CA2146637C - Pharmaceutical compositions and methods for treating cold symptoms - Google Patents
Pharmaceutical compositions and methods for treating cold symptoms Download PDFInfo
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- CA2146637C CA2146637C CA002146637A CA2146637A CA2146637C CA 2146637 C CA2146637 C CA 2146637C CA 002146637 A CA002146637 A CA 002146637A CA 2146637 A CA2146637 A CA 2146637A CA 2146637 C CA2146637 C CA 2146637C
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- cold
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- 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
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- 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]
Abstract
Pharmaceutical compositions comprising a safe and effective amount of at least one pharmaceutical cold active; 3-1-menthoxy propane 1,2-diol; and a pharmaceutically-acceptable carrier material suitable for oral or nasal administration. The present invention also includes methods for treating cough, cold, cold-like, allergy and/or 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.
Description
WO 94/08551 ~ ~ ~ 6 ~ , ~ PCT/US93/08887 PHARMACEUTICAL COMPOSITIONS AND METHODS
FOR TREATING COLD SYMPTOMS
BACKGROUND OF THE INVENTION
The present invention relates to orally or nasally administrable 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). 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.
Pharmaceutical compositions safe and effective for treating colds, flu, and allergies are well known. Over-the-counter medica 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.
It is an object of the present invention to provide 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.
These and other objects of the present invention will become WO 94/08551 PCT/US93/0888', _p_ readily apparent from the detailed description which follows.
All percentages and ratios used herein are by weight, and all measurements are made at 25'C, unless otherwise specified.
SUMMARY OF THE INVENTION
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.
~FTAILED DESCRIPTION OF THE INVENTION
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. The components of the compositions according to the present invention, and representative amounts, as well as the present invention methods are described in detail as follows.
Pharmaceutical Cold Actives:
The pharmaceutical compositions according to the present inven tion comprise pharmaceutical cold actives useful for treating cough, cold, cold-like, allergy and/or flu symptoms. Such 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.
The 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, fominoben, their pharmaceutically-acceptable salts; an expec-torant or mucolytic such as glyceryl guaiacolate, terpin hydrate, ammonium chloride, N-acetylcysteine and bromhexine, ambroxol, their pharmaceutically-acceptable salts; and an antihistamine such as chlorpheniramine, brompheniramine, dexchlorpheniramine, dexbromphreniramine, triprolidine, azatadine, doxylamine, tripelennamine, cyproheptadine, hydroxyzine, clemastine, carbinoxamine, phenindamine> bromodiphenhydramine, pyrilamine, their pharmaceutically-acceptable salts, as well as the non-sedating antihistamines which include acrivastine, AHR-11325, astemizole, azelastine, cetirizine, ebastine, ketotifen, lodoxamide> loratidine, levocabastine, mequitezine> oxatomide, setastine, tazifylline, temelastine, and terfenadine, their pharmaceutically-acceptable salts: all of these components, as well as their acceptable dosage ranges are described in the following: U.S. 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.
Also useful are bronchodilators such as terbutaline, atropine, aminophylline, epinephrine, isoprenaline, metaproterenol, bitoterol, theophylline and albuterol. Also used are analgesic compounds such as acetylsalicylic acid, acetaminophen, ibuprofen, and naproxen; and topical anesthetics/analgesics such as phenol, benzocaine, hexyl resorcinol, and dyclonine.
The compositions of the present invention comprise a safe and effective amount of at least one pharmaceutical cold active. The phrase "safe and effective amount", as used herein, means an amount of a compound or composition high enough when administered orally or nasally 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 pharmaceutically-acceptable carrier utilized, and like factors within the knowledge and expertise of the attending physician. Typically, the pharmaceutical cold actives) comprise from about 0.001 to about 99.9, by weight, of the pharmaceutical compositions of the present invention, preferably from about O.OOli to about 75i> and most preferably from about 0.01 to about 30%.
i. ;
21~ss3~
3-1-Menthoxy Propane 1 2-Diol:
The pharmaceutical compositions of the present invention also comprise 3-1-menthoxy propane 1,2-diol ("MPD"). This material is described in detail in U.S. Patent 4,459.425, issued July 10, 1984 to Amano et. al.
Whi 1 a not to be 1 i mi ted by theory, i t i s bel i eyed that the benefi is obtai ned by the use of MPD i n the composi ti ons of the present i nventi on are the resul t of the uni que cool i ng profi 1 a for thi s compound . MPD i s commerci al 1 y 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, preferably from about 0.01% to about 5%, and most preferably from about 0.01% to about 0.5%.
Pharmaceutically-Acc~~table Carrier Material' The term "pharmaceutically-acceptable carrier materials", as used herein, 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. The term "compatible", as used herein, means that the components of the compositions 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 situations. 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.
The choice of pharmaceutically-acceptable carrier materials to be used in conjunction with the pharmaceutical cold active of the present compositions is basically determined by the dose form for the compositions.
The preferred dosage forms are liquid solutions, liquid suspensions, tablets, capsules and the like, comprising a safe and effective amount of the pharmaceutical actives. Pharmaceutically-acceptable carrier materials suitable for the preparation of dosage forms for oral and nasal (e. g., nasal sprays) administration are well-known in the art. Their selection will depend on secondary considerations like taste, cost, shelf stability, which are not critical for the purposes of the present invention, and can be made without difficulty by a person skilled in the art. Preferably the present invention compositions comprise from about 0.1% to about 99.99% of one or more pharmaceutically-acceptable carrier materials.
t,., 2146637_ Various oral dosage forms can be used, including such solid forms as tablets, capsules, granules, lozenges and bulk powders and liquid forms such as syrups and suspensions. These oral forms comprise a safe and effective amount of the pharmaceutical cold active component. 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 component. 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.
Techniques and compositions for making solid oral dosage forms are described in Marshall, "Solid Oral Dosage Forms," Modern Pharmaceutics.
Vol. 7. (Banker and Rhodes, editors), 359-427 (1979). Techniques and compositions for making tablets (compressed and molded), capsules (hard and soft gelatin) and pills are described in Remington's Pharmaceutical Sciences (Arthur Osol, editor). 1553-1593 (1980).
Liquid oral dosage forms include aqueous and nonaqueous solutions, 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. Specific examples of pharmaceutically-acceptable carriers and excipients that may be used to formulate oral dosage forms, are described in U.S. Patent 3,903.297, Robert, issued September 2, 1975. Although water itself may make up the entire carrier, typical liquid formulations preferably contain a co-solvent, for example, propylene glycol, polyethylene glycol, 4 .:
WO 94/08551 1 ~ s s ~ 7 » PCT/US93/0888' 4~
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.
Other optional 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 1 i ke to provide a pal atabl a and pl easant 1 ooki ng fi nal 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. 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 5f., more preferably from about 0.001% to about 0.5%), and mixtures thereof. A preferred optional component is also caffeine.
Method of Treatment:
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 0.5Ye) of MPD, and from about 0.1% to about 99.999% (preferably from about 709:-.to about 99.99%) of~harmaceutically-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.
The following examples further describe and demonstrate embodi-ments within the scope of the present invention. These examples are given solely for the purpose of illustration and are not to be con-strued as a limitation of the present invention as many variations thereof are possible without departing from the spirit and scope.
Example 1 - Couah Svrup Ingredient Amount/15m1 dose Dextromethorphan HBr 20 mg Glyceryl Guaiacolate 200 mg ~21 46 fi37 ~.~ WO 94/08551 PGT/US93/08887 _7_ Sucrose 8.16 grams Alcohol 1 ml .Citric Acid, Anydrous 4 mg Sodium Citrate 300 mg MPD1) 15 mg WS-32) 0.75 mg Menthol 7.5 mg Coloring Agent 4.5 mg Water, Purified Q.S. to 15 ml 1) 3-1-menthoxy propane 1, 2-diol, supplied by Takasago Perfumery Co., Ltd., Tokyo, Japan 2) N-ethyl-p-menthane-3-carboxamide, supplied by Sterling Drugs This composition is prepared.by first dissolving the dextromethor-phan and glyceryl guaiacolate in alcohol and then adding with constanx mixing the menthol, MPD and WS-3. In separate containers dissolve the sucrose in a small portion of the water, dissolve the coloring agent i n a separate smal 1 part i on of the water, and i n st i 11 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 drinking 15 ml) of this composition to a human patient having a cough associated with the common cold provides rapid, long-lasting relief of t-he cough in said human patient.
Example 2 - Couqh Droe % Composition Ingredient (y W/WJi Menthol, Natural 0.2211 Eucalyptus Oil 0.1455 MPD 0.0700 WS-3 0.0300 FD&C Blue ~1 0.0022 Sugar QS*
Low DE Corn Syrup QS*
*60/40 Sugar/Low DE Corn Syrup (before cook); candy base used.
2~4s.s3~
WO 94/08551 PCT/US93/0888' _g_ This composition is prepared by standard drop forming techniques.
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.
FOR TREATING COLD SYMPTOMS
BACKGROUND OF THE INVENTION
The present invention relates to orally or nasally administrable 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). 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.
Pharmaceutical compositions safe and effective for treating colds, flu, and allergies are well known. Over-the-counter medica 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.
It is an object of the present invention to provide 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.
These and other objects of the present invention will become WO 94/08551 PCT/US93/0888', _p_ readily apparent from the detailed description which follows.
All percentages and ratios used herein are by weight, and all measurements are made at 25'C, unless otherwise specified.
SUMMARY OF THE INVENTION
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.
~FTAILED DESCRIPTION OF THE INVENTION
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. The components of the compositions according to the present invention, and representative amounts, as well as the present invention methods are described in detail as follows.
Pharmaceutical Cold Actives:
The pharmaceutical compositions according to the present inven tion comprise pharmaceutical cold actives useful for treating cough, cold, cold-like, allergy and/or flu symptoms. Such 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.
The 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, fominoben, their pharmaceutically-acceptable salts; an expec-torant or mucolytic such as glyceryl guaiacolate, terpin hydrate, ammonium chloride, N-acetylcysteine and bromhexine, ambroxol, their pharmaceutically-acceptable salts; and an antihistamine such as chlorpheniramine, brompheniramine, dexchlorpheniramine, dexbromphreniramine, triprolidine, azatadine, doxylamine, tripelennamine, cyproheptadine, hydroxyzine, clemastine, carbinoxamine, phenindamine> bromodiphenhydramine, pyrilamine, their pharmaceutically-acceptable salts, as well as the non-sedating antihistamines which include acrivastine, AHR-11325, astemizole, azelastine, cetirizine, ebastine, ketotifen, lodoxamide> loratidine, levocabastine, mequitezine> oxatomide, setastine, tazifylline, temelastine, and terfenadine, their pharmaceutically-acceptable salts: all of these components, as well as their acceptable dosage ranges are described in the following: U.S. 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.
Also useful are bronchodilators such as terbutaline, atropine, aminophylline, epinephrine, isoprenaline, metaproterenol, bitoterol, theophylline and albuterol. Also used are analgesic compounds such as acetylsalicylic acid, acetaminophen, ibuprofen, and naproxen; and topical anesthetics/analgesics such as phenol, benzocaine, hexyl resorcinol, and dyclonine.
The compositions of the present invention comprise a safe and effective amount of at least one pharmaceutical cold active. The phrase "safe and effective amount", as used herein, means an amount of a compound or composition high enough when administered orally or nasally 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 pharmaceutically-acceptable carrier utilized, and like factors within the knowledge and expertise of the attending physician. Typically, the pharmaceutical cold actives) comprise from about 0.001 to about 99.9, by weight, of the pharmaceutical compositions of the present invention, preferably from about O.OOli to about 75i> and most preferably from about 0.01 to about 30%.
i. ;
21~ss3~
3-1-Menthoxy Propane 1 2-Diol:
The pharmaceutical compositions of the present invention also comprise 3-1-menthoxy propane 1,2-diol ("MPD"). This material is described in detail in U.S. Patent 4,459.425, issued July 10, 1984 to Amano et. al.
Whi 1 a not to be 1 i mi ted by theory, i t i s bel i eyed that the benefi is obtai ned by the use of MPD i n the composi ti ons of the present i nventi on are the resul t of the uni que cool i ng profi 1 a for thi s compound . MPD i s commerci al 1 y 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, preferably from about 0.01% to about 5%, and most preferably from about 0.01% to about 0.5%.
Pharmaceutically-Acc~~table Carrier Material' The term "pharmaceutically-acceptable carrier materials", as used herein, 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. The term "compatible", as used herein, means that the components of the compositions 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 situations. 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.
The choice of pharmaceutically-acceptable carrier materials to be used in conjunction with the pharmaceutical cold active of the present compositions is basically determined by the dose form for the compositions.
The preferred dosage forms are liquid solutions, liquid suspensions, tablets, capsules and the like, comprising a safe and effective amount of the pharmaceutical actives. Pharmaceutically-acceptable carrier materials suitable for the preparation of dosage forms for oral and nasal (e. g., nasal sprays) administration are well-known in the art. Their selection will depend on secondary considerations like taste, cost, shelf stability, which are not critical for the purposes of the present invention, and can be made without difficulty by a person skilled in the art. Preferably the present invention compositions comprise from about 0.1% to about 99.99% of one or more pharmaceutically-acceptable carrier materials.
t,., 2146637_ Various oral dosage forms can be used, including such solid forms as tablets, capsules, granules, lozenges and bulk powders and liquid forms such as syrups and suspensions. These oral forms comprise a safe and effective amount of the pharmaceutical cold active component. 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 component. 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.
Techniques and compositions for making solid oral dosage forms are described in Marshall, "Solid Oral Dosage Forms," Modern Pharmaceutics.
Vol. 7. (Banker and Rhodes, editors), 359-427 (1979). Techniques and compositions for making tablets (compressed and molded), capsules (hard and soft gelatin) and pills are described in Remington's Pharmaceutical Sciences (Arthur Osol, editor). 1553-1593 (1980).
Liquid oral dosage forms include aqueous and nonaqueous solutions, 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. Specific examples of pharmaceutically-acceptable carriers and excipients that may be used to formulate oral dosage forms, are described in U.S. Patent 3,903.297, Robert, issued September 2, 1975. Although water itself may make up the entire carrier, typical liquid formulations preferably contain a co-solvent, for example, propylene glycol, polyethylene glycol, 4 .:
WO 94/08551 1 ~ s s ~ 7 » PCT/US93/0888' 4~
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.
Other optional 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 1 i ke to provide a pal atabl a and pl easant 1 ooki ng fi nal 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. 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 5f., more preferably from about 0.001% to about 0.5%), and mixtures thereof. A preferred optional component is also caffeine.
Method of Treatment:
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 0.5Ye) of MPD, and from about 0.1% to about 99.999% (preferably from about 709:-.to about 99.99%) of~harmaceutically-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.
The following examples further describe and demonstrate embodi-ments within the scope of the present invention. These examples are given solely for the purpose of illustration and are not to be con-strued as a limitation of the present invention as many variations thereof are possible without departing from the spirit and scope.
Example 1 - Couah Svrup Ingredient Amount/15m1 dose Dextromethorphan HBr 20 mg Glyceryl Guaiacolate 200 mg ~21 46 fi37 ~.~ WO 94/08551 PGT/US93/08887 _7_ Sucrose 8.16 grams Alcohol 1 ml .Citric Acid, Anydrous 4 mg Sodium Citrate 300 mg MPD1) 15 mg WS-32) 0.75 mg Menthol 7.5 mg Coloring Agent 4.5 mg Water, Purified Q.S. to 15 ml 1) 3-1-menthoxy propane 1, 2-diol, supplied by Takasago Perfumery Co., Ltd., Tokyo, Japan 2) N-ethyl-p-menthane-3-carboxamide, supplied by Sterling Drugs This composition is prepared.by first dissolving the dextromethor-phan and glyceryl guaiacolate in alcohol and then adding with constanx mixing the menthol, MPD and WS-3. In separate containers dissolve the sucrose in a small portion of the water, dissolve the coloring agent i n a separate smal 1 part i on of the water, and i n st i 11 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 drinking 15 ml) of this composition to a human patient having a cough associated with the common cold provides rapid, long-lasting relief of t-he cough in said human patient.
Example 2 - Couqh Droe % Composition Ingredient (y W/WJi Menthol, Natural 0.2211 Eucalyptus Oil 0.1455 MPD 0.0700 WS-3 0.0300 FD&C Blue ~1 0.0022 Sugar QS*
Low DE Corn Syrup QS*
*60/40 Sugar/Low DE Corn Syrup (before cook); candy base used.
2~4s.s3~
WO 94/08551 PCT/US93/0888' _g_ This composition is prepared by standard drop forming techniques.
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.
Claims (13)
1. A pharmaceutical composition comprising:
(a) at least one pharmaceutical cold active;
(b) 3-1-menthoxy propane-1,2-diol; and (c) pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
(a) at least one pharmaceutical cold active;
(b) 3-1-menthoxy propane-1,2-diol; and (c) pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
2. The pharmaceutical composition according to Claim 1 wherein the pharmaceutical cold active is selected from the group consisting of analgesics, anti-inflammatories, anesthetics, antihistamines, decongestants, cough suppressants, demulcents, antitussives, expectorants, and mixtures thereof.
3. The pharmaceutical composition according to Claim 2 wherein the pharmaceutical cold active is selected from the group consisting of pseudoephedrine, phenylpropanolamine, phenylephrine, ephedrine, dextromethorphan, chlophedianol, carbetapentane, caramiphen, noscapine, diphenhydramine, codeine, menthol, hydrocodone, hydromorphone, fominoben, glyceryl guaiacolate, terpin hydrate, ammonium chloride, N-acetylcysteine and bromhexine, ambroxol, chlorpheniramine, brompheniramine, dexchlorpheniramine, dexbromphreniramine, triprolidine, azatadine, doxylamine, tripelennamine, cyproheptadine, hydroxyzine, clemastine, carbinoxamine, phenindamine, bromodiphenhydramine, pyrilamine, acrivastine, AHR-11325, astemizole, azelastine, cetirizine, ebastine, ketotifen, lodoxamide, loratidine, levocabastine, mequitazine, oxatomide, setastine, tezifylline, temelastine, terfenadine, terbutaline, atropine, aminophylline, epinephrine, isoprenaline, metaproterenol, bitoterol, theophylline, albuterol, acetylsalicylic acid, acetaminophen, ibuprofen, naproxen, phenol, benzocaine, hexyl resorcinol, dyclonine, the pharmaceutically-acceptable salts thereof, and mixtures thereof.
4. The pharmaceutical composition according to Claim 1 comprising from about 0.001% to about 10% of 3-1-menthoxy propane 1,2-diol.
5. A pharmaceutical composition comprising:
(a) from about 0.001% to about 99.9% of at least one pharmaceutical cold active;
(b) from about 0.001% to about 10% of 3-1-menthoxy propane 1,2-diol; and (c) from about 0.1% to about 99.99% of pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
(a) from about 0.001% to about 99.9% of at least one pharmaceutical cold active;
(b) from about 0.001% to about 10% of 3-1-menthoxy propane 1,2-diol; and (c) from about 0.1% to about 99.99% of pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
6. The pharmaceutical composition according to Claim 5 wherein the pharmaceutical cold active is selected from the group consisting of analgesics, anti-inflammatories, anesthetics, antihistamines, decongestants, cough suppressants, demulcents, antitussives, expectorants, and mixtures thereof.
7. The pharmaceutical composition according to Claim 6 wherein the pharmaceutical cold active is selected from the group consisting of pseudoephedrine, phenylpropanolamine, phenylephrine, ephedrine, dextromethorphan, chlophedianol, carbetapentane, caramiphen, noscapine, diphenhydramine, codeine, menthol, hydrocodone, hydromorphone, fominoben, glyceryl guaiacolate, terpin hydrate, ammonium chloride, N-acetylcysteine and bromhexine, ambroxol, chlorpheniramine, brompheniramine, dexchlorpheniramine, dexbromphreniramine, triprolidine, azatadine, doxylamine, tripelennamine, cyproheptadine, hydroxyzine, clemastine, carbinoxamine, phenindamine, bromodiphenhydramine, pyrilamine, acrivastine, AHR-11325, astemizole, azelastine, cetirizine, ebastine, ketotifen, lodoxamide, loratidine, levocabastine, mequitazine, oxatomide, setastine, tezifylline, temelastine, terfenadine, terbutaline, atropine, aminophylline, epinephrine, isoprenaline, metaproterenol, bitoterol, theophylline, albuterol, acetylsalicylic acid, acetaminophen, ibuprofen, naproxen, phenol, benzocaine, hexyl resorcinol, dyclonine, the pharmaceutically-acceptable salts thereof, and mixtures thereof.
8. The pharmaceutical composition according to Claim 5 further comprising a material in addition to 3-1-menthoxy propane 1,2-diol having cooling properties.
9. The Pharmaceutical composition according to Claim 8 wherein the additional material having cooling properties is selected from menthol, N-ethyl-p-menthane-3-carboxamide, and mixtures thereof.
10. A pharmaceutical composition comprising:
(a) from about 0.01% to about 30% of at least one pharmaceutical cold active;
(b) from about 0.01% to about 0.5% 3-1-menthoxy propane 1,2-diol;
and (c) from about 70% to about 99.99% of pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
(a) from about 0.01% to about 30% of at least one pharmaceutical cold active;
(b) from about 0.01% to about 0.5% 3-1-menthoxy propane 1,2-diol;
and (c) from about 70% to about 99.99% of pharmaceutically-acceptable carrier material suitable for oral or nasal administration.
11. The pharmaceutical composition according to Claim 10 wherein the pharmaceutical cold active is selected from the group consisting of analgesics, anti-inflammatories, anesthetics, antihistamines, decongestants, cough suppressants, demulcents, antitussives, expectorants, and mixtures thereof.
12. The pharmaceutical composition according to Claim 11 wherein the pharmaceutical cold active is selected from the group consisting of pseudoephedrine, phenylpropanolamine, phenylephrine, ephedrine, dextromethorphan, chlophedianol, carbetapentane, caramiphen, noscapine, diphenhydramine, codeine, menthol, hydrocodone, hydromorphone, fominoben, glyceryl guaiacolate, terpin hydrate, ammonium chloride, N-acetylcysteine and bromhexine, ambroxol, chlorpheniramine, brompheniramine, dexchlorpheniramine, dexbromphreniramine, triprolidine, azatadine, doxylamine, tripelennamine, cyproheptadine, hydroxyzine, clemastine, carbinoxamine, phenindamine, bromodiphenhydramine, pyrilamine, acrivastine, AHR-11325, astemizole, azelastine, cetirizine, ebastine, ketotifen, lodoxamide, loratidine, levocabastine, mequitazine, oxatomide, setastine, tezifylline, temelastine, terfenadine, terbutaline, atropine, aminophylline, epinephrine, isoprenaline, metaproterenol, bitoterol, theophylline, albuterol, acetylsalicylic acid, acetaminophen, ibuprofen, naproxen, phenol, benzocaine, hexyl resorcinol, dyclonine, the pharmaceutically-acceptable salts thereof, and mixtures thereof.
13. The pharmaceutical composition according to Claim 10 further comprising from about 0.001% to about 5% of N-ethyl-p-menthane-3-carboxamide.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95501392A | 1992-10-09 | 1992-10-09 | |
| US955,013 | 1992-12-22 | ||
| PCT/US1993/008887 WO1994008551A2 (en) | 1992-10-09 | 1993-09-22 | Pharmaceutical compositions and methods for treating cold symptoms |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2146637C true CA2146637C (en) | 2001-02-13 |
Family
ID=25496254
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002146637A Expired - Fee Related CA2146637C (en) | 1992-10-09 | 1993-09-22 | Pharmaceutical compositions and methods for treating cold symptoms |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP0662840A1 (en) |
| JP (1) | JPH08502288A (en) |
| AU (1) | AU678561B2 (en) |
| CA (1) | CA2146637C (en) |
| MX (1) | MX9306295A (en) |
| NZ (1) | NZ256346A (en) |
| WO (1) | WO1994008551A2 (en) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2160874C (en) * | 1993-04-30 | 1999-05-11 | William Fletcher Beck | Nasal aromatic releasing compositions |
| WO1995025518A1 (en) * | 1994-03-18 | 1995-09-28 | Ciba-Geigy Ag | Aqueous solution of levocabastine for ophthalmic use |
| US5698181A (en) * | 1994-12-09 | 1997-12-16 | Warner-Lambert Company | Breath-freshening edible compositions comprising menthol and an N-substituted-P-menthane carboxamide and methods for preparing same |
| US5626831A (en) * | 1995-12-20 | 1997-05-06 | Van Moerkerken; Arthur | Method for relief and prevention of common cold, and compositions |
| US6469009B1 (en) | 1996-04-08 | 2002-10-22 | Ucb, S.A. | Pharmaceutical compositions for the treatment of rhinitis |
| US5891885A (en) * | 1996-10-09 | 1999-04-06 | Algos Pharmaceutical Corporation | Method for treating migraine |
| US6013632A (en) * | 1997-01-13 | 2000-01-11 | Emory University | Compounds and their combinations for the treatment of influenza infection |
| GB9707978D0 (en) * | 1997-04-21 | 1997-06-11 | Procter & Gamble | Throat soothing compositions |
| GB9707977D0 (en) * | 1997-04-21 | 1997-06-11 | Procter & Gamble | Centre filled confectionery |
| DE19814256A1 (en) * | 1998-03-31 | 1999-10-07 | Asta Medica Ag | Solid, fast-breaking cetirizine formulations |
| US6132758A (en) | 1998-06-01 | 2000-10-17 | Schering Corporation | Stabilized antihistamine syrup |
| MXPA04002066A (en) * | 2001-09-04 | 2005-02-17 | Techno Network Shinoku Co Ltd | Anti-influenza drugs. |
| DE60319685T2 (en) | 2002-04-04 | 2009-03-26 | Pfizer Products Inc., Groton | WELCOME COFFEE BAG |
| GB2389530B (en) | 2002-06-14 | 2007-01-10 | Cipla Ltd | Pharmaceutical compositions |
| WO2006034495A2 (en) * | 2004-09-23 | 2006-03-30 | Matias Jonathan R | Methods of using menthol propyleneglycol-carbonate and analogs thereof for producing anti-inflammatory and anti-angiogenic effects |
| US20070249727A1 (en) | 2006-04-21 | 2007-10-25 | The Proctor & Gamble Company | Compositions and kits useful for treatment of respiratory illness |
| US10022339B2 (en) | 2006-04-21 | 2018-07-17 | The Procter & Gamble Company | Compositions and methods useful for treatment of respiratory illness |
| AU2016219620B2 (en) * | 2006-04-21 | 2017-05-11 | The Procter & Gamble Company | Compositions and methods useful for treatment of respiratory illness |
| EP2714021A1 (en) * | 2011-02-02 | 2014-04-09 | Max Reynolds | Composition of monoterpenoids having bactericidal properties |
| US10195153B2 (en) | 2013-08-12 | 2019-02-05 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| CA2955229C (en) | 2014-07-17 | 2020-03-10 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| CA2964628A1 (en) | 2014-10-20 | 2016-04-28 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
| MX2020012233A (en) | 2018-05-16 | 2021-01-29 | Bayer Healthcare Llc | High concentration suspension formulation for cold and flu soft gel capsule medications. |
| CN112972439A (en) * | 2019-12-16 | 2021-06-18 | 南京亿华药业有限公司 | Yumei effervescent tablet and preparation method thereof |
| AU2021217209A1 (en) | 2020-02-03 | 2022-09-29 | Johnson & Johnson Consumer Inc. | A single layer chewable tablet comprising cetirizine |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1353381A (en) * | 1971-02-04 | 1974-05-15 | Wilkinson Sword Ltd | Substituted p-menthanes and compositions containing them |
| JPS5888334A (en) * | 1981-11-20 | 1983-05-26 | Takasago Corp | 3-l-menthoxypropane-1,2-diol |
| ATE128351T1 (en) * | 1991-04-04 | 1995-10-15 | Procter & Gamble | EDIBLE PHARMACEUTICAL COMPOSITIONS FOR TREATING DIGESTIVE TRACT PAIN. |
-
1993
- 1993-09-22 NZ NZ256346A patent/NZ256346A/en unknown
- 1993-09-22 WO PCT/US1993/008887 patent/WO1994008551A2/en not_active Application Discontinuation
- 1993-09-22 EP EP93921692A patent/EP0662840A1/en not_active Withdrawn
- 1993-09-22 AU AU49307/93A patent/AU678561B2/en not_active Ceased
- 1993-09-22 JP JP6510004A patent/JPH08502288A/en active Pending
- 1993-09-22 CA CA002146637A patent/CA2146637C/en not_active Expired - Fee Related
- 1993-10-08 MX MX9306295A patent/MX9306295A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| AU4930793A (en) | 1994-05-09 |
| EP0662840A1 (en) | 1995-07-19 |
| WO1994008551A2 (en) | 1994-04-28 |
| NZ256346A (en) | 1997-04-24 |
| WO1994008551A3 (en) | 1994-06-23 |
| AU678561B2 (en) | 1997-06-05 |
| MX9306295A (en) | 1994-04-29 |
| JPH08502288A (en) | 1996-03-12 |
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