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WO2012030308A2 - Formulation comprenant la cellobiose - Google Patents

Formulation comprenant la cellobiose Download PDF

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Publication number
WO2012030308A2
WO2012030308A2 PCT/TR2011/000198 TR2011000198W WO2012030308A2 WO 2012030308 A2 WO2012030308 A2 WO 2012030308A2 TR 2011000198 W TR2011000198 W TR 2011000198W WO 2012030308 A2 WO2012030308 A2 WO 2012030308A2
Authority
WO
WIPO (PCT)
Prior art keywords
cellobiose
pharmaceutical composition
composition according
average particle
particle size
Prior art date
Application number
PCT/TR2011/000198
Other languages
English (en)
Other versions
WO2012030308A3 (fr
Inventor
Mahmut Bilgic
Original Assignee
Mahmut Bilgic
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Mahmut Bilgic filed Critical Mahmut Bilgic
Priority to EP11776267.4A priority Critical patent/EP2611431A2/fr
Publication of WO2012030308A2 publication Critical patent/WO2012030308A2/fr
Publication of WO2012030308A3 publication Critical patent/WO2012030308A3/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—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
    • 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
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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 a pharmaceutical composition
  • a pharmaceutical composition comprising a carrier and one or more than one active agents developed in order to be used in the treatment of respiratory tract diseases such as asthma and COPD.
  • the patent numbered EP0464171 disclosed that the particle size of the carrier comprised in the dry powder formulation could be in the range of 5 to 1000 ⁇ . While it is possible to adjust the particle size of the carrier so as to ensure a more effective inhalation, one can also add another excipient along with the carrier.
  • the patent numbered WO8705213 relates to a dry powder formulation comprising a lubricant in addition to the carrier. Both of these patents in the prior art particularly emphasize lactose.
  • lactose is used in the products on the market such as FORADIL® and ASTMEROL®.
  • lactose is a good carrier, it leads to many problems due to its hygroscopic nature.
  • the dry powder formulation may be agglomerated and adhere to the surfaces. Since this adhesion also comprises the active agents, amount of the active agent in the formulation that reaches the patient's mouth decreases, therefore the quality of the treatment.
  • novel formulations that would be developed in order to improve the quality of the treatment and minimize the specified problems.
  • the inventor has surprisingly found that therapeutic effect is increased when long-acting ⁇ 2 - agonist and/or pharmaceutically acceptable derivatives thereof are carried with cellobiose.
  • cellobiose is used as carrier in the dry powder formulations of the present invention, it has been seen that the rate of agglomeration of the formulation and adhesion to the device surfaces is decreased. By this means, the amount of active agent reaching the mouth therefore the lungs of the patient increases. Thus, it provides a more effective treatment with reduced dose frequency.
  • the present invention provides a pharmaceutical composition
  • a pharmaceutical composition comprising long-acting Pa- agonist and/or pharmaceutically acceptable derivatives thereof as active agent and cellobiose as carrier developed in order to be used in the treatment of respiratory diseases such as asthma and COPD.
  • the present invention provides a dry powder formulation comprising long- acting p -agonist and/or pharmaceutically acceptable derivatives thereof and cellobiose.
  • the amount of cellobiose in the dry powder formulation comprising long-acting p 2 -agonist and/or pharmaceutically acceptable derivatives thereof is in the range of 0-50 mg and preferably in the range of 3-20 mg.
  • the present invention provides a medicament in which the average particle size of cellobiose that the pharmaceutical composition comprises is in the range of 0,01 to 1000 ⁇ , preferably in the range of 5 to 500 ⁇ .
  • amount of active agent reaching the mouth and lungs of the patient is increased by adjusting the particle size of the carrier.
  • the present invention provides a pharmaceutical composition comprising cellobiose which has two different particle sizes.
  • the dry powder formulation of the present invention can comprise cellobiose which has two different particle sizes as coarse and fine in addition to the active agent.
  • the active agent can reach the lungs more easily during inhalation.
  • Fine particles adsorb onto the active areas on the coarse particles that the formulation comprises. Fine particles also have active areas. Thus, the number of active areas required for the active agent to adsorb and be carried is increased.
  • coarse particles may get caught in the upper respiratory tract. In this case, the fine particles on the active areas of the coarse particles are released with the active agents and effectively transmitted to the lungs.
  • a formulation lacks fine particles, when the coarse particles get caught in the upper respiratory tract, active agent is released there and cannot reach the lungs.
  • fine particles can fly without coarse particles and remain in the patient's mouth. Consequently, it provides advantages in the treatment that cellobiose comprised in the dry powder formulation of the present invention has two different particle sizes.
  • Average particle size of cellobiose particles comprised in the pharmaceutical composition of the present invention is smaller than 10 ⁇ , preferably smaller than 5 ⁇ and more preferably smaller than 3 ⁇ .
  • Average particle size of the coarse cellobiose particles is in the range of 10 to 1000 ⁇ , preferably in the range of 100 to 600 ⁇ and more preferably in the range of 150 to 300 ⁇ .
  • long-acting p 2 -agonist and/or pharmaceutically acceptable derivatives thereof in the medicament formulation comprises pharmaceutically acceptable solvates, hydrates, enantiomers or diastereomers, racemates, free base, organic salts, inorganic salts, esters, polymorphs, crystalline forms and amorphous forms of long-acting p 2 -agonist or a combination thereof.
  • long-acting 2 -agonist and/or pharmaceutically acceptable derivatives thereof comprised in the dry powder formulation can be selected from a group comprising salmeterol, bambuterol, clenbuterol, formoterol, arformoterol, carmoterol, indacaterol, milveterol, olodaterol or a combination thereof, though it is probably formoterol, arformoterol and carmoterol.
  • amount of the active agent in the dry powder formulation comprising long-acting p 2 -agonist and/or pharmaceutically acceptable derivatives thereof is in the range of 0,01 to 25 ⁇ , preferably in the range of 0,1 to 20 ⁇ and more preferably 0,5 to 15 ⁇ .
  • the present invention provides a medicament comprising long- acting 2 -agonist and/or pharmaceutically acceptable derivatives thereof in micronized sizes.
  • Average particle size of long-acting 2 -agonist and/or pharmaceutically acceptable derivatives thereof comprised in the formulation of the present invention is in the range of 0,01 to 30 ⁇ , preferably in the range of 0,05 to 10 ⁇ and more preferably in the range of 1 to 5 ⁇ . Adjustment of particle sizes is very important for medicaments administered by the inhalation route. Coarse particles can be caught in the upper respiratory tract after inhaled and this makes it harder for the particles to reach the lungs.
  • the present invention provides inhalation of the medicament comprising long-acting ⁇ 2 - agonist and/or pharmaceutically acceptable derivatives thereof as active agent and cellobiose as carrier via dry powder inhalers.
  • the present invention provides inhalation of the dry powder formulation comprising long-acting p 2 -agonist and/or pharmaceutically acceptable derivatives thereof and cellobiose from a capsule or blister.
  • the present invention provides administration of the dry powder formulation comprising long-acting 2 -agonist and/or pharmaceutically acceptable derivatives thereof and cellobiose in aerosol form.
  • aerosol refers to dispersion or suspension of a liquid, solution or solid particles in air or gas.
  • the dry powder formulation can be administered in aerosol form which is characterized by containing propellant gas or not.
  • the dry powder formulation comprising cellobiose can additionally comprise other excipients.
  • excipients can be selected from a group comprising monosaccharides (glucose, etc.), disaccharides (lactose, cellobiose, saccharose, maltose, etc.), oligosaccharides and polysaccharides (dextran, etc.), polyalcohols (sorbitol, mannitol, xyolitol, etc.), salts (sodium chloride, calcium carbonate, etc.), inositol and/or isomers (myoinositol, etc.) or a combination thereof.
  • the pharmaceutical composition comprising long-acting ⁇ 2 - agonist and/or pharmaceutically acceptable derivatives thereof can additionally comprise one or more active agents and/or pharmaceutically acceptable derivatives thereof selected from a group comprising anticholinergic, adrenergic agonist, glucocorticosteroid, xanthine, anti leukotriene, PDEIV inhibitor, EGFR inhibitor, anti-allergic, anti-inflammatory, antihistaminic and antimuscarinic substances.
  • the pharmaceutical composition comprising long-acting ⁇ 2 - agonist and/or pharmaceutically acceptable derivatives thereof can additionally comprise one or more substances and/or pharmaceutically acceptable derivatives thereof selected from a group comprising anticholinergics such as tiotropium, ipratropium, glycopyrronium and oxytropium; p 2 -agonists such as salbutamol, fenoterol, terbutaline, carbuterol and pirbuterol; corticosteroids such as beclomethasone, budesonide, ciclesonide, fluticasone and mometasone; xanthines such as doxyphyllin, theobromine, theophylline and aminophylline; antileukotrienes such as montelukast, pranlucast, zafirlukast, ritolukast, sulukast, tomelukast, verlukast, iralukas
  • the pharmaceutical composition comprising long-acting p 2 -agonist and/or pharmaceutically acceptable derivatives thereof according to the present invention can be used in the treatment of many respiratory diseases, particularly in asthma, allergic rhinitis and chronic obstructive pulmonary disease (COPD).
  • COPD chronic obstructive pulmonary disease
  • these respiratory diseases can be, but not limited to, asthma at any stage, 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 and COPD.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention concerne une composition pharmaceutique, comprenant un excipient et un ou plusieurs agents actifs, qui a été développée pour être utilisée dans le traitement des maladies des voies respiratoires telles que l'asthme et la BPCO.
PCT/TR2011/000198 2010-09-01 2011-08-24 Formulation comprenant la cellobiose WO2012030308A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP11776267.4A EP2611431A2 (fr) 2010-09-01 2011-08-24 Formulation comprenant la cellobiose

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR2010/07250 2010-09-01
TR2010/07250A TR201007250A2 (tr) 2010-09-01 2010-09-01 Selobioz içeren formülasyon.

Publications (2)

Publication Number Publication Date
WO2012030308A2 true WO2012030308A2 (fr) 2012-03-08
WO2012030308A3 WO2012030308A3 (fr) 2012-08-09

Family

ID=44883366

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/TR2011/000198 WO2012030308A2 (fr) 2010-09-01 2011-08-24 Formulation comprenant la cellobiose

Country Status (3)

Country Link
EP (1) EP2611431A2 (fr)
TR (1) TR201007250A2 (fr)
WO (1) WO2012030308A2 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150202148A1 (en) * 2012-07-05 2015-07-23 Arven llac Sanayi Ve Ticaret Anonim Sirketi Dry powder inhalers comprising a carrier other than lactose
DE202016008304U1 (de) 2015-01-22 2017-07-05 Pfeifer & Langen GmbH & Co. KG Cellobiose in Zusammensetzungen zum Verzehr oder zur Einnahme
US10105316B2 (en) 2012-07-05 2018-10-23 Arven llac Sanayi Ve Ticaret A.S. Inhalation compositions comprising muscarinic receptor antagonist
IT201900008340A1 (it) * 2019-06-07 2020-12-07 Genetic S P A Sali di montelukast e loro composizioni farmaceutiche

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1987005213A1 (fr) 1986-03-04 1987-09-11 Chiesi Farmaceutici S.P.A. Nouvelles compositions pharmaceutiques destinees a etre inhalees
EP0464171A1 (fr) 1990-01-24 1992-01-08 Nat Res Dev Supports d'aerosols.

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0012261D0 (en) * 2000-05-19 2000-07-12 Astrazeneca Ab Novel process
US6482429B1 (en) * 2001-06-20 2002-11-19 Boehringer Ingelheim Pharmaceuticals, Inc. Stable powder inhalation dosage formulation
GB0208609D0 (en) * 2002-04-13 2002-05-22 Glaxo Group Ltd Compositions
GB0312148D0 (en) * 2003-05-28 2003-07-02 Aventis Pharma Ltd Stabilized pharmaceutical products
GB0315889D0 (en) * 2003-07-08 2003-08-13 Aventis Pharma Ltd Stable pharmaceutical products
JP2009513531A (ja) * 2003-07-11 2009-04-02 グラクソ グループ リミテッド 糖エステルを含む吸入可能医薬製剤

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1987005213A1 (fr) 1986-03-04 1987-09-11 Chiesi Farmaceutici S.P.A. Nouvelles compositions pharmaceutiques destinees a etre inhalees
EP0464171A1 (fr) 1990-01-24 1992-01-08 Nat Res Dev Supports d'aerosols.

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150202148A1 (en) * 2012-07-05 2015-07-23 Arven llac Sanayi Ve Ticaret Anonim Sirketi Dry powder inhalers comprising a carrier other than lactose
EP2682097B1 (fr) 2012-07-05 2016-10-05 Arven Ilac Sanayi Ve Ticaret A.S. Inhalateurs de poudre sèche comprenant un support autre que le lactose
US10105316B2 (en) 2012-07-05 2018-10-23 Arven llac Sanayi Ve Ticaret A.S. Inhalation compositions comprising muscarinic receptor antagonist
DE202016008304U1 (de) 2015-01-22 2017-07-05 Pfeifer & Langen GmbH & Co. KG Cellobiose in Zusammensetzungen zum Verzehr oder zur Einnahme
IT201900008340A1 (it) * 2019-06-07 2020-12-07 Genetic S P A Sali di montelukast e loro composizioni farmaceutiche
WO2020245358A1 (fr) * 2019-06-07 2020-12-10 Genetic S.P.A. Sels de montélukast et compositions pharmaceutiques les contenant
US20220218690A1 (en) * 2019-06-07 2022-07-14 Genetic S.P.A. Montelukast salts and pharmaceutical compositions containing the same

Also Published As

Publication number Publication date
WO2012030308A3 (fr) 2012-08-09
TR201007250A2 (tr) 2012-03-21
EP2611431A2 (fr) 2013-07-10

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