WO2012087094A1 - Composition pharmaceutique inhalable utilisée pour le traitement de l'asthme, administrable par les voies aériennes au moyen d'un dispositif d'aspiration entraînant l'aérosol - Google Patents

Composition pharmaceutique inhalable utilisée pour le traitement de l'asthme, administrable par les voies aériennes au moyen d'un dispositif d'aspiration entraînant l'aérosol Download PDF

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Publication number
WO2012087094A1
WO2012087094A1 PCT/MX2011/000148 MX2011000148W WO2012087094A1 WO 2012087094 A1 WO2012087094 A1 WO 2012087094A1 MX 2011000148 W MX2011000148 W MX 2011000148W WO 2012087094 A1 WO2012087094 A1 WO 2012087094A1
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WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
composition according
inhalable pharmaceutical
concentration range
inhalable
Prior art date
Application number
PCT/MX2011/000148
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English (en)
Spanish (es)
Inventor
Jacobo Alejandro GOMEZ RICO
David Silvino CARMONA NAVARRO
Original Assignee
Techsphere S.A. De C.V.
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 Techsphere S.A. De C.V. filed Critical Techsphere S.A. De C.V.
Publication of WO2012087094A1 publication Critical patent/WO2012087094A1/fr

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Classifications

    • 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
    • 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
    • A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • 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

Definitions

  • the present invention relates to an inhalable pharmaceutical composition for the treatment of asthma for administration by air via an aerosol emulation sucker.
  • Such pharmaceutical composition consists of an active ingredient, a surfactant, an isosmotic agent, a diluent, a viscosifying agent. , a preservative and an agent to adjust the pH.
  • Asthma is a frequent chronic disease, the most used therapeutic option for its treatment is the use of inhaled steroids.
  • the increase in cases of asthma as well as its impact on the quality of life of patients have led to increased efforts for their treatment.
  • This condition is a chronic pulmonary inflammatory disorder, characterized by a variable and reversible obstruction of airway flow.
  • inflammation of the lungs causes pathophysiological disorders such as epithelial and microvascular damage, bronchial hyperactivity and hypersecretion of the submucosal glands.
  • Inhaled steroids are the main treatment for the chronic form of this disease (Rodr ⁇ guez, Alain, R., et al. Inhaled steroids.
  • an electronic device of the aerosol emulation suction type as a route of administration of an inhalable pharmaceutical composition for the treatment of asthma, by air, since said device is portable, which confers the advantage over others. fogging devices that are bulky and need to be plugged into some power source. In addition, the device does not need to be connected to the electric current to operate, it works with rechargeable batteries. Another reason is that the device has electronic components and sensors that give it the advantage of activating the nebulization system through the natural aspiration of the user, which provides advantages over other pressurized pulmonary administration inhaler devices that require the application of a force mechanical to activate, in addition to the latter, user training is needed to synchronize that mechanical activation and the moment of aspiration.
  • the proposed device has the particularity of being able to integrate an electronic system that restricts the amount of suctions or inhalations per given time interval, which gives it the advantage of being able to dose from one more effective drug administration.
  • Another advantage of using this device is that with it you can integrate an electronic order that restricts the time of inhalation, which gives you the advantage of dosing.
  • An object of the present invention is to provide an inhalable pharmaceutical composition for the treatment of asthma.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air, by an electronic device.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air, by a portable electronic device.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air, by means of a portable electronic device, which works with rechargeable batteries.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air, by means of a portable electronic device that does not need the application of mechanical force to activate.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, via aerial, using a portable electronic device that does not need special training to use.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air, by means of a portable electronic device with which no substantial part of the medicament is lost in the mouth.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air, by means of a portable electronic device that restricts the amount of suctions or inhalations per time interval.
  • Another object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air, by means of a portable electronic device that restricts the inhalation time.
  • a further object of this invention is to provide an inhalable pharmaceutical composition for the treatment of asthma, by air, by means of a portable electronic device for inhalation by means of an aerosol emulation sucker.
  • US 3282791 discloses the use of inhaled dexamethasone for use in the treatment of asthma.
  • the use of inhalers requires special training to master the synchronization between the dosing apparatus and breathing or inhalation, so this form of administration is not considered practical use.
  • Patent 4414209 discloses the use of an anti-inflammatory steroid for the treatment of asthma, by inhalation.
  • the use of inhalers requires special training to master the synchronization between the dosing apparatus and breathing or inhalation, so this form of administration is not considered practical use.
  • US 5837699, US 5889015 and US 6057307 disclose the administration of aerosolized mometasone furoate particles in the form of dry powders, aqueous solutions or suspensions for the treatment of diseases of the upper and lower airways and / or of the lungs that They respond to corticosteroids, asthma among them.
  • the dependence on the use of a dispenser of considerable size makes this treatment ineffective.
  • US 5962445 discloses the use of 2-methoxystradiol in the treatment of asthma, by inhalation. This method of administration is complex because it requires special training to achieve the coupling between the device and the inhalation, so this form of administration is not considered practical use.
  • US 7029656 discloses the use of a water-soluble compound by means of a nebulizer for the treatment of asthma, however the nebulizers are, in general, bulky and noisy devices, in addition, the treatment time can be between 5 and 10 minutes, and, in the case of its use in a child, if he cries, the treatment is ineffective.
  • the pharmaceutical composition consists of an active ingredient, a surfactant, an isosmotic agent, a diluent or solvent, a viscosifying agent, a preservative and an agent for adjusting the pH.
  • active ingredients for the preparation of an inhalable pharmaceutical composition for the treatment of asthma for administration by air via an aerosol emulation sucker the following may be used, among others:
  • surfactants for the preparation of an inhalable pharmaceutical composition for the treatment of asthma for administration by air by means of an aerosol emulation sucker, the following may be used, among others:
  • polysorbate 20 polysorbate 80, dioctyl sodium sulfosuccinate, polyoxyethylated castor oil.
  • isosmotic agents for the preparation of an inhalable pharmaceutical composition for the treatment of asthma for administration by air via an aerosol emulation sucker the following may be used, among others:
  • an aerosol emulation sucker As diluents for the preparation of an inhalable pharmaceutical composition for the treatment of asthma for administration by air via an aerosol emulation sucker, the following may be used, among others:
  • viscous agents for the preparation of an inhalable pharmaceutical composition for the treatment of asthma for administration by air via an aerosol emulation sucker the following may be used, among others:
  • preservatives for the preparation of an inhalable pharmaceutical composition for the treatment of asthma for administration by air via an aerosol emulation sucker the following may be used, among others:
  • agents for adjusting the pH for the preparation of an inhalable pharmaceutical composition for the treatment of asthma for administration by air via an aerosol emulation sucker may be used, among others:
  • Hydrochloric acid phosphoric acid, maleic acid, sodium hydroxide, sulfuric acid, citric acid.
  • Salbutamol 5.0 mg was dissolved with 0.5 mL of propylene glycol and 0.5 mL of water, 0.02 mL of polysorbate 80 as a surface active agent, 1 mg of dextrose to adjust osmolarity, 0.03 mL of benzalkonium chloride as preservative were added to this same solution. and 0.25 mL of 1 N hydrochloric acid to adjust to pH 7.0.
  • Salbutamol 4.0 mg was dissolved with 0.1 mL of propylene glycol and 0.9 mL of water, 0.01 was added to this same solution.
  • mL of polysorbate 80 as a surfactant 0.5 mg of dextrose to adjust osmolarity 0.01 mL of benzalkonium chloride as a preservative and 0.2 mL of 1 N hydrochloric acid to adjust to pH 6.0. All raw materials used were pharmaceutical grade.
  • Fluticasone 1.0 mg was dissolved with 0.25 mL of polyethylene glycol 400 and 0.5 mL benzylbenzoate, 0.02 mL of polysorbate 20 as a surface active agent, 3 mg of mannitol to adjust osmolarity, 0.03 mL of benzalkonium chloride as a preservative were added to this same solution. and 0.3 mL of 0.1 N sodium hydroxide to adjust to pH of 6.9.
  • Fluticasone 2.5 mg was dissolved with 0.15 mL of polyethylene glycol 400 and 0.85 mL of benzylbenzoate, 0.01 mL of polysorbate 20 was added as a surface active agent, 2 mg of mannitol to adjust osmolarity, 0.04 mL of benzalkonium chloride as preservative was added to this same solution. and 0.1 mL of 0.1 N sodium hydroxide to adjust to pH 7.0.
  • Fluticasone 4.5 mg was dissolved with 0.3 mL of polyethylene glycol 400 and 0.70 mL benzylbenzoate, 0.03 mL of polysorbate 20 as a surface active agent, 1 mg of mannitol to adjust osmolarity, 0.01 mL of benzalkonium chloride as preservative was added to this same solution. and 0.3 mL of 0.1 N sodium hydroxide to adjust to pH 7.2. All raw materials used were pharmaceutical grade.
  • dioctyl sodium sulfosuccinate as a surfactant
  • 1 mg of dextrose to adjust osmolarity
  • 0.02 mg of propylparaben as a preservative
  • 0.03 mL of 0.1 N maleic acid to adjust to pH 7.2.
  • Budesonide 0.5 mg was dissolved with 0.15 mL of polyethylene glycol 3350 and 0.85 mL of water, 0.1 mL of sodium dioctyl sulfosuccinate as a surface active agent, 2 mg of dextrose to adjust osmolarity, 0.01 mg of propylparaben as preservative were added to this solution. and 0.01 mL of 0.1 N maleic acid to adjust to pH 7.0.
  • Budesonide was dissolved with 0.45 mL of polyethylene glycol 3350 and 0.55 mL water, 0.05 mL of sodium dioctyl sulphosuccinate as a surface active agent, 0.5 mg of dextrose to adjust osmolarity, 0.02 mg of propylparaben as preservative were added to this solution. and 0.04 mL of 0.1 N maleic acid to adjust to pH 6.0.
  • Ipratropium bromide 0.5 mg was dissolved with 0.25 mL of glycine and 0.5 mL of polyethylene glycol 300, to this same solution was added, 0.3 mL of polyoxyethylated castor oil as a surface active agent, 0.5 mg of glycerin to adjust osmolarity, 0.1 mg of methylparaben as conservative and 0.3 mL of 0.1 N maleic acid to adjust to pH 6.7
  • Ipratropium bromide 1.0 mg was dissolved with 0.35 mL of glycine and 0.65 mL polyethylene glycol 300, this same solution was given added, 0.03 mL polyoxyethylated castor oil as a surface active agent, 1.0 mg of glycerin to adjust osmolarity, 0.01 mg of methylparaben as a preservative and 0.2 mL of 0.1 N maleic acid to adjust to pH 6.7
  • Ipratropium bromide with 0.5 mL of glycine and 0.5 mL polyethylene glycol 300 were dissolved, 0.05 mL polyoxyethylated castor oil as a surface active agent, 1.5 mg of glycerin to adjust osmolarity, 0.03 mg of methylparaben as added to this same solution conservative and 0.1 mL of 0.1 N maleic acid to adjust to pH 7.3.
  • 0.2 mg salmeterol Xinafoate was dissolved with 0.5 mL of water and 0.2 mL polyethylene glycol 400, 0.03 mL polysorbate 80 was added to this same solution as a surface active agent, 0.1 mg of sodium chloride, 0.05 mg of propylparaben as a 0.25 mL preservative of 1 N hydrochloric acid to adjust to pH 6.7.
  • polysorbate 80 as a surface active agent, 0.1 mg of sodium chloride, 0.01 mg of propylparaben as a preservative 0.15 mL of hydrochloric acid 1
  • Salmeterol Xinafoate 4.0 mg was dissolved with 0.2 mL of water and 0.8 mL polyethylene glycol 400, 0.05 mL polysorbate 80 was added to this same solution as a surface active agent, 3.0 mg of sodium chloride, 0.06 mg of propylparaben as a 0.1 mL preservative of 1 N hydrochloric acid to adjust to pH 5.0.
  • Example 19 of the preparation of an inhalable pharmaceutical composition for the treatment of asthma for administration by air via an aerosol emulation sucker 2.0 mg of Formoterol fumarate with 0.3 mL of propylene glycol and 0.7 mL of water were dissolved, 0.02 mL of polysorbate 80 as a surface active agent, 0.03 mL of propylparaben as a preservative and 0.15 mL of 1 N hydrochloric acid were added to this solution. to adjust to pH 7.3.
  • Terbutaline 0.25 mg was dissolved with 0.25 mL of polyethylene glycol 3350 and 0.25 mL water, 0.03 mL of sodium dioctyl sulfosuccinate as a surface active agent, 2 mg of water were added to this same solution. Na Cl to adjust osmolarity, 0.03 mg of propylparaben as a preservative and 0.03 mL of 0.1 N maleic acid to adjust to pH 7.2.
  • Terbutaline 0.5 mg was dissolved with 0.15 mL of polyethylene glycol 3350 and 0.85 mL of water, 0.01 mL of sodium dioctyl sulfosuccinate as a surfactant, 1 mg of Na Cl to adjust osmolarity, 0.02 mg of propylparaben as added to this same solution conservative and 0.01 mL of 0.1 N maleic acid to adjust to pH 6.5.
  • Terbutaline 1.0 mg was dissolved with 0.45 mL of polyethylene glycol 3350 and 0.55 mL water, 0.02 mL of dioctyl sodium sulfosuccinate as a surface active agent, 0.5 mg of Na Cl to adjust osmolarity, 0.01 mg of propylparaben as added to this same solution conservative and 0.02 mL of 0.1 N maleic acid to adjust to pH 7.1.
  • Ciclesonide 0.1 mg was dissolved with 0.5 mL of glycine and
  • Ciclesonide 0.5 mg was dissolved with 0.3 mL of glycine and
  • Ciclesonide 2 mg was dissolved with 0.4 mL of glycine and 0.6 mL polyethylene glycol 300, 0.01 mL polyoxyethylated castor oil as a surfactant, 0.2 mg of NaCl to adjust osmolarity, 0.04 mg of methylparaben as preservative and 0.03 mL of 0.1 N maleic acid to adjust to pH of this solution were added 7.0.
  • This electronic device for the administration of an inhalable pharmaceutical composition for the treatment of asthma is based on the invention described in patent application MX2008013527, which is an aerosol emulation sucker; It consists of the following parts: a body with battery, electronic circuits and sensors inside; a nebulizer, a heating element that is inside the nebulizer chamber, a liquid container and a nozzle to assemble the liquid container to the body with the battery, electronic circuits and sensors. This device will be used to administer the pharmaceutical compositions described herein.

Abstract

La présente invention concerne une composition pharmaceutique inhalable utilisée pour le traitement de l'asthme qui contient, en tant que principe actif, du salbutamol ainsi que des excipients tels qu'un agent tensio-actif, un agent isosmotique, un diluant, un agent viscosant, un conservateur et un agent d'ajustement du pH.
PCT/MX2011/000148 2010-12-21 2011-12-02 Composition pharmaceutique inhalable utilisée pour le traitement de l'asthme, administrable par les voies aériennes au moyen d'un dispositif d'aspiration entraînant l'aérosol WO2012087094A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
MXMX/A/2011/000068 2010-12-21
MX2011000068 2010-12-21

Publications (1)

Publication Number Publication Date
WO2012087094A1 true WO2012087094A1 (fr) 2012-06-28

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Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2085468T3 (es) * 1990-01-05 1996-06-01 Sepracor Inc Albuterol r(-) opticamente puro para tratar el asma.
WO2004022132A2 (fr) * 2002-09-05 2004-03-18 Collegium Pharmaceutical, Inc. Systeme d'administration de produits pharmaceutiques pour inhalation orale par nebulisation, compose d'un substrat impregne d'une ou plusieurs substances a solubiliser ou a mettre en suspension avant utilisation
US20070183982A1 (en) * 2006-02-09 2007-08-09 Erhard Berkel Pharmaceutical composition for aerosols with two or more active substances and at least one surfactant
WO2007137204A2 (fr) * 2006-05-18 2007-11-29 Tika Läkemedel Ab Méthodes de distribution d'un agoniste bêta2 pour induire une bronchodilatation et formulations utilisées dans ces procédés

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2085468T3 (es) * 1990-01-05 1996-06-01 Sepracor Inc Albuterol r(-) opticamente puro para tratar el asma.
WO2004022132A2 (fr) * 2002-09-05 2004-03-18 Collegium Pharmaceutical, Inc. Systeme d'administration de produits pharmaceutiques pour inhalation orale par nebulisation, compose d'un substrat impregne d'une ou plusieurs substances a solubiliser ou a mettre en suspension avant utilisation
US20070183982A1 (en) * 2006-02-09 2007-08-09 Erhard Berkel Pharmaceutical composition for aerosols with two or more active substances and at least one surfactant
WO2007137204A2 (fr) * 2006-05-18 2007-11-29 Tika Läkemedel Ab Méthodes de distribution d'un agoniste bêta2 pour induire une bronchodilatation et formulations utilisées dans ces procédés

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
"Inhalacion of salbutamol", 6 July 2010 (2010-07-06), Retrieved from the Internet <URL:http://web.archive.org/web/20100706071450/http://www.nl...h.gov/medlineplus/spanish/druginfo/meds/a682145-es.html> [retrieved on 20120329] *
"Salbutamol", 23 November 2010 (2010-11-23), Retrieved from the Internet <URL:http://in.wikipedia.org/w/index.php?title=Salbutamol&oldid=398407396> [retrieved on 20120402] *
GONZALEZ BURCHARD E. ET AL.: "Lower bronchodilator responsiveness in Puerto Rican than in Mexican subjects with asthma", AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, vol. 169, no. 3, 14 November 2003 (2003-11-14), pages 386 - 392 *

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