WO2003068206A1 - Pharmaceutical compositions comprising terbutaline or salbutamol in combination with guaiphenesine - Google Patents
Pharmaceutical compositions comprising terbutaline or salbutamol in combination with guaiphenesine Download PDFInfo
- Publication number
- WO2003068206A1 WO2003068206A1 PCT/IB2003/000475 IB0300475W WO03068206A1 WO 2003068206 A1 WO2003068206 A1 WO 2003068206A1 IB 0300475 W IB0300475 W IB 0300475W WO 03068206 A1 WO03068206 A1 WO 03068206A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- pharmaceutically acceptable
- terbutaline
- salbutamol
- combination
- antihistamine
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K31/075—Ethers or acetals
- A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
- A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
Definitions
- THIS invention relates to pharmaceutical compositions and their use in the symptomatic relief of cough and flu.
- Cough is a common symptom of coryza (common cold), croup, tracheobronchitis, pneumonia and influenza.
- the cause of the underlying disease is usually viral in origin however primary or secondary bacteria infections may arise. The majority of viral cases can be treated symptomatically.
- Symptomatic therapy with the co-administration of antibiotics is used to treat patients with bacteria or mixed infections.
- Cough is a protective reflex that can expel secretions, exudates, transudates or extraneous materials from the respiratory tract.
- the mechanism of cough is complex. A number of treatment options are available depending on whether the cough is productive in nature or not. When a cough is productive, it should rarely be suppressed (unless it is preventing rest, sleep or is exhausting the patient).
- the pharmacologically treatment of a productive cough usually makes use of one or more classes of drugs used alone or in combination. Expectorants, demulcents, decongestants, antihistamines, bronchodilators and mucolytics are frequently used.
- a pharmaceutical composition comprises a combination of (i) a bronchodilator selected from salbutamol and terbutaline, and pharmaceutically acceptable salts or derivatives thereof, and (ii) guaiphenesin, or a pharmaceutically acceptable salt or derivative thereof, and a pharmaceutically acceptable carrier.
- a pharmaceutical composition comprises a combination of (i), (ii) and (iii) an antihistamine, or a pharmaceutically acceptable salt or derivative thereof, and a pharmaceutically acceptable carrier.
- the invention extends to the use of either combination in a method of providing symptomatic relief of cough and/or flu, in particular that associated with bronchoconstriction and mucous production.
- the invention also extends to the use of a combination of (i) and (ii), or of (i), (ii) and (iii), in the manufacture of a medicament for use in treating or preventing cough and/or flu.
- the invention also extends to a method of treating or preventing cough and/or flu, comprising administering to a patient in need thereof a combination of (i) and (ii), or of (i), (ii) and (iii).
- a method of treating or preventing cough and/or flu comprising administering to a patient in need thereof a combination of (i) and (ii), or of (i), (ii) and (iii).
- compositions of the invention are suitable for the symptomatic relief of cough and/or flu, including but not limited to that associated with bronchoconst ction and excessive mucous production. They can also be used in the treatment or prevention of these illnesses.
- the first ingredient is a bronchodilator selected from salbutamol and terbutaline, and pharmaceutically acceptable salts or derivatives thereof.
- Salbutamol which is typically provided as its sulphate salt, is a direct- acting symphathomimetic agent with predominantly beta-ad renergic activity and a selective action on beta 2 receptors. It is a bronchodilator indicated for conditions which result in bronchoconstriction, and is used mostly in the treatment of bronchial asthma.
- the salbutamol is provided in the composition in an amount such that the daily dose thereof is typically in the range of about 1 mg to about 30 mg, preferably about 4 mg to about 16 mg, expressed in terms of salbutamol base.
- Terbutaline which is also typically provided as its sulphate salt, is also a direct-acting sympathomimetic agent with actions and uses similar to those of salbutamol. It is also used in the treatment of bronchial asthma.
- the terbutaline is provided in the composition in an amount such that the daily dose of the terbutaline active ingredient is typically in the range of about 0.5 mg to about 5 mg given orally every 8 hours, preferably about 1.0 mg to about 3 mg, expressed in terms of terbutaline base.
- the second ingredient is guaiphenesin or a pharmaceutically acceptable salt or derivative thereof. It is an expectorant that is reported to reduce the viscosity of tenacious sputum and is indicated for productive coughs.
- the guaiphenesin is provided in the composition in an amount such that the daily dose thereof is typically in the range of about 50 mg to about 3500 mg, preferably about 200 mg to about 1600 mg.
- a pharmaceutical composition comprising a combination of the above two ingredients includes a pharmaceutically acceptable carrier and may include other necessary non-active excipients such as, for example, sorbitol, sucrose, water, alcohol, citric acid propylene glycol, polyethylene glycol, and xanthan gum.
- the pharmaceutical composition may be provided in any appropriate dosage form such as, for example, tablets, capsules, granules, suspensions, solutions or other liquid forms, and is intended for oral or intravenous administration.
- Such a pharmaceutical composition is provided for the symptomatic relief of cough, including but not limited to that associated with bronchoconstriction and mucous production.
- the dosage form will typically be administered to a patient from 1 to 6 times per day.
- a further pharmaceutical composition of the invention includes the abovementioned two active ingredients in combination with a suitable antihistamine or a pharmaceutically acceptable salt or derivative thereof.
- Antihistamines dry up excessive mucous and some have a cough suppressant effect.
- suitable antihistamines include diphenhydramine, chlorpheniramine, diphenylpyraline, dexchlorpheniramine, loratidine and cetirizine. Particularly preferred are diphenhydramine and diphenylpyraline.
- the daily dose of the antihistamine will depend on the particular active ingredient chosen.
- the daily dose is typically in the range of about 3.5 mg to about 200 mg, preferably about 7 mg to about 170 mg.
- diphenylpyraline When diphenylpyraline is incorporated into the pharmaceutical composition of the invention its daily dose is in the range of about 0.5 mg to about 50 mg, preferably about 1.25 mg to about 30 mg.
- a pharmaceutical composition comprising all three active ingredients in combination includes a pharmaceutically acceptable carrier and may also include other non-active excipients. It may be provided in any appropriate dosage form such as, for example, tablets, capsules, granules, suspensions, solutions or other liquid forms, and is intended for oral or intravenous administration.
- the pharmaceutical composition is provided for the symptomatic relief of cough and flu, including but not limited to that associated with bronchoconstriction and excessive mucous production.
- the dosage form will typically be administered to a patient from 1 to 6 times per day.
- Guaiphenesin produces its anti-tussive effect by decreasing the viscosity of bronchial secretions, thereby facilitating their removal.
- Expectorants of this type increase the amount of respiratory tract fluid, exerting a demulcent action on the mucosal lining.
- the effects of bronchospasm are rapidly reversed by the action of bronchodilators.
- the antihistamines are intended to suppress the cough reflex, dry excess secretions and in some cases may produce sedation which will assist in the patient's rest and sleep patterns.
- Combinations of each of the active ingredients were combined with acceptable pharmaceutical carriers, including formulations as shown in the above examples, and were exposed to International Conference of Harmonization (ICH) Stability Test conditions. Samples thereof were assayed by High Pressure Liquid Chromatographic (HPLC) methods. The samples complied with the tested parameters up to a period of 6 months.
- ICH International Conference of Harmonization
- each of the active ingredients is provided in a therapeutic amount, it is envisaged that one or more of the ingredients may be provided in sub-therapeutic amounts, provided that the pharmaceutical composition is therapeutic.
Landscapes
- 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)
- Emergency Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
Claims
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
AU2003205974A AU2003205974A1 (en) | 2002-02-13 | 2003-02-13 | Pharmaceutical compositions comprising terbutaline or salbutamol in combination with guaiphenesine |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ZA2002/1244 | 2002-02-13 | ||
ZA200201244 | 2002-02-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2003068206A1 true WO2003068206A1 (en) | 2003-08-21 |
Family
ID=27735422
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/IB2003/000475 WO2003068206A1 (en) | 2002-02-13 | 2003-02-13 | Pharmaceutical compositions comprising terbutaline or salbutamol in combination with guaiphenesine |
Country Status (2)
Country | Link |
---|---|
AU (1) | AU2003205974A1 (en) |
WO (1) | WO2003068206A1 (en) |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB2424185B (en) * | 2005-03-16 | 2009-12-30 | Atulkumar Sumanbhai Patel | A cough mixture |
WO2011027248A1 (en) * | 2009-09-03 | 2011-03-10 | Sulur Subramaniam Vanangamudi | Oral liquid formulation comprising salbutamol and guaifenesin |
EP2808010A1 (en) * | 2013-05-28 | 2014-12-03 | Sanovel Ilac Sanayi ve Ticaret A.S. | Syrup Formulation of Salbutamol |
US10105324B2 (en) * | 2015-11-13 | 2018-10-23 | Sovereign Pharmaceuticals, Llc | Immediate release oral guaifenesin solution |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1996035452A1 (en) * | 1995-05-10 | 1996-11-14 | Adcock Ingram Limited | Pharmaceutical composition containing acetylcysteine, carbocysteine or erdosteine in combination with a beta 2 agonist and an expectorant for the treatment of respiratory tract disorders |
-
2003
- 2003-02-13 AU AU2003205974A patent/AU2003205974A1/en not_active Abandoned
- 2003-02-13 WO PCT/IB2003/000475 patent/WO2003068206A1/en not_active Application Discontinuation
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1996035452A1 (en) * | 1995-05-10 | 1996-11-14 | Adcock Ingram Limited | Pharmaceutical composition containing acetylcysteine, carbocysteine or erdosteine in combination with a beta 2 agonist and an expectorant for the treatment of respiratory tract disorders |
Non-Patent Citations (4)
Title |
---|
BIANCHI A ET AL: "Clinical and physiopathological results of a bronchodynamic mucolytic association, RG 089/12, in bronchopneumopathic patients", GAZZETTA MEDICA ITALIANA 1976, vol. 135, no. 7-8, 1976, pages 386 - 392, XP009010537 * |
BUNDESVERBAND DER PHARMAZEUTISCHEN INDUSTRIE (EDITOR): "Rote Liste 1985", 1985, EDITIO CANTOR, AULENDORF, XP002240394 * |
GRUBER W ET AL: "Symptomatic therapy for coughing in colds. An analysis of controlled studies", MONATSSCHRIFT FUR KINDERHEILKUNDE 2000 GERMANY, vol. 148, no. 2, 2000, pages 156 - 164, XP002240393, ISSN: 0026-9298 * |
PEDROZA MELENDEZ A: "A mucolytic-bronchodilator association in the treatment of hypersecretory asthmatic bronchitis in children", INVESTIGACION MEDICA INTERNACIONAL 1988 MEXICO, vol. 15, no. 3, 1988, pages 162 - 168, XP001148025, ISSN: 0185-2108 * |
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB2424185B (en) * | 2005-03-16 | 2009-12-30 | Atulkumar Sumanbhai Patel | A cough mixture |
WO2011027248A1 (en) * | 2009-09-03 | 2011-03-10 | Sulur Subramaniam Vanangamudi | Oral liquid formulation comprising salbutamol and guaifenesin |
CN102573796A (en) * | 2009-09-03 | 2012-07-11 | 苏鲁·苏布拉马尼·瓦南加穆迪 | Oral liquid preparation containing salbutamol and guaifenesin |
EP2808010A1 (en) * | 2013-05-28 | 2014-12-03 | Sanovel Ilac Sanayi ve Ticaret A.S. | Syrup Formulation of Salbutamol |
WO2014191414A1 (en) * | 2013-05-28 | 2014-12-04 | Sanovel Ilac Sanayi Ve Ticaret A.S. | Syrup formulation of salbutamol |
US10105324B2 (en) * | 2015-11-13 | 2018-10-23 | Sovereign Pharmaceuticals, Llc | Immediate release oral guaifenesin solution |
Also Published As
Publication number | Publication date |
---|---|
AU2003205974A1 (en) | 2003-09-04 |
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