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
  • A61K33/24—Heavy metals; Compounds thereof
  • A61K33/30—Zinc; Compounds thereof

Definitions

• the invention relates to an antiasthmatic remedy used in human medicine for treatment of bronchial asthma and asthmatic bronchitis.
• Xanthins are known with their stimulating effect on breathing and relieving of bronchospasms (Martindale 1989) .
• Xanthins are known with their combinations with other medicinal substances, having a preventive and prophylactic effect mainly (BE 903065) .
• Atropine sulphate is known as an antimuscarine agent, as well as its use in cases of asthma (Paterson J.W. £ Ta- rala R.A. , Med. J.Aust., 1985, 143,390).
• Papaverine hydrochloride is known as an incontestable spasmolytic agent. It removes bronchial spasms and soothes the center of breathing and cough (Martindale, 1989).
• Ergotamine is known as a sympatholitic agent (Martin ⁇ dale, 1989), as well as its specific effect in congestive states of the lungs, this probably being due to the vaso- constrictive effect on the bronchial vascula.
• Corticosteroid preparations are known as medicines used in treating bronchial asthma and asthmatic bronchitis (Martindale, 1989). Their shotcomings consist in that they can lead to cases of medicinal hypercorticism, e.g. obesity, arterial hypertonia, osteoporosis, gastic and duodenal ul ⁇ cers, infections, etc. After medical treatment is started, the sick person becomes fully dependent on exogenous corti- costeroids, and new fits are not averted, although the con ⁇ dition of the patient improves to a certain extent. The problem consists in making an antiasthmatic remedy breaking off the disease fits and leading to a long remis ⁇ sion for years, i.e. to healing, without showing the grave side effects of corticosteroids.
• the female sex hormone orestrone (diethylstilbestrol) is included in the combination.
• the remedy is used for males, the hormone methandienone is added.
• the combination of active substances according to the invention is suitable for preparation of phar aceutic forms using subsidiary substances and carriers usual for the pharmaceutic technology.
• Sex hormones shall obligatorily be added once to the daily dose of the combination.
• the advantages of the remedy according to the invention are: asthmatic fits are stopped within 30-40 min. ; new cases of painful asthmatic breathing and subsequent asthmatic fits are avoided for a period of 10 or more years; at the same time, the remedy is welltole- rated and does not show the grave side effects and compli ⁇ cations caused by corticosteroids
• Atropine sulphate 1,00 mg Papaverine hydrochloride 100,00 mg
• Caffeine purum 100,00 mg
• mice Male white rats of the Wistar breed with a weight of 180 to 200 grams. The rats were raised under standard food and water conditions. For the tests were used 300 rats altogether.
• the substances were dissolved in Tween 80 upon through grinding, and then they were perorally introduced through a probe in a volume of lml/lOOg bodily weight (b.w.).
• test results are generalised in the table 1. It shows that the substances can be arranged as follows with a view to their toxicity: ergotamine is the most toxic; then come caffeine, papaverine, atropine and zinc sulphate. The combined preparation showed toxicity between those of papaverine and atropine.
• the obtained LD50 values show that the quantities of ergotamine, atropine, zinc sulphate and somewhat papaverine in the combined preparation are far from the respective LD50 values obtained. This is enough to draw the conclusion that the combination toxicity is unlikely to be determined thereby.
• the remedy according to Example 1 is applied orally in the form of pills. During the first 30 days it is given four times a day, one pill at interval of at least 4 hour. The combination containing sex hormones is given to the patient once a day in the bedtime pill.
• the pill taken at bedtime shall contain sex hormones.
• the drug is given only once a day at bedtime, and it must contain sex hormones.
• the medicine according to the invention was tested on 300 patients having bronchial asthma or chronic asthmatic bronchitis. In all cases there was improvement of the condition after the first 30-40 min. upon taking the pill. No side effects and complications, incidental to corti ⁇ costeroids, were observed in the patients under control. Healing is lasting, and no relapses have been observed.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Inorganic Chemistry (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Chemical & Material Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Nitrogen Condensed Heterocyclic Rings (AREA)

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ID=3925621

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• 1994
  • 1994-03-23 BG BG98678A patent/BG61430B1/bg unknown
• 1995
  • 1995-03-22 WO PCT/BG1995/000003 patent/WO1996031222A1/en not_active Application Discontinuation
  • 1995-03-22 EP EP95944853A patent/EP0760669A1/en not_active Withdrawn

Non-Patent Citations (1)

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