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
  • A61K9/0087—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
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
  • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

• the present invention relates to orally or nasally administrate pharmaceutical compositions comprising at least one pharmaceutical active, 3-1-menthoxy propane 1,2-diol (herein referred to as "MPD") and pharmaceutically-acceptable carrier material(s).
• MPD 3-1-menthoxy propane 1,2-diol
• the present invention also relates to methods for treating cough, cold, cold-like, allergy and/or flu symptoms in a human or lower animal by adminis ⁇ tering, orally or nasally, a composition comprising MPD.
• compositions safe and effective for treating colds, flu, and allergies are well known. Over-the-counter edica- tions provide symptomatic relief of such illnesses. Typical symptoms of the common cold are mild malaise, sore throat and nasal complaints. Nasal discharge, nasal congestion and/or sneezing frequently are present. Also common are sore, dry or scratchy throat and hoarseness and cough. Other symptoms may include mild burning of the eyes, loss of smell and taste, a feeling of pressure or fullness in the sinuses or ears, headache, and vocal impairment. Flu symptoms are similar but usually of greater severity, including fever, generalized aches and pains, fatigue and weakness, and chest discomfort. Allergy symptoms are more akin to the common cold, with more frequent/severe sinus pressure, drainage and headaches.
• Prior art formulations for treating cough, cold, cold-like, allergy and/or flu symptoms and the discomfort, pain, fever and general malaise associated therewith typically contain one or more of the pharmaceutical actives which are analgesics, anesthetics, antihis- tamines, decongestants, cough suppressants, antitussives and expector ⁇ ants.
• compositions and methods useful for treating cough, cold, cold-like, allergy and flu symptoms in humans and lower animals in need of such treatment Another object is to provide such compositions and methods having increased perceived efficacy, e.g., speed of relief and/or duration of relief, and/or improved aesthetics.
• the present invention is directed to pharmaceutical compositions comprising: (a) a safe and effective amount of at least one pharma ⁇ ceutical cold active; (b) 3-1-menthoxy propane 1,2-diol; and (c) a pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
• the present invention is also directed to methods for treating cough, cold, cold-like, allergy, and flu symptoms in a human or lower animal, said method comprising administering to a human or lower animal in need of such treatment, by oral or nasal administration, a composition comprising 3-1-menthoxy propane 1,2-diol.
• the present invention relates to pharmaceutical compositions comprising: (a) at least one pharmaceutical cold active; (b) 3-1- menthoxy propane 1,2-diol ("MPD"); and (c) pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
• MPD 3-1- menthoxy propane 1,2-diol
• pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
• compositions according to the present inven- tion comprise pharmaceutical cold actives useful for treating cough, cold, cold-like, allergy and/or flu symptoms.
• pharmaceutical actives are well known, and are generally recognized as being an active having analgesic, anti-inflammatory, anesthetic, antihistamine, decongestant, cough suppressant, demulcents, antitussive, and/or expectorant properties.
• compositions of this invention therefore contain one or more known pharmaceutical cold actives, particularly those commonly utilized in cough/cold preparations, such as, for example, a decon ⁇ gestant such as pseudoephedrine, phenylpropanolamine, phenylephrine " and ephedrine, their pharmaceutically acceptable salts; an antitussive such as dextromethorphan, chlophedianol, carbetapentane, caramiphen, noscapine, diphenhydramine, codeine, menthol, hydrocodone, hydromor- phone, fo inoben, their pharmaceutically-acceptable salts; an expec- torant or ucolytic such as glyceryl guaiacolate, terpin hydrate, ammonium chloride, N-acetylcysteine and bromhexine, ambroxol, their pharmaceutically acceptable salts; and an antihistamine such as chlorpheniramine, brompheniramine, dexchlorpheni
• Patent 4,783,465 to Sunshine et al. issued November 8, 1988
• U.S. Patent 4,619,934 to Sunshine et al. issued October 28, 1986, which are incorporated by reference herein.
• broncho- dilators such as terbutaline, atropine, aminophylline, epinephrine, isoprenaline, metaproterenol, bitoterol, theophylline and albuterol.
• analgesic compounds such as aspirin, acetaminophen, ibuprofen, and naproxen; and topical anesthetics/analgesics such as phenol, benzocaine, hexyl resorcinol, and dyclonine.
• compositions of the present invention comprise a safe and effective amount of at least one pharmaceutical cold active.
• safe and effective amount means an amount of a compound or composition high enough when administered orall or nasaTly to significantly positively modify the condition to be treated, but low enough to avoid serious side effects (at a reasonable benefit/risk ratio), within the scope of sound medical judgment.
• the safe and effective amount of the pharmaceutical cold active will vary with the particular condition being treated, the age and physical condition of the patient being treated, the severity of the condition, the duration of the treatment, the nature of concurrent therapy, the specific pharmaceutical cold active employed, the particular pharma ⁇ ceutically-acceptable carrier utilized, and like factors within the knowledge and expertise of the attending physician.
• the pharmaceutical cold active(s) comprise from about 0.001% to about 99.9%, by weight, of the pharmaceutical compositions of the present invention, preferably from about 0.001% to about 75%, and most prefer- ably from about 0.01% to about 30%.
• 3-1-Menthoxy Propane 1.2-Diol
• compositions of the present invention also comprise 3-1-menthoxy propane 1,2-diol ("MPD").
• MPD 3-1-menthoxy propane 1,2-diol
• This material is described in detail in U.S. Patent 4,459,425, issued July 10, 1984 to Amano et. al, incorporated herein by reference in its entirety. While not to be limited by theory, it is believed that the benefits obtained by the use of MPD in the compositions of the present invention are the result of the unique cooling profile for this compound.
• MPD is commercially available, being sold by Takasago Perfumery Co., Ltd., Tokyo, Japan.
• MPD typically comprises from about 0.001% to about 10% by weight of the pharmaceutical compositions of the present invention, prefer ⁇ ably from about 0.01% to about 5%, and most preferably from about 0.01% to about 0.5%.
• pharmaceutically-acceptable carrier materials means one or more compatible solid or liquid filler diluents or encapsulating substances which are suitable for oral and/or nasal administration to a human or lower animal.
• compatible means that the components of the com ⁇ positions of the present invention are capable of being commingled with the pharmaceutical cold active, and with each other, in a manner such that there is no interaction which would substantially reduce the pharmaceutical efficacy of the compositions under ordinary use situa ⁇ tions.
• Pharmaceutically-acceptable carrier materials must, of course, be of sufficiently high purity and sufficiently low toxicity to render them suitable for administration to the human being treated.
• compositions comprise from about 0.1% to about 99.99% of one or more pharmaceutically-acceptable carrier materials.
• Solid oral dosage forms preferably contain from about 0.1% to about 99%, more preferably from about 25% to about 99%, and most preferably from about 50% to about 99% of the pharmaceutical cold active compo ⁇ nent.
• Liquid oral dosage forms preferably contain from about 0.001% to about 25% and more preferably from about 0.001% to about 10% and most preferably from about 0.01% to about 5% of the pharmaceutical cold active component.
• Tablets can be compressed, molded, triturated, enteric-coated, sugar-coated, film-coated or multiple compressed, containing suitable binders, lubricants, diluents, disintegrating agents, coloring agents, flavoring agents, preservatives and flow-inducing agents. Also useful are soft gelatin capsules.
• Liquid oral dosage forms include aqueous and nonaqueous solu ⁇ tions, emulsions, pseudo emulsions, suspensions, and solutions and/or suspensions reconstituted from non-effervescent granules, containing suitable solvents, preservatives, emulsifying agents, suspending agents, diluents, sweeteners, coloring agents, and flavoring agents.
• suitable solvents preservatives, emulsifying agents, suspending agents, diluents, sweeteners, coloring agents, and flavoring agents.
• typical liquid formulations preferably contain a co-solvent, for example, propylene glycol, polyethylene glycol, alcohol, glycerin, sorbitol solution and the like, to assist solubili- zation and incorporation of water-insoluble ingredients, such as flavoring oils and the like into the composition.
• a co-solvent for example, propylene glycol, polyethylene glycol, alcohol, glycerin, sorbitol solution and the like, to assist solubili- zation and incorporation of water-insoluble ingredients, such as flavoring oils and the like into the composition.
• ingredients well known to the pharmacist's art may also be included in amounts generally known for these ingredients, for example, natural or artificial sweeteners, flavoring agents, colorants and the like to provide a palatable and pleasant looking final prod ⁇ uct, antioxidants, for example, butylated hydroxy anisole or butylated hydroxy toluene, and preservatives, for example, methyl or propyl paraben, potassium sorbate, or sodium benzoate, to prolong and enhance shelf life.
• natural or artificial sweeteners for example, butylated hydroxy anisole or butylated hydroxy toluene
• preservatives for example, methyl or propyl paraben, potassium sorbate, or sodium benzoate
• a preferred optional component is also materials other than MPD having cooling properties, such as menthol and menthol-like compounds such as N-ethyl-p-menthane-3-carboxamide (preferably at from about 0.001% to about 5%, more preferably from about 0.001% to about 0.5%), and mixtures thereof.
• a preferred optional component is also caffeine.
• the present invention also relates to a method for treating cough, cold, cold-like, allergy and flu symptoms in a human or lower animal.
• Said method comprises administering to a human or lower animal in need of such treatment, by oral or nasal administration, a composition comprising MPD.
• Preferred pharmaceutical compositions for administration according to the present invention method comprise from about 0.001% to about 10% (preferably from about 0.01% to about 0.5%) of MPD, and from about 0.1% to about 99.999% (preferably from about 70%-to about 99.99%) of-pharmaceutically-acceptable carrier material(s).
• Preferred is administering, either orally or nasally, a safe and effective amount of a composition according to the present invention. Most preferred is oral administration.
• This composition is prepared by first dissolving the dextromethor- phan and glyceryl guaiacolate in alcohol and then adding with constant mixing the menthol, MPD and WS-3. In separate containers dissolve the sucrose in a small portion of the water, dissolve the coloring agent in a separate small portion of the water, and in still another con ⁇ tainer dissolve the sodium citrate and citric acid in a small portion of the water. Finally, all the premixes and the remaining water are mixed with constant mixing to prepare a composition of the present invention having 20 mg of dextromethorphan and 200 mg of glyceryl guaiacolate per 15 ml of composition.
• Administration by sucking of drops to a human patient having a cough- associated with the common cold provides rapid, long lasting relief of the cough in said human patient.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Epidemiology (AREA)
• General Chemical & Material Sciences (AREA)
• Rheumatology (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Pain & Pain Management (AREA)
• Engineering & Computer Science (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines Containing Plant Substances (AREA)

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Cited By (27)

Citations (2)

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• 1993
  • 1993-09-22 CA CA002146637A patent/CA2146637C/en not_active Expired - Fee Related
  • 1993-09-22 NZ NZ256346A patent/NZ256346A/en unknown
  • 1993-09-22 AU AU49307/93A patent/AU678561B2/en not_active Ceased
  • 1993-09-22 JP JP6510004A patent/JPH08502288A/ja active Pending
  • 1993-09-22 EP EP93921692A patent/EP0662840A1/en not_active Withdrawn
  • 1993-09-22 WO PCT/US1993/008887 patent/WO1994008551A2/en not_active Application Discontinuation
  • 1993-10-08 MX MX9306295A patent/MX9306295A/es not_active IP Right Cessation

Patent Citations (2)

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