Classifications

• • 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
  • A61K31/16—Amides, e.g. hydroxamic acids
• • 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
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
  • A61K31/365—Lactones
  • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof

Definitions

• Anti-cold kit anti-cold preparation and use thereof
• Common cold is one of the world's most widespread diseases. In some countries it is estimated that about 15 % of all absence from work due to illness is caused by common cold, and although the disease is not considered to be one of the most dangerous ones, it is in any case among the most expensive for society. It is also often a precursor for other respiratory passage diseases, such as bronchitis and pneumonia.
• about one milliliter of drops according to the invention if taken topically provides 1000 times greater levels of ascorbate in the nose than 15 g vitamin C orally in one dose.
• the synergistic effect of the preparation according to the invention results in a desirable prolonged effect on the mucous membrane.
• an anti-cold preparation which is in the form of a substantially isotonic aqueous solution comprising dexpanthenol and a water-soluble, physiologically acceptable ascorbate. It is a further object of the invention to provide an anti-cold kit which comprises a watersoluble, physiologically acceptable ascorbate and dexpanthenol. Furthermore the invention is directed to the use of said kit for the manufacture of said anti-cold preparation. A further object of the invention is the use of the preparation according to the invention for treatment or prophylaxis of conditions responsive to the disclosed synergistic combination of a watersoluble, physiologically acceptable ascorbate and dexpanthenol.
• a water-soluble, physiologically acceptable ascorbate is e. g. an alkali metal ascorbate , such as sodium or potassium ascorbate, or an ascorbate such as calcium ascorbate, zinc ascorbate or ammonium ascorbate.
• An alkali metal ascorbate is preferred, especially preferred is sodium ascorbate of the formula
• D-panthenol also known as D-panthenol, is (R)-2,4-dihydroxy-N-(3-hydroxypro ⁇ yl)-3,3-dimethylbutaneamide of the formula
• kits and the preparation comprise an ascorbate as defined hereinbefore and dexpanthenol as the essential active ingredients, in a preferred embodiment as their only active ingredients.
• the ascorbate and dexpanthenol should be used in a molar ratio of about 5:1 to 1:5, preferably of about 2:1 to 1:2, most preferably in about the same molar amounts. It is possible to use an excess of one or the other component in the preparation, since the components also separately have a favourable effect on their own.
• the preparation must be essentially isotonic, it must be non-irritating and compatible with the tissue and have a pH close to that which is normally found in the nose (mouth, throat).
• An isotonic solution is generally defined as a solution being isoosmotic with a 0,9 % sodium chloride solution.
• the instant essentially isotonic preparation may be slightly hypertonic, but generally the tonicity of the preparation is equivalent to a 0,9 % sodium chloride solution or in the range of a 0.9 % sodium chloride solution.
• the pH of nasal secretion is slightly alkaline (pH between 8 and 9). Accordingly the pH of the preparation is preferably about neutral, e.g. about pH 6 to 7.
• solutions which comprise about 3 % by weight of dexpanthenol and an equimolar amount of ascorbate.
• a preferred preparation comprises about 3 % by weight of sodium ascorbate and about 3 % by weight of dexpanthenol.
• the preparation may also contain isotonicity or pH regulating additions and acceptable flavouring agents and preserving agents.
• pH-regulating additions are buffers, e.g. borate buffers, or preferably phosphate buffers.
• Suitable preserving agents are e.g. methyl- or propyl-p-hydroxy-benzoate, chlorobutanol or, being preferred, benzalkoniumchloride.
• Flavouring agents or artificial sweeteners may be present, such as banana extract (especially for children), anis, menthol, or pineapple. These ingredients are optional and, if present, are present in small amounts.
• a basic salt such as e.g. sodium carbonate
• a pH of the preparation near to neutral.
• Freshly prepared preparations have a redox potential rH (derived according to Clark's formula) of 15.5 whereas the mucus of the nose has an average rH of 23-24 (For details see example 4). Accordingly the preparation of the present invention lowers the redox potential in the nose which is beneficial in that a lower potential is detrimental to the growing conditions of the common cold viruses.
• R.1 2 % aqueous solution of potassium ferricyanide
• R.2 4 % aqueous solution of ferric chloride.
• the flask was then filled to the mark with distilled water.
• the mixing of R.1 and R.2 forms a brown colour, but the presence of any reducing agent will render the solution blue, due to the formation of the Berlin blue colour.
• the intensity of the blue colour was measured using a Lovibond tintometer (cell width 1/2 inch.) and Table 1 gives the experimental results.
• the measurements were made 3 minutes after adding the reagents.
• the values obtained are in direct proportion to the reducing power of the nose washings and are thus an indication of the activity of the solutions as antioxidants i.e.
• the preparation as a kit of two separate units, wherein one unit contains a dry, water-soluble physiologically acceptable ascorbate, such as sodium ascorbate, suitably in a glass bottle equipped with a pipette.
• a dry, water-soluble physiologically acceptable ascorbate such as sodium ascorbate
• An aqueous solution of dexpanthenol is kept in another unit, such as a glass bottle.
• the contents of the two units are mixed, for instance by pouring an aqueous solution of dexpanthenol into the glass bottle containing the starting ascorbate.
• the amount of starting ascorbate and of dexpanthenol must be adjusted so that the resulting solution becomes essentially isotonic.
• the preparation may also be prepared from a kit comprising calculated weighed amounts of the neat active ingredients, ascorbate and dexpanthenol, without the presence of water.
• This kit will be stable for a prolonged time, and a suitable amount of distilled water is added thereto immediately before use, whereby there is obtained a solution which may be used directly.
• the final preparation may also be kept in frozen condition.
• the new preparation may be used as a prophylactic agent or after a cold has broken out. It is suitably used as a prophylactic agent, for instance after a cold epidemic has broken out, and it will then to a considerable extent prevent those who have been treated with the preparation, from catching a cold.
• the new kit and preparation may be beneficial and/or prophylactic against dust or polluted air, and may be used as an antiallergic or antihistaminic agent, e.g. for mammmals, especially human beings, suffering from hey fever.
• the preparation has been successfully tested on several individuals, who have either not caught a cold even if they have been in an environment with much cold, or who have rapidly recovered after having caught a cold.
• a larger systematic test was carried out in a military camp in which all the voluntary test persons were of approximately the same age and were exposed to approximately the same conditions.
• a group of the test persons received a preparation containing the described components, (see example 1), while another group only received a placebo preparation, in each case about 1 ml (20 to 30 drops) in each nostril about 5 times daily. None of the test persons knew whether they received the placebo preparation or a preparation containing the active components.
• a further testing was carried out mainly at the Training Center of the Royal Norwegian Air Force at Kjevik in Southern Norway and also at the University of Oslo.
• the subjects were asked to apply the nosedrops according to the invention into both nostrils so that they could clearly feel it trickling down the back of the nasal cavity and into the throat.
• a small amount was also sprayed into the mouth cavity, over the palate, and in the throat, so that the mucous membranes of the upper respiratory tract were well moistened with the solution.
• the subjects were asked to report on special forms the effects of the drops.
• the preparation (but not the placebo) was also used as a prophylactic during military manoeuvres in the mountains in the winter of 1985. Although the soldiers slept in snow caves where the temperature was well below freezing point (between -15 and -30°C.), none of the participants developed a cold during the manoevres which lasted for about 12 days. In previous years more than 50 % of the soldiers had developed a cold during same type of manoeouvres.
• the clinical tests give the following results showing the distribution of subjects in the two groups, - the group relative to treatment and the placebo-group - having reference to the category and results of treatment and showing the significant level of difference between the two groups:
• Example 1 3.16 g (0.0155 moles) of dexpanthenol are dissolved in 100 ml distilled water, and the solution is filled into a 100 ml bottle. In another 100 ml bottle 3.05 g (0.0155 moles) sodium ascorbate are charged. The content in the two bottles is stable for a long time.* Immediately before use the dexpanthenol solution is filled into the bottle containing the solid sodium ascorbate which dissolves. The resulting solution represents an essentially isotonic preparation ready for use.
• Example 2 The same amounts as above of the two starting materials are mixed and kept in a sterile bottle. The same amount (100 ml) of sterile, distilled water is added immediately before use and results in a clear solution.
• Example 3 After mixing 0.9 g sodium ascorbate (dry substance) with the attached 30 ml solution of stabilized buffered dexpanthenol in water the final mixture has the following composition:
• This preparation of 30 ml has a pH of 6.5. Stability is guaranteed for 1 week.
• E ref standard potential of reference electrode.
• E N value of electrode slope VS temperature. Nernst potential.
• MV Millivolt measured at reference (Platinum/silver chloride) electrode.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Polymers With Sulfur, Phosphorus Or Metals In The Main Chain (AREA)
• Non-Silver Salt Photosensitive Materials And Non-Silver Salt Photography (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Applications Claiming Priority (2)

Publications (1)

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ID=19888883

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• 1986
  • 1986-04-22 NO NO861585A patent/NO161779C/no unknown
• 1987
  • 1987-04-15 GB GB08729227A patent/GB2198946A/en active Pending
  • 1987-04-15 JP JP62502527A patent/JPS63503068A/ja active Pending
  • 1987-04-15 NL NL8720186A patent/NL8720186A/nl unknown
  • 1987-04-15 WO PCT/EP1987/000203 patent/WO1987006465A1/en not_active Application Discontinuation
  • 1987-04-15 EP EP87902498A patent/EP0264410A1/en not_active Withdrawn
  • 1987-04-15 DE DE19873790208 patent/DE3790208T1/de not_active Withdrawn
  • 1987-04-15 FI FI875624A patent/FI875624A0/fi not_active Application Discontinuation
  • 1987-04-15 KR KR1019870701206A patent/KR880701100A/ko not_active Withdrawn
  • 1987-04-15 AU AU72399/87A patent/AU7239987A/en not_active Abandoned
  • 1987-04-22 IL IL82281A patent/IL82281A0/xx unknown
  • 1987-04-22 ZA ZA872824A patent/ZA872824B/xx unknown
  • 1987-12-18 SE SE8705060A patent/SE8705060D0/xx not_active Application Discontinuation
  • 1987-12-21 DK DK674587A patent/DK674587D0/da not_active Application Discontinuation

Non-Patent Citations (1)

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