiring direct therapeutic efficacy

Method used

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  • Treatment of postpartum haemorrhage with chemically modified heparin or heparan sulphate and a uterotonic agent
  • Treatment of postpartum haemorrhage with chemically modified heparin or heparan sulphate and a uterotonic agent
  • Treatment of postpartum haemorrhage with chemically modified heparin or heparan sulphate and a uterotonic agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Oxidation of nonsulfated glucuronic and iduronic acids (residues), AT-binding pentasaccharides and anticoagulation active deletion

[0070] About 3000 grams of heparin was dissolved in purified water to obtain a 10-20% w / v solution. The pH of the solution was adjusted to 4.5-5.5. Then, sodium metaperiodate (NaIO 4 ) into the production solution; the amount of periodate is 15-25% of the heparin weight. The pH was again adjusted to 4.5-5.5. Protect from light for reaction. The process solution was allowed to react for 18-24 hours under continuous stirring, maintaining a temperature of 13-17°C, with the temperature dropped to 5°C during the last two hours.

[0071] Termination of oxidation reactions and removal of iodine-containing compounds

[0072] Ethanol (95-99.5%) was added to the reaction mixture over 0.5-1 hour at a temperature of 5-25°C with gentle stirring. The volume of ethanol added is in the range of 1-2 volumes of ethanol per volume of process solu...

Embodiment 2

[0080] Oxidation of glucuronic acid and iduronic acid (residues), deletion of anticoagulant activity

[0081] About 3000 grams of heparin was dissolved in purified water to obtain a 10-20% w / v solution. The pH of the solution was adjusted to 4.5-5.5. Then, sodium metaperiodate (NaIO 4 ) into the production solution; the amount of periodate is 15-25% of the heparin weight. The pH was again adjusted to 4.5-5.5. Protect from light for reaction. The process solution was allowed to react for 22-26 hours under continuous stirring, maintaining a temperature of 13-17°C, with the temperature dropped to 5°C during the last two hours. Measure and record the pH at the end of the reaction period.

[0082] Termination of oxidation reactions and removal of iodine-containing compounds

[0083] Ethanol (95-99.5%) was added to the reaction mixture over 0.5-1 hour at a temperature of 5-25°C with gentle stirring. The volume of ethanol added is in the range of 1-2 volumes of ethanol per...

Embodiment 3

[0090] Oxidation of glucuronic acid and iduronic acid (residues), deletion of anticoagulant activity

[0091] About 3000 grams of heparin was dissolved in purified water to obtain a 10-20% w / v solution. The pH of the solution was adjusted to 4.5-5.5. Then, sodium metaperiodate (NaIO 4 ) into the production solution; the amount of periodate is 15-25% of the heparin weight. The pH was again adjusted to 4.5-5.5. Protect from light for reaction. The process solution was allowed to react for 18-24 hours under continuous stirring, maintaining a temperature of 13-17°C, with the temperature dropped to 5°C during the last two hours.

[0092] Depolymerization of polysaccharide chains by the alkaline β-elimination process

[0093] While maintaining a temperature of 5-25°C, 4M NaOH solution was added slowly until a pH of 10.5-12 was obtained. Initiate and run the reaction for 15-95 minutes. At this point, the pH of the solution was recorded and 4M HCl was added slowly until a pH ...

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Abstract

The present invention refers to the use of certain sulfated glycosaminoglycans for treatment or prevention of postpartum haemorrhage. The sulfated glycosaminoglycans have a reduced anticoagulant activity and are administered in combination with at least one uterotonic agent capable of promoting myometrial contractions of the uterus and thereby compress the vessels and cease the bleeding.

Description

technical field [0001] The present invention relates to the use of certain sulfated glycosaminoglycans for the prevention and treatment of postpartum hemorrhage (PPH). Background technique [0002] Postpartum hemorrhage (PPH) is a major factor in maternal mortality and can cause several serious complications related to rapid blood loss. There are various definitions of PPH, but it is usually associated with blood loss in excess of 500-1000ml. There are several potential causes of major bleeding following PPH and for onset within 24 hours of delivery, the most common including uterine atony, retained placenta, coagulation disorders, and uterine prolapse, see CW Su; Prime Care Clin Office Part, Vol. 39, 2192, pp 167-187. The most common clinical cause is uterine atony, which results in insufficient contraction of myometrial fibers and inadequate occlusion of the spiral arteries leading to uncontrolled bleeding. The article cited by CW Su lists several risk factors for uteri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/727A61K38/11A61P15/04A61K38/095
CPCA61K31/727A61K31/48A61K31/5575A61K2300/00A61P15/04A61P7/04A61K38/095A61K45/06
Inventor G·埃克曼-奥德贝格A·马尔姆斯特伦
Owner DILAFOR
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