WO2008119146A2 - Combi-preparation of phosphoethanolamine and omega-3-fatty acid for treating bronchial asthma and copd - Google Patents

Combi-preparation of phosphoethanolamine and omega-3-fatty acid for treating bronchial asthma and copd Download PDF

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Publication number
WO2008119146A2
WO2008119146A2 PCT/BR2008/000093 BR2008000093W WO2008119146A2 WO 2008119146 A2 WO2008119146 A2 WO 2008119146A2 BR 2008000093 W BR2008000093 W BR 2008000093W WO 2008119146 A2 WO2008119146 A2 WO 2008119146A2
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day
omega
phosphoethanolamine
bronchial asthma
specifically
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PCT/BR2008/000093
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French (fr)
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WO2008119146A8 (en
WO2008119146A3 (en
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Dair, Bicudo Piai
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Priority to PCT/BR2008/000093 priority Critical patent/WO2008119146A2/en
Publication of WO2008119146A2 publication Critical patent/WO2008119146A2/en
Publication of WO2008119146A3 publication Critical patent/WO2008119146A3/en
Publication of WO2008119146A8 publication Critical patent/WO2008119146A8/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/20Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/202Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/683Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics

Definitions

  • Invention describes the Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive Pulmonary Disease (COPD), characterized by the composition of the combination of Phosphoethanolamine and Omega-3 in pre-established proportions, in the ratio of 400 to 1200 mg/day of Phosphoethanolamine; 500 to 3200 mg/day of COPD
  • Eicosapentaenoic acid "EPA” and 350 to 2000 mg/day of Docosahexaenoic acid “DHA”, emphasizing that the combination of these components should be consumed by time by the patient in capsule or liquid form.
  • Phosphate, Ca-EAP is a phosphoester existing in all organisms, and it is made up of Ethanolamine phosphorylation and synthesizes one of the Phospholipids, phosphatidylethanolamine.
  • a second component is made up of Omega-3, which is made up of an unsaturated greasy acid, which has the first 3 double carbon bonds after the methyl terminal.
  • 3 may be of three types, Linolenic acid, eicosapentaenoic acid, "EPA”, and Docosahexaenoic acid “DHA” and, it is incorporated in the body, most specifically in Phospholipids of the cell membrane, where it has structure and metabolic functions, acting as a substrate for the formation of various Cytokines through the metabolism of Eicosanoids.
  • Linolenic acid eicosapentaenoic acid
  • DHA Docosahexaenoic acid
  • Eicosanoids are molecules derived from 20-carbon greasy acids (EPA and Araquidonic acid), with the ability to signal cells, performing an important role in various activities such as inflammatory and immunological response modulation, platelet aggregation, cell growth and differentiation.
  • Phospholipids of the cell membrane by Phospholipase A2 and under the action of Cyclooxygenase ( COX ) produce Prostaglandins and Thromboxanes, and produce Leukotrienes under the action of Lipoxygenase.
  • COX Cyclooxygenase
  • the relative amount of polyunsaturated greasy acids in the cell membrane is the primary factor to regulate the Eicosanoid will be produced, and the hydrolytic release of greasy acid from the cell membrane occurs both with the araquidonic acid (a type of omega-6) and Omega-3.
  • araquidonic acid omega-6
  • Omega-3 Omega-3.
  • the Eicosanoids derived from araquidonic acid produce pro-inflammatory effects, while the Eicosanoids derived from EPA have antiinflammatory effects.
  • Phospholipids phosphatidylethanolamine, phosphatydylserine and phosphatidylcholine, once it is necessary for the availability of these phospholipids in the body for better incorporation.
  • Phosphatidylethanolamine performs a fundamental role in the incorporation of omega-3 in the membrane since besides incorporating the greasy acid, it acts as the substrate for the synthesis of phosphatidylcholine containing omega-3, therefore, increase in phosphatidylethanolamine concentration may lead to a significant increase of the incorporation of omega-3, favoring the modulation of the inflammatory processes. Furthermore, it is also worth emphasizing that the synthesis of Phosphatidylethanolamine has some limiting biochemical stages, depending on the concentration of the substrate, where the most important limiting stage is the conversion of Ethanolamine in phosphoethanolamine, catalyzed by Ethanolamine kinase.
  • This limiting stage may be solved with the supply of ready phosphoethanolamine, which will favor the synthesis of phosphatidylethanolamine, increasing its concentration in the body, thus leading to a greater incorporation of omega-3 in the cells, modulating the inflammatory process in patients with bronchial asthma, chronic obstructive pulmonary disease as well as other diseases.
  • Pulmonary Disease is its use through the intake of capsules or liquids in pre-established doses, to produce, over time, positive effects in these chronic diseases.
  • Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive Pulmonary Disease is (1) characterized by the composition of the combination of Phosphoethanolamine (2) and Omega-3 (3) in pre-established proportions, in the ratio of 400 to 1200 mg/day, more specifically in the mean value of 800 mg/day of Phosphoethanolamine (2) combined with omega-3 (3), made up of 500 to 3200 mg/day, more specifically 1000 mg/day of Eicosapentaenoic acid "EPA” (4) and 350 to 2000 mg/day, more specifically 750 mg/day of Docosahexaenoic acid "DHA” (5).

Abstract

The object of the invention is a composition for the treatment of bronchial asthma and chronic obstructive pulmonary disease, characterized in that the composition comprises phosphoethanolamine and Omega-3 folly acids in pre-established proportions. The preferred dose is 400 to 1200 mg/day, more specifically 800 mg/day for the phosphoethanolamine and 500 to 3200 mg/day, more specifically 1000 mg/day for the cicosapentaenoic acid 'EPA' and 350 to 2000 mg/day, more specifically 750 mg/day for the cocosahexaenoic acid 'DHA'.

Description

"CHEMICAL COMPOSITION IN MASS OF
COMPOUND FOR THE TREATMENT OF BRONCHIAL ASTHMA AND CHRONIC OBSTRUCTIVE PULMONARY DISEASE".
1 - INTRODUCTION. The present descriptive report of the Patent of
Invention describes the Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive Pulmonary Disease (COPD), characterized by the composition of the combination of Phosphoethanolamine and Omega-3 in pre-established proportions, in the ratio of 400 to 1200 mg/day of Phosphoethanolamine; 500 to 3200 mg/day of
Eicosapentaenoic acid "EPA" and 350 to 2000 mg/day of Docosahexaenoic acid "DHA", emphasizing that the combination of these components should be consumed by time by the patient in capsule or liquid form.
From its components, it is worth emphasizing that phosphoethanolamine, also known as Amino Ethanol Phosphate, Colamine
Phosphate, Ca-EAP, is a phosphoester existing in all organisms, and it is made up of Ethanolamine phosphorylation and synthesizes one of the Phospholipids, phosphatidylethanolamine.
This substance can be found in food, in low concentration just as in some food supplements, emphasizing that the synthesis of phosphoethanolamine in laboratories has its patent registered under public dominion.
A second component is made up of Omega-3, which is made up of an unsaturated greasy acid, which has the first 3 double carbon bonds after the methyl terminal.
Furthermore, it is worth emphasizing that the Omega-
3 may be of three types, Linolenic acid, eicosapentaenoic acid, "EPA", and Docosahexaenoic acid "DHA" and, it is incorporated in the body, most specifically in Phospholipids of the cell membrane, where it has structure and metabolic functions, acting as a substrate for the formation of various Cytokines through the metabolism of Eicosanoids.
Eicosanoids are molecules derived from 20-carbon greasy acids (EPA and Araquidonic acid), with the ability to signal cells, performing an important role in various activities such as inflammatory and immunological response modulation, platelet aggregation, cell growth and differentiation.
These greasy acids are separated from the
Phospholipids of the cell membrane by Phospholipase A2, and under the action of Cyclooxygenase ( COX ) produce Prostaglandins and Thromboxanes, and produce Leukotrienes under the action of Lipoxygenase.
The relative amount of polyunsaturated greasy acids in the cell membrane is the primary factor to regulate the Eicosanoid will be produced, and the hydrolytic release of greasy acid from the cell membrane occurs both with the araquidonic acid (a type of omega-6) and Omega-3. As araquidonic acid (omega-6) makes up greater part of the polyunsaturated greasy acids in the cell membrane, greater part of the Eicosanoids produced will be series-2 prostanoids ( prostaglandins and thromboxanes ) and series-4 leukotrienes.
Furthermore, it is also worth emphasizing that EPA is a substrate for the production of series-3 Prostanoids and series-5 Leukotrienes.
The Eicosanoids derived from araquidonic acid produce pro-inflammatory effects, while the Eicosanoids derived from EPA have antiinflammatory effects.
Therefore, the combination of these compound components of the application for concession of privilege, results in the largest incorporation of omega-3 in the cell membrane predominantly through the
Phospholipids, phosphatidylethanolamine, phosphatydylserine and phosphatidylcholine, once it is necessary for the availability of these phospholipids in the body for better incorporation.
Phosphatidylethanolamine performs a fundamental role in the incorporation of omega-3 in the membrane since besides incorporating the greasy acid, it acts as the substrate for the synthesis of phosphatidylcholine containing omega-3, therefore, increase in phosphatidylethanolamine concentration may lead to a significant increase of the incorporation of omega-3, favoring the modulation of the inflammatory processes. Furthermore, it is also worth emphasizing that the synthesis of Phosphatidylethanolamine has some limiting biochemical stages, depending on the concentration of the substrate, where the most important limiting stage is the conversion of Ethanolamine in phosphoethanolamine, catalyzed by Ethanolamine kinase. This limiting stage may be solved with the supply of ready phosphoethanolamine, which will favor the synthesis of phosphatidylethanolamine, increasing its concentration in the body, thus leading to a greater incorporation of omega-3 in the cells, modulating the inflammatory process in patients with bronchial asthma, chronic obstructive pulmonary disease as well as other diseases.
2.- FIELD OF APPLICATION. The field of application of this Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive Pulmonary Disease refers to the area of health, specifically the treatment of diseases such as bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, cancer, Parkinson's and Alzheimer's diseases, multiple sclerosis and schizophrenia.
3 - PURPOSE.
The purpose of this Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive
Pulmonary Disease, as its name implies, is its use through the intake of capsules or liquids in pre-established doses, to produce, over time, positive effects in these chronic diseases.
4.- STATUS OF THE TECHNIQUE. According to knowledge verified by investigators and technicians in the areas of health, nutrition and others, it is confirmed that the use of Phosphoethanolamine alone was introduced into the market for the treatment of Multiple Sclerosis and Omega-3 through fish-oil capsules to partially benefit asthmatic patients with bronchospasms. 5.- TECHNOLOGICAL DEVELOPMENT.
With the aim of presenting differential alternative techniques and improvement in the results obtained from these disease and others, the Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive Pulmonary Disease among Other Diseases was created and developed, and it implements a compound whose technological development is based on the use of a compound comprising the association of Phosphoethanolamine with Omega-3 in predetermined mass proportions, which produce positive effects in the following diseases:
Bronchial asthma, ■ Chronic obstructive pulmonary disease,
Rheumatoid arthritis,
■ Cancer,
Parkinson's Disease,
Alzheimer's Disease, ■ Multiple Sclerosis,
Schizophrenia.
6.- DESCRIPTION OF THE DRAWINGS.
To obtain a full and complete picture of how this
Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive Pulmonary Disease, matter and object of the present patent of invention, is constituted, see the attached illustrative table, which makes references as follows:
Shows illustrative table of the quantities of each ingredient, distributed in intervals of masses and their respective mean values.
Chemical Composition in Mass
Figure imgf000006_0001
7.- DESCRIPTION OF THE INVENTION.
According to the table above, which is also a part of this report, Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive Pulmonary Disease is (1) characterized by the composition of the combination of Phosphoethanolamine (2) and Omega-3 (3) in pre-established proportions, in the ratio of 400 to 1200 mg/day, more specifically in the mean value of 800 mg/day of Phosphoethanolamine (2) combined with omega-3 (3), made up of 500 to 3200 mg/day, more specifically 1000 mg/day of Eicosapentaenoic acid "EPA" (4) and 350 to 2000 mg/day, more specifically 750 mg/day of Docosahexaenoic acid "DHA" (5).
8.- CONCLUSION.
It is confirmed by all that was described and illustrated that is about a Chemical Composition in Mass of Compound for the Treatment of Bronchial Asthma and Chronic Obstructive Pulmonary Disease (1), which perfectly classifies within the standards ruling the Patent of Invention, filling the important gap existing in the market, deserving the respective privilege based on what was described and illustrated.

Claims

1) CHEMICAL COMPOSITION IN MASS OF
COMPOUND FOR THE TREATMENT OF BRONCHIAL ASTHMA AND
CHRONIC OBSTRUCTIVE PULMONARY DISEASE (1), characterized by composition of the combination of Phosphoethanolamine (2) and Omega-3 (3) in pre-established proportions, in the ratio of 400 to 1200 mg/day, more specifically in the mean value of 800 mg/day of Phosphoethanolamine (2) combined with omega-3 (3), made up of 500 to 3200 mg/day, more specifically 1000 mg/day of
Eicosapentaenoic acid "EPA" (4) and 350 to 2000 mg/day, more specifically 750 mg/day of Docosahexaenoic acid "DHA" (5).
PCT/BR2008/000093 2007-03-29 2008-03-31 Combi-preparation of phosphoethanolamine and omega-3-fatty acid for treating bronchial asthma and copd WO2008119146A2 (en)

Priority Applications (1)

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PCT/BR2008/000093 WO2008119146A2 (en) 2007-03-29 2008-03-31 Combi-preparation of phosphoethanolamine and omega-3-fatty acid for treating bronchial asthma and copd

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
BRPI0701374-4 2007-03-29
PCT/BR2008/000093 WO2008119146A2 (en) 2007-03-29 2008-03-31 Combi-preparation of phosphoethanolamine and omega-3-fatty acid for treating bronchial asthma and copd

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017177296A1 (en) * 2016-04-13 2017-10-19 Acolli S.A. Food supplement based on 2-aminoethyl dihydrogen phosphate and synthesis method

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993021912A1 (en) * 1992-04-28 1993-11-11 Fresenius Ag Use of an emulsion containing omega-3 fatty acids to produce a medicament to be parenterally administered for treating inflammatory diseases
WO2004064716A2 (en) * 2003-01-24 2004-08-05 Pabay Investments Limited Eicosapentaenoic acid and docosapentaenoic acid for treating inflammatory disorders
US20050080052A1 (en) * 1998-11-26 2005-04-14 Britannia Pharmaceuticals Limited Anti-asthmatic combinations comprising surface active phospholipids
WO2005089744A2 (en) * 2004-03-17 2005-09-29 The Brigham And Women's Hospital, Inc. Use of docosatrienes, resolvins and their stable analogs in the treatment of airway diseases and asthma
WO2007026071A1 (en) * 2005-09-01 2007-03-08 Pieroni Gerard Use of dha in the form of phospholipids for the preparation of a composition that is intended for the treatment of respiratory failure

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993021912A1 (en) * 1992-04-28 1993-11-11 Fresenius Ag Use of an emulsion containing omega-3 fatty acids to produce a medicament to be parenterally administered for treating inflammatory diseases
US20050080052A1 (en) * 1998-11-26 2005-04-14 Britannia Pharmaceuticals Limited Anti-asthmatic combinations comprising surface active phospholipids
WO2004064716A2 (en) * 2003-01-24 2004-08-05 Pabay Investments Limited Eicosapentaenoic acid and docosapentaenoic acid for treating inflammatory disorders
WO2005089744A2 (en) * 2004-03-17 2005-09-29 The Brigham And Women's Hospital, Inc. Use of docosatrienes, resolvins and their stable analogs in the treatment of airway diseases and asthma
WO2007026071A1 (en) * 2005-09-01 2007-03-08 Pieroni Gerard Use of dha in the form of phospholipids for the preparation of a composition that is intended for the treatment of respiratory failure

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017177296A1 (en) * 2016-04-13 2017-10-19 Acolli S.A. Food supplement based on 2-aminoethyl dihydrogen phosphate and synthesis method

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WO2008119146A3 (en) 2008-12-18

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