WO2015012779A1 - Médicament à effet cardioprotecteur - Google Patents

Médicament à effet cardioprotecteur Download PDF

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Publication number
WO2015012779A1
WO2015012779A1 PCT/UA2013/000127 UA2013000127W WO2015012779A1 WO 2015012779 A1 WO2015012779 A1 WO 2015012779A1 UA 2013000127 W UA2013000127 W UA 2013000127W WO 2015012779 A1 WO2015012779 A1 WO 2015012779A1
Authority
WO
WIPO (PCT)
Prior art keywords
mexidol
meldonium
drug
cardioprotective
heart
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/UA2013/000127
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English (en)
Russian (ru)
Inventor
Глеб Владимирович ЗАГОРИЙ
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Individual
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Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of WO2015012779A1 publication Critical patent/WO2015012779A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

  • the invention relates to medicine and the pharmaceutical industry, in particular for the creation, production and use of drugs with cardioprotective effects, in particular for the treatment of myocardial infarction, coronary heart disease, as agents for the treatment of disorders of the cardiovascular system that improve metabolism stabilizing the electrophysical parameters of the heart.
  • Cardiovascular diseases have acquired the character of an epidemic in recent decades and they are the leading cause of death in many economically developed countries. Ukraine is no exception, where these diseases account for up to 60% of total mortality. It should also be noted that of all individual risk factors, cardiovascular complications have the most powerful effect on life expectancy.
  • a well-known drug adopted for the prototype which reflects a drug containing meldonium, which is a coronary anti-ischemic drug that limits the development of necrosis in acute myocardial ischemia (patent of Ukraine N ° 52848 of January 15, 2003).
  • this drug restores the balance between delivery and oxygen demand of cells, eliminates the accumulation of toxic metabolic products in cells, protecting them from damage; also has a tonic effect.
  • the body acquires the ability to withstand the load and quickly restore energy reserves. Due to these properties, this drug is used to treat various disorders of the cardiovascular system, blood supply to the brain, as well as increase physical and mental performance.
  • blood circulation improves blood circulation in the focus of ischemia, promotes the redistribution of blood in favor of the ischemic area.
  • IHD angina pectoris, myocardial infarction
  • chronic heart failure cardialgia on the background of dishormonal myocardial dystrophy
  • acute and chronic cerebrovascular disorders stroke, cerebrovascular insufficiency
  • withdrawal syndrome in chronic alcoholism (in combination with specific therapy)
  • ophthalmology with hemophthalmia and retinal hemorrhage of various etiologies
  • thrombosis of the central retinal vein and its branches retinopathies of various etiologies (diabetic, hypertonic) - only for parabulbar administration.
  • the disadvantages of the prototype include the fact that it does not have sufficient antioxidant properties and, accordingly, is not able to prevent violations of cell membranes and degenerative-dystrophic lesions of cardiomyocytes associated with hypoxic conditions and oxidative stress, is not able to effectively limit alternative processes in the myocardium, does not reduce the presence of side effects effects and contraindications, which would additionally prevent the development of myocardial infarction.
  • the basis of the invention is the task of creating a cardioprotective drug for the treatment of heart diseases, as part of complex therapy - IHD (angina pectoris, myocardial infarction), chronic
  • SUBSTITUTE SHEET (RULE 26) heart failure, cardialgia on the background of dishormonal myocardial dystrophy; and which improves not only metabolism, but also enhances antioxidant properties and is an effective tool in the treatment of such diseases and human conditions as physical and mental stress, cerebrovascular syndromes in cardiovascular diseases, retinal hemorrhage, eyeball diseases, and strokes, not specified as hemorrhage or heart attack; during the recovery period after surgery, as well as when restricting activities caused by reduced ability to work, etc., by selecting a qualitative and quantitative composition of components that would ensure a sufficiently high level and a wide range of specific activity, reduce or eliminate the presence of side effects and contraindications , expanded the range of indications.
  • Mexidol is added in the following ratio of components, g:
  • Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) is an inhibitor of free radical processes (an antioxidant drug that prevents lipid peroxidation of cell membranes) and has a more pronounced antihypoxic (increasing tissue resistance to oxygen deficiency) effect.
  • Mexidol has a wide spectrum of biological activity. It is effective in different types of hypoxia (with insufficient supply of tissue with oxygen or a violation of its absorption). Increases the body’s resistance to diseases associated with myocardial infarction, angina pectoris [angina pectoris], acute myocardial infarction, in chronic ischemic heart diseases, in strokes not specified as hemorrhage or heart attack, in pain in the heart region, during recovery from surgery, as well as
  • SUBSTITUTE SHEET (RULE 26) restriction of activity caused by a decrease in disability and in other conditions accompanied by tissue hypoxia.
  • Combined drugs combine metabolic and vasoactive properties, allowing to achieve a better effect in a shorter time and reduce the dose of active substances in comparison with their separate use.
  • the technical result obtained by carrying out the invention is to achieve a high level and a wide range of cardioprotective activity in combination of two active substances, with a synergistic effect, which allows to reduce the dose of the active substance and thus reduce side effects and contraindications.
  • a cardioprotective drug for the treatment of heart diseases improves metabolism, increases antioxidant properties, and can be used to treat heart diseases.
  • the inventive drug has a ratio of components, g:
  • the inventive drug has a ratio of components, g:
  • the inventive drug has a ratio of components, g:
  • the inventive drug has a ratio of components, g:
  • the qualitative and quantitative composition of the proposed method fully fulfills the task of the invention to create a highly effective agent for the treatment of heart disease, which also improves metabolism and cerebral circulation.
  • meldonium improves metabolism, inhibits gamma-butyrobetaine hydroxynase, inhibits the synthesis of carnitine and the transport of long-chain fatty acids through cell membranes, and inhibits the accumulation
  • SUBSTITUTE SHEET (RULE 26) in cells of activated forms of unoxidized fatty acids - derivatives of acylcarnitine and acylcoenzyme A.
  • Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) is a derivative of 3-hydroxypyridine, in chemical structure it is an analogue of pyridoxine, the phosphorylated form of which has a neurotropic, antioxidant and energizing effect.
  • Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) - a derivative of 3-hydroxypyridine improves the functional state of the ischemic myocardium with myocardial infarction, and also improves contractile function of the heart, reduces the occurrence of systolic and diastolic left ventricular dysfunctions.
  • Mexidol The antioxidant activity of Mexidol, the ability to inhibit free radical processes that occur during ischemia and myocardial necrosis, especially during reperfusion, reduces the damaging effect of free radicals on cardiomyocytes.
  • mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) helps to maintain the structural and functional organization of the membranes of cardiomyocytes, stimulates the activity of membrane enzymes phosphodiesterase, adenylate cyclase, and acetyl lchol inesterase.
  • Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) supports the activity of aerobic glycolysis, which develops during acute ischemia, and helps to restore mitochondral redox processes under hypoxic conditions, and increases the synthesis of ATP and creatine phosphate. These mechanisms ensure the integrity of morphological structures and physiological functions of the ischemic myocardium.
  • Mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate) normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone,
  • SUBSTITUTE SHEET restores and / or improves electrical activity and myocardial contractility, and also increases coronary circulation in the ischemic zone, increases the rheological properties of blood. Reduces the effects of reperfusion syndrome in acute coronary insufficiency.
  • the cardiological pharmacological activity of the proposed combined drug was confirmed by preclinical studies in rats on a model of myocardial infarction (catecholamine necrosis). It was found that the use of the proposed drug in the selected prescription significantly reduced the activity of serum creatine phosphokinase (a marker of cardiac pathology), normalized the heart mass coefficient, and attenuated or completely prevented inflammatory degenerative damage to the myocardial histostructure.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne la médecine et l'industrie chimico-pharmaceutique, notamment la mise au point, la fabrication et l'utilisation de médicaments cardioprotecteurs utilisés pour traiter les maladies cardiaques. Le médicament contient, en g: Mexidol 10-50; Meldonium 80-200; des substances auxiliaires constituant le reste jusqu'à 1 l. Le résultat technique consiste à assurer un degré élevé et une gamme étendue d'action cadrioprotectrice et, en même temps, à réduire ou éliminer les effets secondaires et les contre-indications.
PCT/UA2013/000127 2013-07-22 2013-11-05 Médicament à effet cardioprotecteur Ceased WO2015012779A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
UAA201309187A UA117898C2 (uk) 2013-07-22 2013-07-22 Фармацевтична композиція кардіопротекторної дії
UAA201309187 2013-07-22

Publications (1)

Publication Number Publication Date
WO2015012779A1 true WO2015012779A1 (fr) 2015-01-29

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Application Number Title Priority Date Filing Date
PCT/UA2013/000127 Ceased WO2015012779A1 (fr) 2013-07-22 2013-11-05 Médicament à effet cardioprotecteur
PCT/UA2014/000075 Ceased WO2015012781A1 (fr) 2013-07-22 2014-07-22 Agent médicamenteux à action cardio-protectrice

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/UA2014/000075 Ceased WO2015012781A1 (fr) 2013-07-22 2014-07-22 Agent médicamenteux à action cardio-protectrice

Country Status (3)

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RU (1) RU2014130111A (fr)
UA (1) UA117898C2 (fr)
WO (2) WO2015012779A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2661010C1 (ru) * 2017-11-28 2018-07-11 федеральное государственное бюджетное образовательное учреждение высшего образования "Хакасский государственный университет им. Н.Ф. Катанова" (ФГБОУ ВО ХГУ им. Н.Ф. Катанова) Способ лимфатической терапии при панкреатитах у собак

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2425835A1 (fr) * 2010-08-18 2012-03-07 Grindeks, a joint stock company Nouvelle utilisation médicale de dihydrate propionate 3-(2,2,2-trimethylhydrazinium) et dérivés de flavonoïdes naturels

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LV14268B (lv) * 2009-06-25 2011-03-20 Grindeks, A/S Meldonija sukcinātu saturoši medicīniskie produkti
RU2485953C1 (ru) * 2012-04-12 2013-06-27 Общество с ограниченной ответственностью "Научно-внедренческий центр Агроветзащита" Комплекс 3-(2,2,2-триметилгидразиний) пропионат-2-этил-6-метил-3-гидроксипиридина дисукцинат, обладающий антигипоксическим и адаптогенным действием, и способ его получения

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2425835A1 (fr) * 2010-08-18 2012-03-07 Grindeks, a joint stock company Nouvelle utilisation médicale de dihydrate propionate 3-(2,2,2-trimethylhydrazinium) et dérivés de flavonoïdes naturels

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"Instruktsiia po meditsinskomu primeneniiu preparata Meldonii.", 13 August 2008 (2008-08-13), Retrieved from the Internet <URL:http://grls.rosminzdrav.ra/Grls_View.aspx?idReg=9764&is01d=l&t=5e7e4e22-Idd4-404a-8e86-42136dfb456d> *
"Instruktsiia po primeneniiu preparata Meksikor", 22 September 2008 (2008-09-22), Retrieved from the Internet <URL:http://grls,rosminzdrav.ra/Grls_View.aspx?idReg=11081&is01d=1&t=46f4ca5e-403f-4b9f-9e90-21c549cedfbc> *

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Publication number Publication date
RU2014130111A (ru) 2016-02-10
WO2015012781A1 (fr) 2015-01-29
UA117898C2 (uk) 2018-10-25

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