1,6-diphospho-d-fructose ester arginine salt and its pharmaceutical uses

A technology of arginine salt and fructose ester, applied in 1 field, can solve the problems of injection local pain, irritation unsuitable for intramuscular injection, numbness and the like

Inactive Publication Date: 2007-08-01
GUANGDONG ZHONGKE DRUG R&D
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Sodium fructose diphosphate has the following problems in clinical use: 1) The instructions clearly point out that the use of this product will cause lip numbness, injection local pain, and occasional side effects such as dizziness, chest tightness and allergic reactions; 2) strong irritation As a result, this product is not suitable for intramuscular injection; 3) When this drug is used to treat myocardial ischemia and coronary heart disease, patients with severe infections, burns, hypertension, heart and kidney insufficiency, and other patients who need to control sodium ion intake often encounter patients, sodium fructose diphosphate large amounts of sodium ions into the body puts these patients at risk of hypernatremia
[0005] At present, there is still a lack of a solution to produce compounds with lower toxicity, less irritation, and the risk of hypernatremia on the basis of maintaining the efficacy of sodium fructose diphosphate

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1: Preparation of 1,6-diphosphate-D-fructose ester arginine salt

[0019] Fully dissolve 55.0 g of sodium fructose diphosphate in 100 ml of purified water under stirring, pass through a strong cation exchange resin at 0° C. to obtain a fructose diphosphate solution, and add 52.3 g of arginine to the solution. The mixture was freeze-dried at -40°C for 80 hours to obtain 104.3 g. Content determination and analysis: 97% of 1,6-diphospho-D-fructose ester arginine, and the obtained salt contains two crystal waters. Elemental analysis: (theoretical value: C 31.7%, H 5.9%, N 18.5%, O35.2%, P 8.6%; measured value: C 31.5%, H 5.8%, N 18.4%, O 35.1%, P 8.5% %).

Embodiment 2

[0020] Embodiment 2: Preparation of 1,6-diphosphate-D-fructose ester arginine salt

[0021] Fully dissolve 55.0 g of sodium fructose diphosphate in 100 ml of purified water under stirring, pass through a strong cation exchange resin at 0° C. to obtain a fructose diphosphate solution, and add 52.3 g of arginine to the solution. The mixture was freeze-dried at -40°C for 80 hours to obtain 103.4 g. Content determination and analysis: 96.7% of 1,6-diphospho-D-fructose ester arginine, and the obtained salt contains two crystal waters. Elemental analysis: (theoretical value: C 31.7%, H 5.9%, N18.5%, O 35.2%, P 8.6%; measured value: C 31.9%, H 6.0%, N 18.4%, O 35.1%, P8. 5%).

Embodiment 3

[0022] Embodiment 3: Preparation of 1,6-diphosphate-D-fructose ester arginine salt injection

[0023] Prescription: 1,6-Diphospho-D-Fructose Ester Arginine 200g

[0024] Sodium chloride: 8g

[0025]

[0026] 1000ml

[0027] Accurately weigh 1,6-diphosphate-D-fructose ester arginine salt according to the prescription amount, put it in a container, add an appropriate amount of water for injection, stir 8g of sodium chloride, after completely dissolving, adjust the pH to 8.5-8.8, Add water for injection to 1000ml, add 2g of activated carbon for needles, boil for 15min, decarburize by suction filtration, filter the solution through a 0.22μm microporous membrane, and fill the solution in a 100ml infusion bottle (each bottle contains 1,6-diphosphoric acid-D - fructose ester arginine salt 20g), the preparation can be sterilized under pressure at 115°C for 30min.

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PUM

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Abstract

The invention disclose the arginine salt of 1, 6- diphosphoric acid- D- fructose esters in hydrate type, and one or more than one of the four function groups is salinized by arginine. The salt precipitation with 1, 6- diphosphoric acid- D- fructose esters and arginine solves problems of strong side effect of sodium fructose diphosphate, and starting circuit, high natremia risk. It is demonstrated through pharmacological test that arginine salt can cooperate with drug and the toxcity is low.

Description

Technical field: [0001] The present invention relates to a salt of 1,6-diphosphate-D-fructose ester and an organic amine, and to a pharmaceutical composition containing their active ingredients. Background technique: [0002] Sodium fructose diphosphate is a clinical first-line drug, mainly used for adjuvant treatment of coronary heart disease, angina pectoris, acute myocardial infarction, heart failure and arrhythmia, hemorrhagic, toxic and cardiogenic shock, acute adult respiratory distress syndrome, extracorporeal circulation and other adjuvant therapy. Sodium fructose diphosphate stimulates the activity of phosphofructokinase and pyruvate kinase to produce sufficient ATP and phosphocreatine, promotes the influx of potassium ions, increases the stability of cell membranes, and prevents cells from producing oxygen free radicals, thereby preventing ischemia and hypoxia. Oxygen and reperfusion injured cells play a protective role, and can still improve the systolic and dias...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H11/04A61K31/7024A61P3/12A61P9/10
Inventor 陈文展王伟
Owner GUANGDONG ZHONGKE DRUG R&D
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