WO2011136752A1 - Composition pharmaceutique combinée comprenant du carmotérol et du ciclésonide pour le traitement de maladies respiratoires - Google Patents

Composition pharmaceutique combinée comprenant du carmotérol et du ciclésonide pour le traitement de maladies respiratoires Download PDF

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Publication number
WO2011136752A1
WO2011136752A1 PCT/TR2011/000111 TR2011000111W WO2011136752A1 WO 2011136752 A1 WO2011136752 A1 WO 2011136752A1 TR 2011000111 W TR2011000111 W TR 2011000111W WO 2011136752 A1 WO2011136752 A1 WO 2011136752A1
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medicament
composition according
pharmaceutically acceptable
carmoterol
medicament composition
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PCT/TR2011/000111
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English (en)
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Mahmut Bilgic
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Mahmut Bilgic
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Publication of WO2011136752A1 publication Critical patent/WO2011136752A1/fr

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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
    • A61K31/33—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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators

Definitions

  • the present invention relates to the pharmaceutical composition
  • the pharmaceutical composition comprising the active agents carmoterol and ciclesonide and/or their pharmaceutically acceptable derivatives so as to be used in the treatment of respiratory tract diseases, especially in asthma and chronic obstructive pulmonary disease (COPD), and the delivery of this composition.
  • COPD chronic obstructive pulmonary disease
  • bronchia are the channels which function to distribute the inhaled air into the lung tissues.
  • stimulants such as allergen, infection, good and bad smell, smoke cause contractions in the airway muscles (bronchoconstruction) and/or excessive secretion in glands and results in contractions in the airways.
  • bronchoconstruction obstructive pulmonary disease
  • p 2- agonists induce an alleviating or eliminating effect on bronchoconstriction.
  • Carmoterol (Formula I), which was first described in the patent numbered EP0147719 (Bl), is a p 2- agonist named as 8-hydroxy-5-[(lR)- 1 -hydroxy-2- [ [(2R)- 1 -(4-methoxyphenyl)prophane-2-yl] amino] ethyl] - 1 H-quinoline-2-one .
  • Ciclesonide which has the chemical name 2-[(lS, 2S, 4R, 85, 95,1 IS, 12S, 13i?)-6- cyclohexyl-l l-hydroxy-9, 13 -dimethyl- 16-oxo-5, 7-dioxopentacyclo [10.8.0.0 2 ' 9 .0 4 ' 8 .0 13 ' 18 ] icosa-14, 17-dien-8-yl]- 2-oxoethyl 2-methylpropanoate, is a corticosteroid. Ciclesonide which is a potent anti-inflammatory medicament was first disclosed in the patent numbered US5482934.
  • the present invention provides a medicament comprising carmoterol or a pharmaceutically acceptable derivative thereof and ciclesonide or a pharmaceutically acceptable derivative thereof so as to be used in the treatment of respiratory tract diseases such as asthma, COPD and allergic rhinitis.
  • the inventor has surprisingly found that a significant unexpected therapeutic benefit, particularly a synergistic effect, in the treatment of inflammatory or obstructive airways diseases, is obtained by combination therapy using carmoterol and ciclesonide and/or a pharmaceutically acceptable derivatives thereof.
  • the pharmaceutical composition comprising carmoterol and ciclesonide and/or a pharmaceutically acceptable derivative thereof provides faster onset and has a more long- lasting and efficient therapeutic effect when compared with the pharmaceutical compositions containing only one of these active agents.
  • the present invetion provides a treatment method in which the pharmaceutical composition comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof is used as a symptomatolytic medicament.
  • Carmoterol has a short period of onset of action when taken at particular doses. For that reason, this combination can be used as a symptomatolytic medicament.
  • the present invention provides a medicament in which carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof are reciprocally affected in a positive way. Accordingly, carmoterol enhances the anti-inflammatory effect resulting from attachment of ciclesonide with glucocorticoid receptors since carmoterol strengthens translocation of these receptors. Ciclesonide, on the other hand, increases transcription of ⁇ 2 - receptors with which carmoterol attaches.
  • carmoterol and ciclesonide and/or their pharmaceutically acceptable derivatives induce therapeutic effects at lower doses when they are used in combination compared with their use alone.
  • severity of the side effects that they may cause can be minimized with the help of lower dose use of the active agents.
  • the present invention provides a simplified treatment realized by delivery of the medicament comprising carmoterol which is an ultra long-acting 2 -agonist and ciclesonide which is a corticosteroid inducing anti-inflammatory effect and/or pharmaceutically acceptable derivatives thereof once a day.
  • the active agents according to the present invention provide a long-lasting effect a more effective treatment and thus a simpler treatment in which dosing frequency of the medicament is reduced is provided and patient compatibility is increased.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof is administered by the inhalation route.
  • the medicament taken by the inhalation route is delivered to the target area more quickly compared with the oral and the parenteral route. Therefore, it provides a quicker and more effective relief to the patient.
  • the present invention provides less frequent dose intake of the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof by the inhalation route compared to the oral and the parenteral administration.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof by the inhalation route compared to the oral and the parenteral administration.
  • the medicament comprising carmoterol and ciclesonide and/or a pharmaceutically acceptable derivative thereof is provided for simultaneous, sequential or separate administration by the inhalation route in the treatment of inflammatory or obstructive airways diseases.
  • the present invention provides a medicament formulation in which carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof are preferably formulated in the same dosage form. Having the active agents in the same dosage form provides a more effective, simple and cost-effective treatment. Moreover, it is easier to track the progress of the patients in the treatments utilizing single dosage forms.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof is delivered by single-dose or multi-dose inhalation devices.
  • the active agents of the present invention can be inhaled via different devices while all of the active agents of the present invention can also be administered by a single device. However, it is preferred that the active agents are delivered as together by a single device according to the invention.
  • the medicament comprising carmoterol and ciclesonide and/or a pharmaceutically acceptable derivative thereof is delivered in aerosol, dry powder, solution or suspension forms.
  • the active agents in the medicament of the present invention can be delivered in different dosage forms as well as in the same dosage form. Preferably, all of the active agents of the medicament are delivered in same dosage form.
  • aerosol refers to dispersion or suspension of a liquid, solution or solid substance in the air or in a gas.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can be inhaled in aerosol form via a suitable device.
  • the aerosol composition in the device can be characterized by comprising propellant gas or not.
  • the active agents of the present invention can be inhaled separately in different aerosol compositions as well as together in a single aerosol composition.
  • the active agents of the present invention are preferably inhaled in a single aerosol composition.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof may also comprise propellant gas in addition to the active agents.
  • the medicament comprising propellant gas can be administered by a pressurized metered dose inhalation device.
  • These propellant gases are aimed to deliver the active agents to the lungs more easily.
  • These propellant gases are preferably hydrocarbons and halohydrocarbons. Only one of these hydrocarbons or a mixture of them can be used.
  • the particularly used propellant gases are HFA134a, HFA227 or mixtures thereof; TGI 34a, TG227 or halogenated alkane derivatives selected from the mixtures thereof.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can be transmitted in a propellant-free aerosol composition via a suitable inhalation device such as nebulizers.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can also comprise other substances such as cosolvents, stabilizers, surfactants, antioxidants, lubricants and pH adjusters in addition to the active agent.
  • the medicament delivered in aerosol form and comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can comprise active agents in an amount in the range of 0.001% to 8%, preferably in the range of 0,001% to 5%.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can be tranmitted to patient as propellant- free solution or inhalation composition in suspension form by a nebulization device.
  • the active agents of the present invention can be inhaled in separate propellant-free suspensions or solutions one by one as well as together in a single propellant-free suspension or solution. In these inhalation formulations, water or water-alcohol mixture can be used as solvent.
  • the ratio of ethanol to water can be at most 80%, preferably 60% by volume.
  • pH value of the suspensions or solutions comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can be in the range of 2 to 7, preferably in the range of 2 to 5.
  • Organic or inorganic acids preferably hydrochloric acid, citric acid, ascorbic acid, formic acid, fumaric acid, tartaric acid, malic acid, sulphuric acid or a mixture of one or several of them can be used as a pH adjuster in order to provide a value in these ranges.
  • the propellant-free inhalation formulations in solution or suspension form may comprise edetic acid (EDTA) or its salts, excipients, sodium - edetate, stabilizer or complexing agents in addition to said substances.
  • EDTA edetic acid
  • the amount of sodium edetate included in said solution or suspension can be in the range of Omg/lOOml and 120mg/100ml, preferably in the range of Omg/100 ml to 50mg/100ml, more preferably in the range of Omg/lOOml to lOmg/lOOml.
  • propellant-free solutions or suspensions can comprise cosolvents and/or other excipients and/or preservatives in addition to the active agents.
  • the preferred cosolvents are hydroxyl groups, alcohols, especially other polar groups comprising isopropyl alcohols and glycols.
  • the said excipients are substances which do not have active agent characteristics such as tocopherols, vitamins, provitamins and surfactants.
  • the preservative agents used for preventing contaminations caused by pathogens are cetyl pyridiniumchloride, benzalconium chloride, benzoic acid or benzoates as known in the prior art.
  • the medicament of the present invention comprising carmoterol and ciclesonide and/or a pharmaceutically acceptable derivative thereof is preferably administered in dry powder form and dry powder inhalation devices are used for delivery of the medicament of the present invention.
  • said medicament in dry powder form also comprise pharmaceutically acceptable excipients in addition to the active agent.
  • excipients can be selected from monosaccharides (glucose, etc.), disaccharides (lactose, saccharose, maltose, etc.), oligosaccharides and polysaccharide (dextran, etc.), polyalcohols (sorbitol, mannitol, xylitol, etc.), salts (sodium chloride, calcium carbonate, etc.) or a mixture thereof.
  • lactose is used as an excipient in the medicament of the present invention.
  • the amount of the pharmaceutically acceptable excipient is in the range of 0 to 50 mg, for example in the range of 1 mg to 48 mg, 1 mg to 47 mg, 1 mg to 42 mg, 1 mg to 40 mg, 1 mg to 38 mg, 1 mg to 35 mg, 1 mg to 32 mg, 1 mg to 30 mg, 1 mg to 28 mg, 1 mg to 25 mg , 1 mg to 23 mg, 2 mg to 48 mg, 2 mg to 47 mg, 2 mg to 42 mg, 2 mg to 40 mg, 2 mg to 38 mg, 2 mg to 35 mg, 2 mg to 32 mg, 2 mg to 30 mg, 2 mg to 28 mg, 2 mg to 25 mg , 2 mg to 23 mg, 2 mg to 20 mg, 3 mg to 48 mg, 3 mg to 47 mg, 3 mg to 42 mg, 3 mg to 40 mg, 3 mg to 38 mg, 3 mg to 35 mg, 3 mg to 32 mg, 3 mg to 30 mg, 3 mg to 28 mg, 3 mg to 25 mg.
  • the amount of the pharmaceutically acceptable excipient is most preferably in the range of 3 to 20 mg for example 3 mg to 19 mg, 3.5 mg to 18 mg, 4 mg to 17 mg.
  • the medicament composition comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof is delivered via a dry powder inhaler in which said medicament is stored in peelable blister packs, reservoirs or capsules.
  • inhalation devices designed to ensure transmission of the medicament in dry powder form
  • a certain amount of dry powder medicament is prepared for inhalation in response to each actuation of the device.
  • carmoterol and/or a pharmaceutically acceptable derivative thereof which is one of the active agents included in the medicament comprising the combination of the active agents, is selected from pharmaceutically acceptable solvates, hydrates, enantiomers or diastereomers, racemates, the free base, organic salts, inorganic salts, esters, polymorphs, crystalline forms and amorphous forms of carmoterol and/or the combinations thereof.
  • R,R diastereomer of the carmoterol is preferably used in the medicament of the present invention.
  • ciclesonide and/or a pharmaceutically acceptable derivative thereof which is one of the active agents included in the medicament comprising the combination of active agents, is selected from pharmaceutically acceptable solvates, hydrates, enantiomers or diastereomers, racemates, the free base, organic salts, inorganic salts, esters, polymorphs, crystalline forms and amorphous forms of ciclesonide and/or the combinations thereof.
  • the amount of carmoterol and/or a pharmaceutically acceptable derivative thereof, which is one of the active agents included in the dry powder formulation comprising the combination of carmoterol and ciclesonide is in the range of 0.01 ⁇ g, 0.05 ⁇ 0.1 ⁇ & 0.2 ⁇ g, 0.3 ⁇ g, 0.4 ⁇ g, 0.5 ⁇ g, 0.6 ⁇ 0.7 ⁇ g, 0.8 ⁇ g, 0.9 ⁇ g or 1 ⁇ g to 7 ⁇ 8 ⁇ g, 9 ⁇ g, 10 ⁇ g, 12 ⁇ g, 15 ⁇ g, 17 ⁇ 3 ⁇ 4 20 ⁇ 22 ⁇ g, 25 ⁇ g or 30 ⁇ g, for example 0.01 ⁇ g to 30 ⁇ g, 0.01 ⁇ g to 27 ⁇ 0.01 ⁇ g to 25 ⁇ g, 0.01 ⁇ g to 23 ⁇ g, 0.01 ⁇ g to 20 ⁇ g, 0.01 ⁇ g to 18 ⁇ g, 0.01 ⁇ g to 15 ⁇ g, 0.01 ⁇ g, 0.01
  • the amount of ciclesonide and/or a pharmaceutically acceptable derivative thereof, which is one of the active agents included in the dry powder formulation comprising the combination of carmoterol and ciclesonide is in the range of 1 ⁇ g, 5 ⁇ 10 ⁇ g, 15 ⁇ 25 ⁇ g or 30 ⁇ g to 400 ⁇ g, 450 ⁇ g, 500 ⁇ g, 550 ⁇ g, 600 ⁇ g, 650 ⁇ & 700 ⁇ g, 750 ⁇ g, 800 ⁇ g, 850 ⁇ g, 900 ⁇ 3 ⁇ 4 950 ⁇ g or 1000 ⁇ g for example 1 ⁇ g to 1000 ⁇ 1 ⁇ g to 950 ⁇ g, 1 ⁇ g to 900 ⁇ 1 ⁇ g to 850 ⁇ ⁇ , 1 ⁇ g to 800 ⁇ 1 ⁇ g to 750 ⁇ 1 ⁇ g to 700 ⁇ g, 1 ⁇ g to 650 ⁇ g, 1 ⁇ g to 600 ⁇ g, 1 ⁇ g to 550 ⁇ g
  • the medicament composition in accordance with the present invention is preferably in the form of micronized dry powder particles.
  • the active agents present in said medicament composition have average particle size of 1 ⁇ to 20 ⁇ , preferably from 1 ⁇ to 10 ⁇ , most preferably 1 ⁇ to 6 ⁇ .
  • Lactose particles present in said medicament composition as an excipient has average particle size of not more than 300 ⁇ , preferably not more than 250 ⁇ .
  • the lactose particles in the medicament composition can be found in more than one fraction with different average particle size.
  • the pharmaceutical composition comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can additionally comprise one or more substances selected from a group comprising mast cell stabilizer, anticholinergic, adrenergic agonist, glucocorticosteroid, xanthine, anti leukotriene, PDEIV inhibitor, EGFR inhibitor, anti-allergic, anti-inflamatory, antihistaminic and antimuscarinic substances.
  • the pharmaceutical composition comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can additionally comprise one or more substances selected from a group comprising mast cell stabilizers such as chromoglycate and nedocromile; anticholinergics such as tiotropium, ipratropium, glycopyrronium, chromoglycate and oxytropium; ⁇ 2 ⁇ 8 ⁇ 3 such as formoterol, arformoterol, bambuterol, salmeterol, clenbuterol, salbutamol, fenoterol, terbutaline, carbuterol and pirbuterol; corticosteroids such as beclomethasone, budesonide, fluticasone and mometasone; xanthines such as doxyphyllin, theobromine, theophylline and aminophylline; antileukotrienes such as montelukast, pranlucast, zafirlukas
  • the pharmaceutical composition comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof can additionally comprise chromoglycate and/or a pharmaceutically acceptable derivative thereof.
  • Derivatives of chromoglycate in the present invention comprise pharmaceutically acceptable solvates, hydrates, enantiomers or diastereomers, racemates, the free base, organic salts, inorganic salts, esters, polymorphs, crytsalline forms and amorphous forms of chromoglycate and/or combinations thereof.
  • Sodium chromoglycate is preferably used in the preparation of the medicament of the present invention.
  • the medicament comprising carmoterol and ciclesonide and/or pharmaceutically acceptable derivatives thereof according to the present invention can be used in the treatment of many respiratory diseases, particularly in asthma, chronic obstructive pulmonary disease (COPD) and allergic rhinitis.
  • these respiratory diseases can be, but not limited to, asthma at any phase, acute lung injury (ALI), acute respiratory distress syndrome (ARDS), exacerbation of airway hyperactivity, bronchiectasis, chronic obstructive pulmonary including emphysema and chronic bronchitis, respiratory diseases or lung diseases (COPD, COAD or COLD), pneumoconiosis, aluminosis, anthracosis, asbestosis, chalicosis, ptilosis, siderosis, silicosis, tabacosis, byssinosis.
  • This treatment can be prophylactic or symptomatic.
  • the composition of the present invention is especially used for symptomatic treatment of asthma, COPD and allergic
  • composition pertaining to the present invention can be explained with, but not limited to, the examples given below.
  • the active agent carmoterol given in the following examples comprises all pharmaceutically acceptable racemates, enantiomers or diastereomers, salts, solvates, esters, hydrates and/or the free base, polymorphs, amorphous and crystalline forms thereof.
  • the active agent ciclesonide given in the following examples comprises all pharmaceutically acceptable salts, solvates, esters, hydrates and/or enantiomers, polymorphs, amorphous and crystalline forms thereof.
  • Carmoterol or a pharmaceutically acceptable derivative thereof is preferably in the form of R,R-carmoterol.
  • the pharmaceutically acceptable excipient given in the following examples can optionally be added in a higher or a lower amount.
  • the capsule described in the following examples is made of gelatin; however, it can optionally be made of chitosan, starch and/or starch derivatives, cellulose and/or cellulose derivatives or synthetic polymers.
  • the active agent cromoglycate given in the following examples comprises all pharmaceutically acceptable racemates, enantiomers or diastereomers, solvates, esters, hydrates and/or the free base, polymorphs, amorphous and crystalline forms of cromoglycate.
  • a dry powder formulation suitable to be stored in blister packs for use in a multi-dose inhalation device comprises 1 part of carmoterol , 400 parts of ciclesonide having an average particle size in the range of 1 to 5 ⁇ , and 10000 parts of lactose as an excipient having a particle size below 300 ⁇ all of which were micronised in air jet mill.
  • the example can be repeated by replacing the amounts given in the table below with the amounts given in example 1 :
  • a dry powder formulation which is suitable to be stored in a gelatine capsule used in an inhalator comprises 1 part of carmoterol, 200 parts of ciclesonide having an average particle size in the range of 1 to 5 ⁇ , and 5500 parts of lactose as an excipient having a particle size below 300 ⁇ all of which were micronised in air jet mill.
  • a dry powder formulation suitable to be stored in blister packages for use in multi-dose inhalation devices comprises 2 parts of carmoterol, 200 parts of ciclesonide and 10000 parts of cromoglycate having an average particle size in the range of 1 to 5 ⁇ , and 10000 parts of lactose as an excipient having a particle size below 300 ⁇ all which were micronised in an air jet mill.
  • the dry powder formulation which is suitable to be stored in a gelatine capsule used in the inhalator for capsule forms comprises 2 parts of carmoterol, 200 parts of ciclesonide and 10000 parts of chromoglycate having an average particle size of 1 to 5 ⁇ , and 10000 parts of lactose as an excipient having a particle size below 300 ⁇ all of which were micronised in air jet mill.
  • An aerosol formulation prepared to be used in a metered dose inhalator comprises 2 parts of carmoterol, 200 parts of ciclesonide and excipients in a ratio of 97% by weight of the total formulation.

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Abstract

La présente invention concerne une composition de médicament comprenant une combinaison de carmotérol et/ou un dérivé pharmaceutiquement acceptable de celui-ci et de ciclésonide et/ou un dérivé pharmaceutiquement acceptable de celui-ci de manière à être utilisé dans le traitement de maladies des voies respiratoires, en particulier dans l'asthme et la bronchopneumopathie chronique obstructive (BPCO), et l'administration de cette composition pharmaceutique.
PCT/TR2011/000111 2010-04-26 2011-04-25 Composition pharmaceutique combinée comprenant du carmotérol et du ciclésonide pour le traitement de maladies respiratoires WO2011136752A1 (fr)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013109218A1 (fr) * 2012-01-16 2013-07-25 Mahmut Bilgic Formulations en poudre sèche comprenant du carmotérol et de la ciclésonide

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EP0147719A2 (fr) 1983-12-24 1985-07-10 Tanabe Seiyaku Co., Ltd. Dérivé de carbostyrile et procédé pour sa préparation
US5482934A (en) 1990-09-07 1996-01-09 Especialidades Latinas Medicamentos Universales, S.A. (Elmu, S.A.) Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions
US20060257324A1 (en) * 2000-05-22 2006-11-16 Chiesi Farmaceutici S.P.A. Pharmaceutical solution formulations for pressurised metered dose inhalers
WO2008102128A2 (fr) * 2007-02-19 2008-08-28 Cipla Limited Combinaisons pharmaceutiques
WO2008138939A1 (fr) * 2007-05-16 2008-11-20 Nycomed Gmbh Dérivés de pyrazolone en tant qu'inhibiteurs de la pde4
WO2010007447A1 (fr) * 2008-07-18 2010-01-21 Prosonix Limited Procédé d’amélioration de la cristallinité

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0147719A2 (fr) 1983-12-24 1985-07-10 Tanabe Seiyaku Co., Ltd. Dérivé de carbostyrile et procédé pour sa préparation
US5482934A (en) 1990-09-07 1996-01-09 Especialidades Latinas Medicamentos Universales, S.A. (Elmu, S.A.) Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions
US20060257324A1 (en) * 2000-05-22 2006-11-16 Chiesi Farmaceutici S.P.A. Pharmaceutical solution formulations for pressurised metered dose inhalers
WO2008102128A2 (fr) * 2007-02-19 2008-08-28 Cipla Limited Combinaisons pharmaceutiques
WO2008138939A1 (fr) * 2007-05-16 2008-11-20 Nycomed Gmbh Dérivés de pyrazolone en tant qu'inhibiteurs de la pde4
WO2010007447A1 (fr) * 2008-07-18 2010-01-21 Prosonix Limited Procédé d’amélioration de la cristallinité

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WO2013109218A1 (fr) * 2012-01-16 2013-07-25 Mahmut Bilgic Formulations en poudre sèche comprenant du carmotérol et de la ciclésonide

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