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WO2008037037A2 - Médicament anti-asthmatique - Google Patents

Médicament anti-asthmatique Download PDF

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Publication number
WO2008037037A2
WO2008037037A2 PCT/BG2007/000021 BG2007000021W WO2008037037A2 WO 2008037037 A2 WO2008037037 A2 WO 2008037037A2 BG 2007000021 W BG2007000021 W BG 2007000021W WO 2008037037 A2 WO2008037037 A2 WO 2008037037A2
Authority
WO
WIPO (PCT)
Prior art keywords
hydrochloricum
asthmatic
medicine
sulfuricum
coffeinum
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/BG2007/000021
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English (en)
Other versions
WO2008037037A3 (fr
Inventor
Ivan Hristov
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
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 WO2008037037A2 publication Critical patent/WO2008037037A2/fr
Publication of WO2008037037A3 publication Critical patent/WO2008037037A3/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
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/14—Alkali metal chlorides; Alkaline earth metal chlorides
    • 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
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/48—Ergoline derivatives, e.g. lysergic acid, ergotamine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A61K31/515—Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/30—Zinc; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics

Definitions

  • the invention relates to an anti-asthmatic medicine, which can be implemented in the field of the human medicine for a treatment of the bronchial asthma and the asthmatic bronchitis.
  • the ergotaminum is known as an syr ⁇ pathic ⁇ litic /Martinedale, 1989/. It improves the heart activities - enhances the systole contractions, improves the pulse. It has a specific effect with the lung congestion. This effect probably is due to the vasoconstrictive effect on the bronchial tubes.
  • the ergotamintartarat is a partial agonist and antagonist of the alpha- adrenergic system of the glabrous musculature of the blood vessels of the lung and other organs. It is mainly antagonist in the peripheral and the central nervous system.
  • the papaverinum hydrochloricum is known as an undisputed spasmolitic. It removes the bronchospasm and relieves the respiration center and the cough center /Martinedale, 1989/.
  • the atropinum sulfuricum is implemented for healing of the lung asthma /Paterson J.W. and Tara RA., Med. J.Aust. 1985, 143.390/.
  • the zincum sulfuricum is known. In the recent years a significant attention is paid to the zinc salts having in mind their effects influencing the immunity and the metabolic process in the organism.
  • the quantity of the microelement zinc in the organism is approximately 2g. Dependant on the zinc are important ferments as: corticotropinum, somatotropinum, gonadotropinum, insulin /Bjojovski, R., Tatalay, M. etc. "News in the pharmacology and the medicine", 1995, No 3, p.72-76/.
  • the zinc deficiency in the organism results in an immunity decrease.
  • the zinc is mainly accumulated around the centers regulating the respiration rhythm, the rhythm cheerfulness - sleep, the rhythm of the heart activity, intestinal tract etc.
  • zinc salts are used for treatment of the lung, heart-vessel etc. systems. The original moment in the lung asthma treatment is the adding of a zincum sulfuricum.
  • the aminophyllinum is a medicament for a treatment of the lung asthma. It removes the bronchospasm, reduces the resistance of the blood vessels, reduces the pressure in the lung artery system, expands the coronary vessels.
  • the glaucinum hydrochloricum is known - it has an anti-cough effect. Unlike the codeine, it does not suppress the respiration center, does not influence the motoricity of the intestinal tract and does not result in habitation and infatuation.
  • the sulfaguajacolas is known. It is used for treatment of the respiration organs, especially in childish age.
  • the chlorpyraminum is known. It is a competitive blockator of the histamine in term of Hl- receptors. It is used for treatment of the lung asthma in the intervals between the ebullitions.
  • corticosteroids preparations are known used for treatment of the lung asthma /Martindale, 1989/. They have the disadvantage that they may result in symptoms of medicamentous hypercorticismus - obesity, arterial hypertonia, osteoporosis, stomach and duodendal infections etc. After commencing the treatment the patient becomes completely dependant on exogenous corticosteroids and although an improvement to a certain extent of his condition is demonstrated, the appearance of new ebullitions are not prevented.
  • the invention seeks to provide an anti-asthmatic medicine, to be able to stop the attacks of the disease and to result in prolonged remission in the course of 10-20 years i.e. healing in practice and at the same time not to produce the acute side effects of the corticosteroids.
  • this object is accomplished in an antiasthmatic medicine, containing coffeinum purum, ergotamintartarat, zincum sulfuricum, papaverinum hydrochloricum, atropinum sulfuricum, aminophyllinum, glaucinum hydrochloricum, kalium sulfaguajacolicum and chlorpyraminum, having quantity proportions [in mg] as follows:
  • the anti-asthmatic medicine in accordance with the invention has a number of advantages, as follows: - even the acutest asthmatic ebullitions are being put under control in the course of 30-40 minutes;
  • the anti-asthmatic medicine has a good bearing and does not result in complications.
  • Example 1 The medicine contains, in mg:
  • Example 2 The medicine contains, in mg:
  • Example 3 The medicine contains, in mg:
  • Example 4 The medicine contains, in mg:
  • Example 5 Tests for the acute toxicology of the medicine combination. Tests representation:
  • the tests were used male white rats, breed Wistar, having average weight from 130 to 2QQg.
  • the animals were bred at standard conditions in terms of food and water supply. Taken as a whole 300 rats have been used for the tests.
  • the used substances have been supplied by the applicant and they include: coffeinum purum, ergotaminum, zincum sulfurieum, papaverihum hydrochloricum atropinum sulfurieum.
  • the substances were diluted in Tween 80 after good grind and were brought in by means of sound per orally in volume 1 ml/100g. corporal weight.
  • the tests results are generalized in Table 1.
  • Table 1 shows that the substances are classified, in term of their toxicity, as follows: most toxic is the ergotaminum, followed by coffeinum, papaverinum, atropinum and zincum sulfuricum.
  • the combined preparation shows a toxicity, which is in the range of the toxicity of the papaverinum and the atropinum.
  • 100 mg of the medicine are representing approximately 1/5 of LD50 of the combination (5iO mg/kg), which is the sum of the respective parts of the zincum sulfuricum, papaverinum and coffeinum.
  • the medicine in accordance with the invention is a combination having relatively low acute toxicity.
  • the medicine according to Example 1 is implemented orally in the form of dragees.
  • the anti-asthmatic medicine is tested on 2000 patients suffering from bronchial asthma and a chronic asthmatic bronchitis. The condition of all patients was improved after 30-40 minutes after the acceptance of the dragee. No side effects and complications characteristic of the corticosteroids were observed. The healing is lasting and no recidivations were observed.

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  • 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)
  • Inorganic Chemistry (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne un médicament anti-asthmatique qui peut être utilisé en médecine humaine pour traiter un asthme ou une bronchite asthmatique. Ce médicament contient coffeinum purum, ergotamintartarat, zincum sulfuricum, papaverinum hydrochloricum, atropinum sulfuricum, aminophyllinum, glaucinum hydrochloricum, kalium sulfaguajacolicum et chlorpyraminum, dans les proportions suivantes [en mg] : coffeinum purum 30,00 à 250,00; ergotamintartarat 0,25 à 2,00; zincum sulfuricum 10,00 à 400,00; papaverinum hydrochloricum 30,00 à 200,00; atropinum sulfuricum 0,25 à 1,00; aminophyllinum 40,00 à 250,00; glaucinum hydrochloricum 30,00 à 250,00; kalium sulfaguajacolicum 100,00 à 600,00; chlorpyraminum 30,00 à 200,00. Ce médicament est avantageux en ce qu'il permet de maîtriser les crises d'asthme les plus aigües en l'espace de 30-40 minutes, en ce qu'il empêche la réapparition d'une respiration asthmatique douloureuse et de crises asthmatiques résultantes sur une période de 10 à 20 ans, voire au-delà, c'est-à-dire que la maladie est traitée en pratique, en ce qu'il empêche les effets secondaires importants et les complications causés par les corticostéroïdes et en ce qu'il est très bien supporté et n'engendre pas de complications.
PCT/BG2007/000021 2006-09-26 2007-09-19 Médicament anti-asthmatique Ceased WO2008037037A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
BG109687A BG109687A (bg) 2006-09-26 2006-09-26 Антиастматично лекарствено средство
BG109687 2006-09-26

Publications (2)

Publication Number Publication Date
WO2008037037A2 true WO2008037037A2 (fr) 2008-04-03
WO2008037037A3 WO2008037037A3 (fr) 2008-07-10

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Family Applications (1)

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PCT/BG2007/000021 Ceased WO2008037037A2 (fr) 2006-09-26 2007-09-19 Médicament anti-asthmatique

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BG (1) BG109687A (fr)
WO (1) WO2008037037A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113633710A (zh) * 2021-09-29 2021-11-12 浙江养和健康管理科技有限公司 一种治疗支气管炎、哮喘和肺气肿的中药组合物及其制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BG61430B1 (bg) * 1994-03-23 1997-08-29 Иван ХРИСТОВ антиастматично лекарствено средство
EP1561458B1 (fr) * 1998-07-28 2010-09-15 Takeda Pharmaceutical Company Limited Préparation solide à désintégration rapide
BG819Y1 (bg) * 2001-07-10 2006-07-31 "Софарма" Ад Комбинирано средство за повлияване на дихателнатасистема

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113633710A (zh) * 2021-09-29 2021-11-12 浙江养和健康管理科技有限公司 一种治疗支气管炎、哮喘和肺气肿的中药组合物及其制备方法

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Publication number Publication date
BG109687A (bg) 2008-03-31
WO2008037037A3 (fr) 2008-07-10

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