CN1253508A - Topical nasal antiinflammatory compositions - Google Patents
Topical nasal antiinflammatory compositions Download PDFInfo
- Publication number
- CN1253508A CN1253508A CN98804579A CN98804579A CN1253508A CN 1253508 A CN1253508 A CN 1253508A CN 98804579 A CN98804579 A CN 98804579A CN 98804579 A CN98804579 A CN 98804579A CN 1253508 A CN1253508 A CN 1253508A
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- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
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- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The present invention provides topically applicable nasal compositions comprising a therapeutically effective amount of an antiinflammatory agent and a therapeutically effective amount of at least one agent selected from the group consisting of a vasoconstrictor, a neuramidinase inhibitor, a leukotriene inhibitor, an antihistamine, an antiallergic agent, an anticholinergic agent, an anesthetic and a mucolytic agent. The present compositions are useful as nasal sprays and nose drops for the treatment of nasal and sinus conditions.
Description
Background of invention
In the treatment field of nasal mucosa inflammation, particularly at nose and sinus part disease, alleviate as symptoms of rhinitis, the topical nasal antiinflammatory preparation is known.But, nose and sinus part disease can be to be feature with changeable symptom, need treat with the combination therapy agent.For example, allergic rhinitis can be to be feature with rhinorrhea, rhinocnesmus, sneeze, hyperemia and postnasal drip, therefore except antiinflammatory, also can need hydryllin, Decongestant, antiabnormal reaction agent and narcotic treatment.
Use multiple local nasal formulations to give multiple therapeutic agent and have distinct disadvantage.The liquid volume of nose medication is subjected to the restriction of the bioadhesive of nostril surface area and liquid effectively.In addition, need fully contacting between topical formulations and the nostril surface area, to guarantee enough therapeutic agent dosages.And spray needs the threshold surface tension to form droplet.Therefore, the release volume of each operation only limits to be retained in the nostril not by too early effusive volume.So multiple local nasal formulations administration simultaneously effectively.
Another shortcoming of multiple local nasal formulations administration is to make the patient feel inconvenience.The inconvenience in medication of multiple spray product or nasal drop can make patient's compliance have a greatly reduced quality.Patient's complaint, excessive spray flows into their throat, and can discover taste, thereby needs correctives to cover the bitterness medicine.
Therefore, exist needs to the convenient manner that is used for multiple therapeutic agent nose administration.
Summary of the invention
But the invention provides the nasal composition of local application, it comprises local anti-inflammatory agent for the treatment of effective dose and at least a medicament that is applicable to local nose administration for the treatment of effective dose, and it is selected from the group of being made up of vasoconstrictor, neuraminidase inhibitor, anticholinergic, leukotriene inhibitors, hydryllin, antiabnormal reaction agent, anesthetis and mucolytic agent.
Detailed description of the invention
But the invention provides the nasal composition of local application, it comprises local anti-inflammatory agent and at least a other therapeutic agent.Said composition can be used for treating nose and sinus part disease, for example allergic rhinitis or flu.
Local anti-inflammatory agent in the present composition is the corticosteroid of inflammation-inhibiting known in the art.A kind of preferred embodiment in, the local anti-inflammatory agent is beclomethasone dipropionate, budesonide, dexamethasone, mometasone furoate, Fluticasone Propionate or triamcinolone acetonide.Compositions contains the antiinflammatory of the selection for the treatment of effective dose.Those of ordinary skill in the art can determine to treat the amount of effective inflammation-inhibiting.Accurate amount will depend on medication and curee's age, body weight and situation.Usually, the consumption of antiinflammatory is known in the art, is effective on the therapeutics when nose administration.
The present composition further comprises at least a other therapeutic agent, thereby makes antiinflammatory and the administration expediently in single local nasal composition of at least a other therapeutic agent.Other therapeutic agent is applicable to local nose administration, is selected from the group of being made up of vasoconstrictor, neuraminidase inhibitor, leukotriene inhibitors, anticholinergic, hydryllin, antiabnormal reaction agent, local anesthetic and mucolytic agent.Other therapeutic agent provides adduction and synergism with being used in combination of antiinflammatory in the treatment of nose and sinus part disease.
The vasoconstrictor that is applicable to local nose administration in the present composition is oxymetazoline, naphazoline, xylometazoline and phenylephrine.Leukotriene inhibitors comprises Zha Fulunsite (zafirlukast), and it is the selectivity of three kinds of leukotriene Cs, D4 and E4, competitive receptor antagonist; Pu Lunsite, it is the selectivity of D4, competitive receptor antagonist; And Zileuton, it is a leukotriene inhibitors.Neuraminidase inhibitor comprises Zha Namiwa (zanamivir) (GG-167).The hydryllin that is suitable for comprises that diphenhydramine, chlorphenamine, cetirizine, terfenadine, Fei Nuofending (fenofexadine), astemizole, norastemizole, nitrogen Si fourth and A Zha are for fourth (azatidine).Antiabnormal reaction agent comprises sodium cromoglicate, Nedocromil and Levocabastine.The anticholinergic that can be used for the present composition is an atrovent.Local anesthetic comprises dyclonine, pramocaine and benzocaine.The mucolytic agent that is applicable to local nose administration is acetylcysteine, guaifenesin and carbocisteine (mucocysteine).According to the known application of these medicaments, and consideration medication and curee's age, body weight and situation, the above-mentioned medicament of treatment effective dose can be determined by those of ordinary skill.
The present composition is mixed with aqueous solution, wherein comprises antiinflammatory and at least a other therapeutic agent, further comprise pharmaceutically acceptable nose carrier.Drug combination preparation is normally known in the art, and reference standard textbook easily, " Remington pharmaceutical science " 1985 the 17th editions for example, Mack Publishing Co., Easton, Pennsylvania.
Preferred nasal formulations is nasal drop or nasal spray, contains the buffered aqueous solution of water as carrier.Compositions is preferably isoosmotic.Isotonic agent is known in the art, and for example saccharide and sodium chloride can be included in the said composition.
The present composition also can contain wetting agent, is used for increasing viscosity, moisturizes and the cilium vigor.The wetting agent that is suitable for comprises glycerol, Polyethylene Glycol, propylene glycol and composition thereof.
Additive is known in the art, comprises pharmaceutically acceptable antiseptic, stabilizing agent, correctives and pH regulator agent, also can be included in the present composition.
Another embodiment of the invention provides the compositions of preservative free, comprises antiinflammatory and at least a other therapeutic agent.Owing to reduced sensitivity, improved patient's acceptance, the compositions of preservative free is preferred.They can be made into unit dose or system, have prevented the pollution of solution in storage.
The present composition can be easily with dosage unit form to people's nose administration, to reach the therapeutical effect of required above-mentioned antiinflammatory and other therapeutic agent.Compositions can be with the dosage form administration of nasal spray or nasal drop.Nasal spray can provide in the mode of manual nose atomizing pump of squeeze bottle or metering administration, for example it is designed to discharge required dosage by spraying once or twice.Compositions also can for example be measured the pressure aerosol of administration with the mode administration of aerosol spray, wherein contains propellant, as halogenated hydrocarbon.
Claims (16)
1. but the nasal composition of local application, it comprises local anti-inflammatory agent for the treatment of effective dose and at least a medicament that is applicable to local nose administration for the treatment of effective dose, and it is selected from the group of being made up of vasoconstrictor, neuraminidase inhibitor, anticholinergic, leukotriene inhibitors, hydryllin, antiabnormal reaction agent, anesthetis and mucolytic agent.
2. the compositions of claim 1, wherein said local anti-inflammatory agent is selected from the group of being made up of beclomethasone dipropionate, budesonide, dexamethasone, mometasone furoate, Fluticasone Propionate and triamcinolone acetonide.
3. the compositions of claim 1, wherein said vasoconstrictor is selected from the group of being made up of oxymetazoline, naphazoline, xylometazoline and phenylephrine.
4. the compositions of claim 1, wherein said hydryllin are selected from the group of being made up of for fourth diphenhydramine, chlorphenamine, terfenadine, nitrogen Si fourth, norastemizole, Fei Nuofending (fexofenadine), cetirizine, astemizole and A Zha.
5. the compositions of claim 1, wherein said antiabnormal reaction agent is selected from the group of being made up of sodium cromoglicate, Levocabastine and Nedocromil.
6. the compositions of claim 1, wherein said anticholinergic is an ipratropium bromide.
7. the compositions of claim 1, wherein said local anesthetic is selected from the group of being made up of dyclonine, pramocaine and benzocaine.
8. the compositions of claim 1, wherein said mucolytic agent is selected from the group of being made up of acetylcysteine, guaifenesin and carbocisteine.
9. the compositions of claim 1, wherein said leukotriene inhibitors is selected from the group of being made up of Zha Fulunsite, Pu Lunsite and Zileuton.
10. the compositions of claim 1, wherein said neuraminidase inhibitor is Zha Namiwa.
11. but the nasal composition of local application, it comprises the local anti-inflammatory agent for the treatment of effective dose, be selected from by beclomethasone dipropionate, budesonide, dexamethasone, mometasone furoate, the group that Fluticasone Propionate and triamcinolone acetonide are formed, also comprise at least a medicament for the treatment of effective dose, it is selected from by oxymetazoline, phenylephrine, diphenhydramine, chlorphenamine, terfenadine, astemizole, A Zha is for fourth, sodium cromoglicate, Nedocromil, atrovent, dyclonine, benzocaine, acetylcysteine, the group that guaifenesin and carbocisteine are formed.
12. the compositions of claim 1 or 11 further comprises at least a wetting agent.
13. the compositions of claim 12, wherein said wetting agent is selected from the group of being made up of glycerol, Polyethylene Glycol and propylene glycol.
14. the compositions of claim 1 or 11 comprises pharmaceutically acceptable carrier.
15. the compositions of claim 1 or 11 is mixed with the nasal spray medication.
16. the compositions of claim 1 or 11 is mixed with the nasal drop medication.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4430697P | 1997-04-30 | 1997-04-30 | |
| US60/044,306 | 1997-04-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1253508A true CN1253508A (en) | 2000-05-17 |
Family
ID=21931638
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN98804579A Pending CN1253508A (en) | 1997-04-30 | 1998-04-02 | Topical nasal antiinflammatory compositions |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP0979105A1 (en) |
| JP (1) | JP2001524108A (en) |
| CN (1) | CN1253508A (en) |
| AU (1) | AU6878098A (en) |
| BR (1) | BR9809022A (en) |
| CA (1) | CA2281789A1 (en) |
| IL (1) | IL131492A0 (en) |
| WO (1) | WO1998048839A1 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101128196B (en) * | 2005-03-16 | 2013-01-02 | Meda制药有限及两合公司 | Combination of anticholinergics and leukotriene receptor antagonists for the treatment of respiratory diseases |
| CN104667256A (en) * | 2015-03-18 | 2015-06-03 | 江苏威克斯医疗科技有限公司 | Nasal cavity mucosa cilium nursing flushing fluid and application thereof |
| CN107753485A (en) * | 2017-11-28 | 2018-03-06 | 赵永宏 | A kind of pharmaceutical composition for having nose congestion and anesthetic effect concurrently and its application |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL133420A (en) * | 1997-08-26 | 2004-07-25 | Aventis Pharma Inc | Pharmaceutical composition in form of tablet comprising combination of antihistaminic piperidinoalkanol with decongestant sympathomimetic drug |
| ATE331522T1 (en) * | 1997-12-23 | 2006-07-15 | Schering Corp | COMPOSITION FOR THE TREATMENT OF RESPIRATORY AND SKIN DISEASES WITH AT LEAST ONE LEUCOTRIEN ANTAGONIST AND AT LEAST ONE ANTHISTAMINIC |
| GB9822170D0 (en) * | 1998-10-13 | 1998-12-02 | Danbioyst Uk Ltd | Novel formulations of fexofenadine |
| US6576224B1 (en) * | 1999-07-06 | 2003-06-10 | Sinuspharma, Inc. | Aerosolized anti-infectives, anti-inflammatories, and decongestants for the treatment of sinusitis |
| IT1313567B1 (en) * | 1999-07-27 | 2002-09-09 | Zambon Spa | USE OF N-ACETYL-CISTEIN FOR THE PREPARATION OF TOPICAL PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF ALLERGIC PATHOLOGIES OF |
| DE10007203A1 (en) | 2000-02-17 | 2001-08-23 | Asta Medica Ag | Composition for treating allergic and/or vasomotor rhinitis or allergic conjunctivitis by topical or oral administration, contains synergistic combination of non-sedating antihistamine and leukotriene antagonist |
| DE60209511T2 (en) * | 2001-09-18 | 2006-10-05 | Nycomed Danmark Aps | COMPOSITIONS FOR TREATING SNORING CONTAINING IPRATROPY AND XYLOMETAZOLIN |
| GB2389530B (en) | 2002-06-14 | 2007-01-10 | Cipla Ltd | Pharmaceutical compositions |
| PL373033A1 (en) * | 2002-06-20 | 2005-08-08 | Novartis Consumer Health S.A. | Nasal compositions comprising a mucopolysaccharide and propylene glycol |
| WO2004019955A1 (en) | 2002-08-30 | 2004-03-11 | Altana Pharma Ag | The use of the combination of ciclesonide and antihistamines for the treatment of allergic rhinitis |
| US20070071689A1 (en) * | 2003-08-06 | 2007-03-29 | Galephar M/F | Advantageous combination for inhalation of nacystelyn and bronchodilators |
| US20050255154A1 (en) | 2004-05-11 | 2005-11-17 | Lena Pereswetoff-Morath | Method and composition for treating rhinitis |
| WO2006058022A1 (en) | 2004-11-24 | 2006-06-01 | Medpointe Healthcare Inc. | Compositions comprising azelastine and methods of use thereof |
| US20070020330A1 (en) | 2004-11-24 | 2007-01-25 | Medpointe Healthcare Inc. | Compositions comprising azelastine and methods of use thereof |
| DE602006021452D1 (en) * | 2005-08-26 | 2011-06-01 | Meiji Dairies Corp | ANTIALLERGIC MEDIUM |
| WO2008008373A2 (en) | 2006-07-11 | 2008-01-17 | Arubor Corp | Rhinosinusitis prevention and therapy with proinflammatory cytokine inhibitors |
| JP2008143845A (en) * | 2006-12-11 | 2008-06-26 | Hoshienu Seiyaku Kk | Nasal drop composition and nasal drop spraying tool |
| BR112014029442A2 (en) * | 2012-05-25 | 2017-06-27 | Xlear Inc | xylitol based antimucosal compositions and related methods and compositions |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3482015A (en) * | 1965-02-08 | 1969-12-02 | Merck & Co Inc | Aerosol composition of phenylephrine tartrate and the production of such |
| US4053628A (en) * | 1971-05-12 | 1977-10-11 | Fisons Limited | Composition |
| US4552899A (en) * | 1984-04-09 | 1985-11-12 | Analgesic Associates | Cough/cold mixtures comprising non-steroidal anti-inflammatory drugs |
| JPH0753671B2 (en) * | 1985-12-26 | 1995-06-07 | 積水化学工業株式会社 | Transdermal / transmucosal preparation |
| JPH08508007A (en) * | 1991-11-19 | 1996-08-27 | センター フォー イノベイティブ テクノロジー | Combined treatment of colds with virus-suppressing anti-receptors |
| BR9407414A (en) * | 1993-09-07 | 1996-11-12 | Procter & Gamble | Compositions containing a non-steroidal propionic acid anti-inflammatory agent amino acid salt and at least one decongestant an expectorant an antihistamine and an antitussive |
| WO1997001337A1 (en) * | 1995-06-29 | 1997-01-16 | Mcneil-Ppc, Inc. | The combination of topical nasal antihistamines and topical nasal steroids |
| WO1997001341A1 (en) * | 1995-06-29 | 1997-01-16 | Mcneil-Ppc, Inc. | The combination of topical nasal mast cell stabilizers and topical nasal steroids |
| DE19532714A1 (en) * | 1995-09-05 | 1997-03-06 | Bayer Ag | Combination of 5-lipoxygenase and leukotriene synthesis inhibitors with glucocorticosteroids |
| EP0780127A1 (en) * | 1995-12-19 | 1997-06-25 | The Procter & Gamble Company | A nasal spray containing a steroid and a antihistamine |
-
1998
- 1998-04-02 CN CN98804579A patent/CN1253508A/en active Pending
- 1998-04-02 AU AU68780/98A patent/AU6878098A/en not_active Abandoned
- 1998-04-02 IL IL13149298A patent/IL131492A0/en unknown
- 1998-04-02 BR BR9809022-4A patent/BR9809022A/en not_active Application Discontinuation
- 1998-04-02 JP JP54699898A patent/JP2001524108A/en active Pending
- 1998-04-02 WO PCT/US1998/006483 patent/WO1998048839A1/en not_active Application Discontinuation
- 1998-04-02 EP EP98914420A patent/EP0979105A1/en not_active Withdrawn
- 1998-04-02 CA CA002281789A patent/CA2281789A1/en not_active Abandoned
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101128196B (en) * | 2005-03-16 | 2013-01-02 | Meda制药有限及两合公司 | Combination of anticholinergics and leukotriene receptor antagonists for the treatment of respiratory diseases |
| CN104667256A (en) * | 2015-03-18 | 2015-06-03 | 江苏威克斯医疗科技有限公司 | Nasal cavity mucosa cilium nursing flushing fluid and application thereof |
| CN107753485A (en) * | 2017-11-28 | 2018-03-06 | 赵永宏 | A kind of pharmaceutical composition for having nose congestion and anesthetic effect concurrently and its application |
Also Published As
| Publication number | Publication date |
|---|---|
| IL131492A0 (en) | 2001-01-28 |
| EP0979105A1 (en) | 2000-02-16 |
| JP2001524108A (en) | 2001-11-27 |
| WO1998048839A1 (en) | 1998-11-05 |
| BR9809022A (en) | 2000-08-01 |
| AU6878098A (en) | 1998-11-24 |
| CA2281789A1 (en) | 1998-11-05 |
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