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WO1993015715A1 - Preparations contenant de la lecithine presentees sous forme d'aerosols pour traiter l'asthme ou les affections pulmonaires - Google Patents

Preparations contenant de la lecithine presentees sous forme d'aerosols pour traiter l'asthme ou les affections pulmonaires Download PDF

Info

Publication number
WO1993015715A1
WO1993015715A1 PCT/EP1993/000201 EP9300201W WO9315715A1 WO 1993015715 A1 WO1993015715 A1 WO 1993015715A1 EP 9300201 W EP9300201 W EP 9300201W WO 9315715 A1 WO9315715 A1 WO 9315715A1
Authority
WO
WIPO (PCT)
Prior art keywords
dncg
fenoterol
salbutamol
preparation according
reproterol
Prior art date
Application number
PCT/EP1993/000201
Other languages
German (de)
English (en)
Inventor
Kurt H. Bauer
Gieselher Warnke
Original Assignee
IG Sprühtechnik GmbH
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 IG Sprühtechnik GmbH filed Critical IG Sprühtechnik GmbH
Publication of WO1993015715A1 publication Critical patent/WO1993015715A1/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
    • A61K9/008—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]

Definitions

  • the present invention relates to an aerosol preparation which, in addition to the customary antiasthmatic active ingredients, contains lecithins or phospholipids as auxiliaries, a process for producing aerosol cans which contain such aerosol preparations, and the use of these spray aerosols.
  • spray aerosols has been found to be particularly beneficial in the treatment of asthma, allergic bronchitis and other respiratory diseases. They have proven particularly useful in the treatment of shortness of breath.
  • the patient With a spray directed into the mouth opening, the patient can administer a relatively precisely metered amount of the active substance (s), which is finely atomized as an aerosol, the active substances being held in the mouth and throat, or in the trachea, the bronchi, depending on the particle size and finally get into the alveoli.
  • active substance s
  • Anti-asthmatic aerosol preparations usually contain one or more active ingredients as a suspension in micronized form, but also in dissolved form. If lecithins are added to the aerosol preparations in addition to the active ingredients, liposomes which are friendly to lung tissue and mucous membranes and which contain the active ingredient are formed when sprayed. Various problems arise in aerosol preparations of this type which are formulated as propellants using the physiologically inert, non-flammable and therefore particularly preferred in such cases.
  • the aerosol preparation is in the form of a heterogeneous dispersion, for example suspension, emulsion or a mixture of these two systems, because of the poor water solubility of these propellant gases. If an active ingredient is neither soluble in water nor in the propellant gases, then it is emulsified or suspended in this preparation and not dissolved available. In order to prevent inhomogeneity in the application, sufficient shaking of the aerosol must be ensured by intensive shaking before each inhalation. The fineness of such emulsions or the suspensions or the suspended particles not only determines the dosing accuracy, but also the pulmonary gait and thus the therapeutic effectiveness to a decisive degree.
  • the object of the invention is to eliminate the disadvantages of these spray aerosols known from the prior art.
  • a practically clear, homogeneous, colloidal or molecularly disperse solution should therefore preferably be provided.
  • substances such as middle-chain triglycerides (eg miglyol, myritol), fatty acid esters of lower alcohols (eg isopropyl myristate, isopropyl stearate, ethyl oleate) and partially acetylated glycerides (eg lauryl acetylglyceride), preferably a lipophilic or castor oil or preferably a castor oil or castor oil, can also be used as absorption promoters and as lipophilic solvents Agent, for example Tween 80 (Polysorbate 80) or Tween 20 (Polysorbate 20), Span or Arlacel 20 (Sorbitan fatty acid ester), triacetin, DMSO, PEG, glycerol fatty acid ester or the like in
  • the aerosol preparations according to the invention can also contain cholesterol and / or tocopoferol.
  • Another advantage of the aerosol preparations according to the invention is that the use of dimethyl ether instead of the CFC propellants also improves the environmental compatibility of the sprays.
  • the aerosol preparations according to the invention can be composed, for example, as follows:
  • a typical preparation of the aerosol solution according to the invention is composed as follows:
  • beclo ethasone (0.1-1.0%), budesonide (0.1-1.0%), DNCG (1.0-5.0%), fenoterol (0 , 1-1.0%), ipratropium bromide (0.05-0.5%), salbutamol (0.2-1.0%), reproterol (0.5-2.5%) and terbutaline (1.0 -2.5%).
  • beclomethasone and salbutamol, DNCG and fenoterol, DNCG and reproterol, DNCG and salbutamol or fenoterol and ipratropium bromide can also be used advantageously.
  • difatty acid phosphatidylcholines difatty acid phosphatidylglycerol, dipalmitoylphosphatidylcholine and stearoylpalmitoylphosphatidylglycerol can also be used.
  • a predetermined fill weight e.g. 3 grams of this preparation (solution) are filled through the valve of an airtight sealed (crimped) aerosol can in compliance with the prescribed filling accuracy.
  • the liquefied dimethyl ether is then introduced through the valve under pressure.
  • the amount of dimethyl ether to be refilled depends on the target weight. It can be between 50 to 300 percent by weight of the amount of filler.
  • the amount of diethyl ether is advantageously between 100 and 200 percent by weight per amount of filler.
  • the weight ratio between active ingredient solution and dimethyl ether is consequently between 1: 0.5 and 1: 3, preferably between 1: 1 and 1: 2.

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Otolaryngology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une préparation présentée sous forme d'aérosol qui contient, outre les substances antiasthmatiques habituelles, de la lécithine ou des phospholipides. L'invention concerne également un procédé de fabrication de conditionnements contenant des préparations présentées sous forme d'aérosol de ce type, ainsi que l'utilisation de ces aérosols de pulvérisation.
PCT/EP1993/000201 1992-02-06 1993-01-29 Preparations contenant de la lecithine presentees sous forme d'aerosols pour traiter l'asthme ou les affections pulmonaires WO1993015715A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP4203306.3 1992-02-06
DE19924203306 DE4203306A1 (de) 1992-02-06 1992-02-06 Asthma oder pulmonal-aerosolzubereitungen mit lecithin

Publications (1)

Publication Number Publication Date
WO1993015715A1 true WO1993015715A1 (fr) 1993-08-19

Family

ID=6451026

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1993/000201 WO1993015715A1 (fr) 1992-02-06 1993-01-29 Preparations contenant de la lecithine presentees sous forme d'aerosols pour traiter l'asthme ou les affections pulmonaires

Country Status (2)

Country Link
DE (1) DE4203306A1 (fr)
WO (1) WO1993015715A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995024892A1 (fr) * 1994-03-14 1995-09-21 Abbott Laboratories Formule d'un aerosol medicamenteux contenant de la vitamine e
EP0959874A4 (fr) * 1996-07-03 1999-12-22
US6491897B1 (en) 1995-06-27 2002-12-10 Boehringer Ingelheim Kg Stable pharmaceutical budesonide preparation for producing propellant-free aerosols
EP1438955A1 (fr) * 1996-07-03 2004-07-21 Research Development Foundation Formulations d'un aérosol à liposomes fortement dosés
KR100497564B1 (ko) * 1996-07-03 2005-11-28 리써치 디벨롭먼트 파운데이션 고용량의리포좀에어로졸제제

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2436537C (fr) * 2000-10-31 2009-05-26 Boehringer Ingelheim Pharma Gmbh & Co. Kg Nouvelles compositions pharmaceutiques
DE10062712A1 (de) * 2000-12-15 2002-06-20 Boehringer Ingelheim Pharma Neue Arzneimittelkompositionen auf der Basis von Anticholinergika und Corticosteroiden
MXPA03003750A (es) * 2000-10-31 2004-10-15 Boehringer Ingelheim Pharma Formulacion de una solucion de inhalacion con una sal de tiotropio.
US20020137764A1 (en) 2000-10-31 2002-09-26 Karin Drechsel Inhalable formulation of a solution containing a tiotropium salt
US7776315B2 (en) 2000-10-31 2010-08-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and additional active ingredients
DE10347994A1 (de) 2003-10-15 2005-06-16 Pari GmbH Spezialisten für effektive Inhalation Wässrige Aerosol-Zubereitung
EP1712220A1 (fr) * 2005-04-15 2006-10-18 PARI GmbH Spezialisten für effektive Inhalation Composition d'aérosol pharmaceutique

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2410036A1 (fr) * 1977-11-25 1979-06-22 Schwarzkopf Gmbh Hans Preparation aerosol maintenue sous pression
GB2196254A (en) * 1984-04-13 1988-04-27 Fisons Plc Nedocromil sodium formation
WO1990007469A1 (fr) * 1988-12-29 1990-07-12 Benson Bradley J Administration par voie pulmonaire de substances pharmaceutiquement actives
WO1991011495A1 (fr) * 1990-02-03 1991-08-08 Boehringer Ingelheim Kg Nouveaux melanges de gaz propulseurs et leur utilisation dans des preparations medicamenteuses

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2849591C2 (de) * 1978-11-15 1982-04-01 Hans Schwarzkopf Gmbh, 2000 Hamburg Sicher zu transportierende Dimethyläther-Zubereitungen, Verfahren zu ihrer Herstellung sowie ihre Verwendung
US4371451A (en) * 1982-02-10 1983-02-01 Frank Scotti Lecithin containing surface release compositions
GB8322178D0 (en) * 1983-08-17 1983-09-21 Sterwin Ag Preparing aerosol compositions
DE3340991A1 (de) * 1983-11-12 1985-05-23 Hefa-Frenon Arzneimittel GmbH & Co KG, 4712 Werne Verwendung von dimethylether als treib- und loesungsmittel
DE3815221C2 (de) * 1988-05-04 1995-06-29 Gradinger F Hermes Pharma Verwendung einer Retinol- und/oder Retinsäureester enthaltenden pharmazeutischen Zubereitung zur Inhalation zur Einwirkung auf die Schleimhäute des Tracheo-Bronchialtraktes einschließlich der Lungenalveolen

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2410036A1 (fr) * 1977-11-25 1979-06-22 Schwarzkopf Gmbh Hans Preparation aerosol maintenue sous pression
GB2196254A (en) * 1984-04-13 1988-04-27 Fisons Plc Nedocromil sodium formation
WO1990007469A1 (fr) * 1988-12-29 1990-07-12 Benson Bradley J Administration par voie pulmonaire de substances pharmaceutiquement actives
WO1991011495A1 (fr) * 1990-02-03 1991-08-08 Boehringer Ingelheim Kg Nouveaux melanges de gaz propulseurs et leur utilisation dans des preparations medicamenteuses

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995024892A1 (fr) * 1994-03-14 1995-09-21 Abbott Laboratories Formule d'un aerosol medicamenteux contenant de la vitamine e
US6491897B1 (en) 1995-06-27 2002-12-10 Boehringer Ingelheim Kg Stable pharmaceutical budesonide preparation for producing propellant-free aerosols
US8062626B2 (en) 1995-06-27 2011-11-22 Boehringer Ingelheim Kg Stable pharmaceutical budesonide preparation for producing propellant-free aerosols
EP0959874A4 (fr) * 1996-07-03 1999-12-22
EP1438955A1 (fr) * 1996-07-03 2004-07-21 Research Development Foundation Formulations d'un aérosol à liposomes fortement dosés
KR100497564B1 (ko) * 1996-07-03 2005-11-28 리써치 디벨롭먼트 파운데이션 고용량의리포좀에어로졸제제

Also Published As

Publication number Publication date
DE4203306A1 (de) 1993-08-12

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