US3050443A - Headache remedy containing ammonia - Google Patents

Headache remedy containing ammonia Download PDF

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US3050443A
US3050443A US8993A US899360A US3050443A US 3050443 A US3050443 A US 3050443A US 8993 A US8993 A US 8993A US 899360 A US899360 A US 899360A US 3050443 A US3050443 A US 3050443A
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headache
ammonia
remedy
chloroform
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US8993A
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Clifford E Roop
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JAMES F SCHUYLER
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JAMES F SCHUYLER
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]

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  • This invention relates to a headache remedy and more particularly to a new and improved remedy for rapidly, conveniently, expeditiously and pleasantly relieving the pain of a tension headache.
  • Headache or cephalalgia is one of the most common of all symptoms and may be present in connection with a wide variety of conditions. Headaches of the type resulting from organic disease fall into five general categories. They may be caused by increased pressure on the brain resulting from any one of a number of causes. This type of headache may be classified as intracranial. Other headaches produced by changes in the skull are known as cranial headaches. A third class of headache resulting from organic disease is one involving the sensory nerves of the scalp. Lesions of the eye, middle ear, nasal sinuses or the oral cavity may generate headache of the extracranial type.
  • a headache of this type may be migraine. It may be caused by a toxic state as a result of infection; as a result of alcoholism, uremia, lead, morphine, or carbon monoxide poisoning, or encephalitides. A headache of this type can be induced by administration of histamine. Of all the types of headache falling under the general category of those resulting from vascular disturbances, the most common is that caused by hypertension. A headache resulting from hypertension or nervous excitement or worry may be termed a tension headache.
  • the tension headache discussed hereinabove is characterized by a dilation of the cerebral and extra-cranial blood vessels producing pressures which occasion the pain incident to the headache.
  • Many attempts have been made in the prior art to provide a quick and effective relief for the tension headache. Remedies of the prior art whichhave been successful in any measure require that a pill be taken orally. Before relief is experienced the ingredients making up the pill must be dissolved and must be absorbed into the blood stream. Thus with these remedies some time elapses before relief is experienced.
  • This invention relates to a headache remedy which affords relief from the pain incident to a tension headache in a very short period of time and affords rapid relief from the pain of tension headache without affecting the :digestivesystem.
  • One object of this invention is to provide a headache remedy which gives relief from the pain of a tension headache in an extremely rapid and expeditious manner.
  • a still further object'of the invention is to provide a headache remedy for giving rapid relief from the pain of a tension headache without producing the undesirable side effects which may result from the use of remedies of the prior art.
  • this invention contemplates the provision of a headache remedy comprising an inhalant which will stimulate nasal mucous membranes which inhalant comprises a critical concentration of ammonia.
  • the inhalation of concentrated ammonia vapor will cause edema of the respiratory tract and spasm of the glottis with resultant asphyxia.
  • the maximum concentration of ammonia vapors, for example, which can be tolerated for an exposure of eight hours is only parts per million.
  • ammonia is known to the art. It is administered through aromatic spirit of ammonia which is a solution comprising essentially 10% of 10% ammonia water and is used as an analeptic in syncope. It has also been administered orally in well diluted small doses in cases of hyperacidity. Owing to its pungent, irritating, suffocating odor it cannot be inhaled except in single whiffs.
  • the inventor has discovered that by diluting the ammonia so that the vaporiza'ble or atomizable liquid contains between 0.10% and 0.30% by weight of ammonia that the vapors may be inhaled for a sufficiently long period of time to cause the necessary stimulation of the nasal mucous membranes to afford relief from tension headache.
  • ammonia is critical. Less than substantially .1% is insufficient to afford relief from tension headache. A concentration greater than 30% becomes too pungent and irritating to be inhaled for a sufficiently long period of time to produce the desired relief.
  • the inventor has further discovered that he may combine the ammonia with chloroform and inhibit the pungent, irritating effects of ammonia still further while nevertheless not destroying the mechanism which enables ammonia to produce relief from tension headache.
  • FIGURE 1 is a representation of a photograph of the fundus of the eye of a patient showing the dilation of blood vessels accompanying a tension headache.
  • FIGURE 2 is a representation of a photograph of the fundus of the eye of the same patient showing the uncongested condition of the blood vessels following the administration of the remedy of the subject matter of this invention.
  • aromatic spirit of ammonia which is essentially a solution of 10% of 10% ammonia water in absolute alcohol together with 1% of lemon oil and minor amounts of oil of lavender and oil of myristica. It will be observed that we have substantially 1% of ammonia in spirit of amomnia and it was immediately evident that it was impossible to cure -a headache by inhaling the vapors from aromatic spirit of ammonia owing to its pungent and irritating nature which prevented the inhalation for a sufficiently long period of time to effect the necessary stimulation which resulted in a relieving of the spec res After about .30% there was too much burning for the medication to be inhaled for a sufficiently long period of time. With less than 01% of ammonia there appeared to be insufficient stimulation to effect a relief of the headache.
  • the remedy can readily be administered by soaking a cotton wick in a nasal inhaler with the remedy and inhaling the vapors through the inhaler.
  • the remedy may also be air atomized by means of a conventional nasal atomizer.
  • EXAMPLE A A first formulation was made using 9 parts by weight of spirit of ammonia, 9 parts by weight of chloroform and 82 parts by weight of additional ethyl alcohol.
  • EXAMPLE B Formulation was made using 12 parts by weight of spirit of ammonia, 12 parts by weight of chloroform and 76 parts by weight of added ethyl alcohol.
  • Formula A is at the threshold of the minimum amount of chloroform effective for use in the instant invention and Formula C represents the highest practical formula which can be used.
  • EXAMPLE E A formulation was made using 12 parts by weight of spirit of ammonia, 7 parts by weight of chloroform and 81 parts by weight of Freon 12.
  • the remedy of the instant invention can be administered in a number of different ways.
  • An ampule containing some of the remedy may be surrounded by a wick.
  • the ampule is adapted to be broken to saturate the wick enabling the remedy to be inhaled.
  • Absorbent cotton may be saturated with the remedy and placed in a nasal inhaler adapted to be maintained sealed.
  • the remedy may be placed in an atomized bottle and atomized by means of air.
  • a small aerosol bomb containing the remedy may be used as a dispenser and the Freon propellant adapted to propel into contact with the mucous membranes.
  • An inhalent headache medicament including in combination between about .10% by weight and about .30% by weight of ammonia dissolved in a major amount of a volatile fluid.
  • An inhalent headache medicament comprising in combination between about 10% by weight and about 30% by weight of ammonia dissolved in a major amount by weight of ethyl alcohol.
  • An inhalent headache medicament including in combination between about .10% by weight and 30% by weight of ammonia and a major amount of dichlorodifluoromethane.
  • An inhalent headache medicament including in combination between about .10% by weight and about 30% by weight of ammonia, between about 5.00% by weight and 30.00% by weight of chloroform and a major amount of a volatile fluid.
  • a nasal inhalent headache medicament including in combination between about .10% by weight and about 30% by weight of ammonia, between about 5.00% by weight and 30.00% by weight of chloroform and a major amount of ethyl alcohol.
  • a nasal inhalent headache medicament including in combination between about .10% by weight and about 30% by weight of ammonia, between about 5.00% by weight and 30.00% by weight of chloroform and a major amount of dichlorodifluoromethane.
  • a nasal inhalent headache medicament including in combination about .12% by weight of ammonia, about 12.00% by weight of chloroform and a major amount of ethyl alcohol.
  • a nasal inhalent headache medicament including in combination about 112% by weight of ammonia, about 7.00% by weight of chloroform and a major amount of dichlorodifluonomethane.

Description

Aug. 21, 1962 K. J. KRAUS 3,050,443
HEADACHE REMEDY CONTAINING AMMONIA Filed Feb. 16, 1960 INVENTOR.
KARL JJfRAUS DECEASED 8V] CLIFFORD EROOP ,AOMl/IISTRATOR BY HTTOE'NEY nite tates atent 3,@50,443 r' atenterl Aug. 21, 1962 3,050,443 HEADACHE REMEDY ONTAINING AMMONIA Karl J. Kraus, deceased, fate of Las Vegas, New, by Clifford E. Roop, administrator, Las Vegas, Nev., assignor to James F. Schuyler, Las Vegas, Nev.
Filed Feb. 16, B69, Ser. No. 8393 8 Claims. (Q1. rev-s4) This invention relates to a headache remedy and more particularly to a new and improved remedy for rapidly, conveniently, expeditiously and pleasantly relieving the pain of a tension headache.
Headache or cephalalgia is one of the most common of all symptoms and may be present in connection with a wide variety of conditions. Headaches of the type resulting from organic disease fall into five general categories. They may be caused by increased pressure on the brain resulting from any one of a number of causes. This type of headache may be classified as intracranial. Other headaches produced by changes in the skull are known as cranial headaches. A third class of headache resulting from organic disease is one involving the sensory nerves of the scalp. Lesions of the eye, middle ear, nasal sinuses or the oral cavity may generate headache of the extracranial type.
The last category of headache resulting from organic disease is that which is caused by vascular disturbances. A headache of this type may be migraine. It may be caused by a toxic state as a result of infection; as a result of alcoholism, uremia, lead, morphine, or carbon monoxide poisoning, or encephalitides. A headache of this type can be induced by administration of histamine. Of all the types of headache falling under the general category of those resulting from vascular disturbances, the most common is that caused by hypertension. A headache resulting from hypertension or nervous excitement or worry may be termed a tension headache.
The tension headache discussed hereinabove is characterized by a dilation of the cerebral and extra-cranial blood vessels producing pressures which occasion the pain incident to the headache. Many attempts have been made in the prior art to provide a quick and effective relief for the tension headache. Remedies of the prior art whichhave been successful in any measure require that a pill be taken orally. Before relief is experienced the ingredients making up the pill must be dissolved and must be absorbed into the blood stream. Thus with these remedies some time elapses before relief is experienced.
In many instances these remedies have produced undesirable reactions in the patient such as digestive disturbances. Various combinations of ingredients have been employed in an attempt to avoid the undesirable side effects .of the pain-relieving ingredient.
This invention relates to a headache remedy which affords relief from the pain incident to a tension headache in a very short period of time and affords rapid relief from the pain of tension headache without affecting the :digestivesystem.
One object of this invention is to provide a headache remedy which gives relief from the pain of a tension headache in an extremely rapid and expeditious manner.
A still further object'of the invention is to provide a headache remedy for giving rapid relief from the pain of a tension headache without producing the undesirable side effects which may result from the use of remedies of the prior art.
Other and further objects of the invention will appear from the following description.
In general this invention contemplates the provision of a headache remedy comprising an inhalant which will stimulate nasal mucous membranes which inhalant comprises a critical concentration of ammonia. The inhalation of concentrated ammonia vapor will cause edema of the respiratory tract and spasm of the glottis with resultant asphyxia. The maximum concentration of ammonia vapors, for example, which can be tolerated for an exposure of eight hours is only parts per million.
The inhalation of ammonia is known to the art. It is administered through aromatic spirit of ammonia which is a solution comprising essentially 10% of 10% ammonia water and is used as an analeptic in syncope. It has also been administered orally in well diluted small doses in cases of hyperacidity. Owing to its pungent, irritating, suffocating odor it cannot be inhaled except in single whiffs. The inventor has discovered that by diluting the ammonia so that the vaporiza'ble or atomizable liquid contains between 0.10% and 0.30% by weight of ammonia that the vapors may be inhaled for a sufficiently long period of time to cause the necessary stimulation of the nasal mucous membranes to afford relief from tension headache. It is to be noted that the amount of ammonia is critical. Less than substantially .1% is insufficient to afford relief from tension headache. A concentration greater than 30% becomes too pungent and irritating to be inhaled for a sufficiently long period of time to produce the desired relief. The inventor has further discovered that he may combine the ammonia with chloroform and inhibit the pungent, irritating effects of ammonia still further while nevertheless not destroying the mechanism which enables ammonia to produce relief from tension headache.
In the accompanying drawing which forms part of the instant specification and which is to be read in conjunction therewith, FIGURE 1 is a representation of a photograph of the fundus of the eye of a patient showing the dilation of blood vessels accompanying a tension headache.
FIGURE 2 is a representation of a photograph of the fundus of the eye of the same patient showing the uncongested condition of the blood vessels following the administration of the remedy of the subject matter of this invention.
More particularly referring now to the drawings, applicant has discovered that by stimulating the receptors in the nasal mucous membranes 2. vase-motor reaction is produced in the cranial vasculature which causes a constriction of the dilated or congested-blood vessels and an accompanying relief from pain. In other words it has been discovered that this stimulation of the mucous membranes of the nasal passages produces a shock effect which causes the mechanism pointed out hereinabove. As a result of this reaction the blood vessels contract. By their very nature most noxious agents are sufficiently shocking to produce the reaction but with most agents the discomfort and damage produced by their use is so extreme as to make them unfit for use as remedies.
Inventor started with aromatic spirit of ammonia which is essentially a solution of 10% of 10% ammonia water in absolute alcohol together with 1% of lemon oil and minor amounts of oil of lavender and oil of myristica. It will be observed that we have substantially 1% of ammonia in spirit of amomnia and it was immediately evident that it was impossible to cure -a headache by inhaling the vapors from aromatic spirit of ammonia owing to its pungent and irritating nature which prevented the inhalation for a sufficiently long period of time to effect the necessary stimulation which resulted in a relieving of the spec res After about .30% there was too much burning for the medication to be inhaled for a sufficiently long period of time. With less than 01% of ammonia there appeared to be insufficient stimulation to effect a relief of the headache.
The variation in the percentage of ammonia was arrived at by starting with aromatic spirit of ammonia and diluting the aromatic spirit of ammonia with diluents to reduce the amount of ammonia present in the solution.
With a number of individuals, however, smarting was such that the remedy, while relieving a headache, was unpleasant. The inventor discovered that by adding chloroform preferably in a ratio of 100 parts chloroform by weight to one part of ammonia by weight that the pain and irritation of ammonia inhalation was obviated and yet surprisingly sufficient stimulation was obtained to permit the mechanism of the instant invention to occur.
The remedy can readily be administered by soaking a cotton wick in a nasal inhaler with the remedy and inhaling the vapors through the inhaler. The remedy may also be air atomized by means of a conventional nasal atomizer.
Work was then done with an aersol employing Freon 12 (a trademark of E. I. du Pont de Nemours and Co.) for dichlorodifluoromethaneCl F It was found that when Freon was used as a propellant the amount of chloroform could be reduced. Instead of a ratio of 100 parts of chloroform by weight to one part of ammonia by weight about 50 to 60 parts of chloroform by weight to 1 part of ammonia by weight could be used. Stated otherwise, the use of a Freon as a propellant for the medicament made the ammonia less pungent and less irritating to a user.
EXAMPLE A A first formulation was made using 9 parts by weight of spirit of ammonia, 9 parts by weight of chloroform and 82 parts by weight of additional ethyl alcohol.
EXAMPLE B Formulation was made using 12 parts by weight of spirit of ammonia, 12 parts by weight of chloroform and 76 parts by weight of added ethyl alcohol.
EXAMPLE C Air Atomized (Percent by Weight) Spirit of Chloro- Added Ammonia form Alcohol The above formulations break down into the following constituents:
Air Atomized (Percent by Weight) NH H3O CHGL3 C 13 OH Misc.
A 0. 09 3. 11 9. 00 87. 40 0. 40 B 0. 12 4. 14 l2. 00 83. 0. 54 C 0. 10. 30. 00 58. 00 1. 35
In the above tables Formula A is at the threshold of the minimum amount of chloroform effective for use in the instant invention and Formula C represents the highest practical formula which can be used.
4 EXAMPLE D A formulation was made employing 9 parts by weight of spirit of ammonia, 5 parts by weight of chloroform and 86 parts by weight of Freon l2.
EXAMPLE E A formulation was made using 12 parts by weight of spirit of ammonia, 7 parts by weight of chloroform and 81 parts by weight of Freon 12.
EXAMPLE F Spirit of Ohloro- Propel- Arnmonia form lant Propellant Atomized (Percent by Weight) NH H O l OHCl; C2H5OH CClzFz I Misc.
D 0. 00 3.11 5.00 5. 40 86. 00 0. 40 E 0.12 4.14 7.00 7.14 81.00 0.60 F 0. a0 10. 40 17. 00 17.80 53. oo 1. so
It will be appreciated that the remedy of the instant invention can be administered in a number of different ways. An ampule containing some of the remedy may be surrounded by a wick. The ampule is adapted to be broken to saturate the wick enabling the remedy to be inhaled. Absorbent cotton may be saturated with the remedy and placed in a nasal inhaler adapted to be maintained sealed. The remedy may be placed in an atomized bottle and atomized by means of air. Preferably, a small aerosol bomb containing the remedy may be used as a dispenser and the Freon propellant adapted to propel into contact with the mucous membranes.
It will be seen that the inventor has accomplished the object of his invention. He has provided a headache remedy which gives relief from the pain of tension headache in an extremely rapid and expeditious manner without producing undesirable side effects which result from the remedies of the prior art. Applicants remedy is simple and convenient to administer and may be taken by a sufferer by means of inhaling the vapors from nasal inhalers, aerosol bombs, atomizers or saturated wicks.
It will be understood that certain features and sub? combinations are of utility and may be employed without reference to other features and subcombinations. This is contemplated by and is within the scope of the claims. It is further obvious that various changes may be made in details within the scope of the claims without departing from the spirit of the invention. It is, therefore, to be understood that the invention is not to be limited to the specific details shown and described.
Having thus described the invention, what is claimed is:
1. An inhalent headache medicament including in combination between about .10% by weight and about .30% by weight of ammonia dissolved in a major amount of a volatile fluid.
2. An inhalent headache medicament comprising in combination between about 10% by weight and about 30% by weight of ammonia dissolved in a major amount by weight of ethyl alcohol.
3. An inhalent headache medicament including in combination between about .10% by weight and 30% by weight of ammonia and a major amount of dichlorodifluoromethane.
4. An inhalent headache medicament including in combination between about .10% by weight and about 30% by weight of ammonia, between about 5.00% by weight and 30.00% by weight of chloroform and a major amount of a volatile fluid.
5. A nasal inhalent headache medicament including in combination between about .10% by weight and about 30% by weight of ammonia, between about 5.00% by weight and 30.00% by weight of chloroform and a major amount of ethyl alcohol.
6. A nasal inhalent headache medicament including in combination between about .10% by weight and about 30% by weight of ammonia, between about 5.00% by weight and 30.00% by weight of chloroform and a major amount of dichlorodifluoromethane.
7. A nasal inhalent headache medicament including in combination about .12% by weight of ammonia, about 12.00% by weight of chloroform and a major amount of ethyl alcohol.
8. A nasal inhalent headache medicament including in combination about 112% by weight of ammonia, about 7.00% by weight of chloroform and a major amount of dichlorodifluonomethane.
References Cited in the file of this patent UNITED STATES PATENTS 66,667 Abbott July 16, 1867 309,655 Scott Dec. 23, 1884 786,453 Mitchell Apr. 4, 1905 2,598,823 OGrady June 3, 1952 2,868,691 Porush Jan. 13, 1959 OTHER REFERENCES King: American Dispensatory 8th edition 1870, Cincinnati, Ohio, page 930.
Pharmaceutical Formulas, eleventh edition, 1944, page 699, the Chemist and Druggist, London, England.
UNITED STATES PATENT. OFFICE CERTIFICATE OF CORRECTION Patent No 8 O5O 443 August 2-1 1-962 Karl J. Kraus et ala, deceased, by Clifford E Hoop administrator It is hereby certified that error appears in the above numbered patent requiring correction and that the said Letters Patent should read as corrected below.
Column 4, line 73 for "30%" read 630% Signed and sealed this 20th day of November 1962 (SEAL) Attest:
ERNEST w, SWIDER DAVID LADD Attesting Officer Commissioner of Patents

Claims (1)

1. AN INHALENT HEADACHE MEDICAMENT INCLUDING IN COMBINATION BETWEEN ABOUT .10% BY WEIGHT AND ABOUT .30% BY WEIGHT OF AMMONIA DISSOLVED IN A MAJOR AMOUNT OF A VOLATILE FLUID.
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4919919A (en) * 1987-09-30 1990-04-24 Nippon Kayaku Kabushiki Kaisha Nitroglycerin spray
US7612033B2 (en) * 1994-11-29 2009-11-03 Imarx Pharmaceutical Corp. Methods for delivering compounds into a cell

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US66667A (en) * 1867-07-16 abbott
US309655A (en) * 1884-12-23 Catarrh remedy
US786453A (en) * 1905-01-03 1905-04-04 William M Mitchell Inhaling compound for firemen's use.
US2598823A (en) * 1947-12-04 1952-06-03 O'grady Austin Peter Joseph Inhalant preparation
US2868691A (en) * 1956-03-21 1959-01-13 Riker Laboratories Inc Self-propelling compositions for inhalation therapy containing a salt of isoproterenol or epinephrine

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US66667A (en) * 1867-07-16 abbott
US309655A (en) * 1884-12-23 Catarrh remedy
US786453A (en) * 1905-01-03 1905-04-04 William M Mitchell Inhaling compound for firemen's use.
US2598823A (en) * 1947-12-04 1952-06-03 O'grady Austin Peter Joseph Inhalant preparation
US2868691A (en) * 1956-03-21 1959-01-13 Riker Laboratories Inc Self-propelling compositions for inhalation therapy containing a salt of isoproterenol or epinephrine

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4919919A (en) * 1987-09-30 1990-04-24 Nippon Kayaku Kabushiki Kaisha Nitroglycerin spray
US7612033B2 (en) * 1994-11-29 2009-11-03 Imarx Pharmaceutical Corp. Methods for delivering compounds into a cell

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