CH668188A5 - Corticosteroid ointment compsns. - comprise e.g. dexamethasone in poly:alkylene glycol base, and are used esp. for treating rhinitis - Google Patents

Corticosteroid ointment compsns. - comprise e.g. dexamethasone in poly:alkylene glycol base, and are used esp. for treating rhinitis Download PDF

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Publication number
CH668188A5
CH668188A5 CH231686A CH231686A CH668188A5 CH 668188 A5 CH668188 A5 CH 668188A5 CH 231686 A CH231686 A CH 231686A CH 231686 A CH231686 A CH 231686A CH 668188 A5 CH668188 A5 CH 668188A5
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Switzerland
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ointment
characterized
polyethylene glycol
nasal
ointment base
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CH231686A
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German (de)
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Franz Rappai
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Franz Rappai
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0043Nose

Abstract

Ointment compsns., esp. for treating allergic and vasomotor rhinitis, contain (a) at least one steroid (I) of the 16-methyl-1,4-pregnadiene-3,20-dione series and (b) an ointment base comprising mainly a physiologically acceptable component (II) which is liq. or semi-liq. at body temp. and is capable of reducing surface tension. (I) is pref. dexamethasone (Ia) or its derivs., e.g. the t-butyl acetate, or beclomethasone (Ib) or its derivs., e.g. the 21-acetate or dipropionate. (II) is a polyalkylene glycol, esp. a polyethylene glycol (PEG) mixt., opt. mixed with a higher fatty alcohol. The compsns. may also contain preservatives and/or NaCl. ADVANTAGE - Unlike conventional nasal sprays, the ointments do not cause drying of the nasal mucosa.

Description


  
 

 **WARNUNG** Anfang DESC Feld konnte Ende CLMS uberlappen **. ** WARNING ** start DESC field could overlap the end of CLMS **.

 



       PATENTANSPRÜCHE   
 1. Mittel in Salbenform, insbesondere zur Behandlung von allergischen und vasomotorischen Rhinitiden, dadurch gekennzeichnet, dass es mindestens eine Steroidverbindung der 16-Methylpregna-1,4-dien-3,20-dion-Reihe und eine Salbengrundlage, welche zur Hauptsache aus einer bei Körpertemperatur flüssigen oder halbflüssigen, die Oberflächenspannung herabsetzenden, physiologisch annehmbaren Komponente besteht, enthält. 1. A composition in ointment form, in particular for the treatment of allergic and vasomotor rhinitis, characterized in that it comprises at least one steroid compound of 16-methylpregna-1,4-diene-3,20-dione series and an ointment base, which mainly of a is at body temperature liquid or semi-liquid, the surface tension reducing physiologically acceptable component contains.



    2. Mittel nach Patentanspruch 1, dadurch gekennzeichnet, dass die Salbengrundlage zur Hauptsache aus Polyalkylenglykolen besteht. 2. The composition according to claim 1, characterized in that the ointment base consists mainly of polyalkylene glycols.



    3. Mittel nach Patentanspruch 1 oder 2, dadurch gekennzeichnet, dass die Polyalkylenglykole aus einem Gemisch von Polyäthylenglykolen von verschiedenem Molekulargewicht bestehen. 3. The composition according to claim 1 or 2, characterized in that the polyalkylene glycols of a mixture of polyethylene glycols of various molecular weight exist.



    4. Mittel nach einem der Patentansprüche 1 bis 3, dadurch gekennzeichnet, dass die Salbengrundlage ausserdem mindestens einen höheren Fettalkohol wie zB Cetylalkohol und/oder Stearylalkohol enthält. 4. Composition according to one of the claims 1 to 3, characterized in that the ointment base also contains at least one higher fatty alcohol such as cetyl alcohol and / or stearyl alcohol.



    5. Mittel nach einem der Patentansprüche 1 bis 4, dadurch gekennzeichnet, dass es ausserdem ein Konservierungsmittel enthält, zB ein Salz- oder einen Ester der Benzoesäure. 5. Agent according to one of the claims 1 to 4, characterized in that it further comprises a preservative, for example, a salt or an ester of benzoic acid.



    6. Mittel nach einem der Patentansprüche 1 bis 5, dadurch gekennzeichnet, dass es ausserdem Natriumchlorid, vorzugsweise in Form von Meersalz, enthält. 6. A composition according to any one of the claims 1 to 5, characterized in that it is preferably in the form of sea salt further comprises sodium chloride.



    7. Mittel nach einem der Patentansprüche 1 bis 6, dadurch gekennzeichnet, dass es als Wirkstoff 9-Fluor 1113, 17,21-trihydroxy-16z-methylpregna- 1 ,4-dien-3,20-dion oder einen Ester davon, zB das tert.-Butylacetat, enthält. 7. Composition according to one of the claims 1 to 6, characterized in that it contains as active ingredient 9-fluoro 1113, 17,21-trihydroxy-16z-methylpregna-1, 4-diene-3,20-dione or an ester thereof, for example contains the tertiary butyl acetate.



    8. Mittel nach einem der Patentansprüche 1 bis 6, dadurch gekennzeichnet, dass es als Wirkstoff 9-Chlor -11 1 7,21-trihydroxy- 1 613-methylpregna-l ,4-dien-3,20-dion oder dessen Ester, zB das 21-Acetat oder das Dipropionat, enthält. 8. Composition according to one of the claims 1 to 6, characterized in that it contains as active ingredient 9-Chloro -11 1 7,21-trihydroxy-1 613 methylpregna-l, 4-diene-3,20-dione or its esters, for example, the 21-acetate or the dipropionate contains.



    BESCHREIBUNG DESCRIPTION



    Die Erfindung betrifft ein Mittel in Salbenform, insbesondere zur Behandlung von allergischen und vasomotorischen Rhinitiden, dessen wesentliche Bestandteile ein oder mehrere Wirkstoffe der 16-Methylpregna-1,4-dien-3,20dion-Reihe sowie eine Salbengrundlage auf der Basis von bei Körpertemperatur flüssigen oder halbflüssigen, die Oberflächenspannung herabsetzenden Verbindungen sind. The invention relates to a composition in ointment form, in particular for the treatment of allergic and vasomotor rhinitis, whose essential components liquid, one or more active ingredients of the 16-methylpregna-1,4-dien-3,20dion series and an ointment base based on at body temperature or semi-liquid, the surface tension releasing compounds are reduced.



    Die als Wirkstoffe verwendeten Corticosteroide üben eine ausgezeichnete antiallergische Wirkung auf die Nasenschleimhäute aus. The corticosteroids used as active ingredients exert an excellent anti-allergic effect on the nasal mucosa.  Bisher wurden sie zu diesem Zweck als Nasensprays eingesetzt, wobei sie aber eine sehr unangenehme und unerwünschte Austrocknung der Schleimhäute hervorriefen. So far, they have been used for this purpose as nasal sprays, but where they caused a very unpleasant and undesirable drying of the mucous membranes.



    Aufgabe der Erfindung war es daher, ein Mittel zu entwickeln, welches die positiven Wirkungen der Corticosteroide ohne das Austrocknen der Nasenschleimhäute erzielt. It is an object of the invention to develop an agent which achieves the positive effects of corticosteroids without drying out the nasal mucous membranes.



    Das erfindungsgemässe Mittel ist in Patentanspruch 1 definiert. The inventive agent is defined in claim. 1



    Das erfindungsgemässe Mittel bekämpft mit Hilfe der Corticosteroide insbesondere die unten genannten Krankheitssymptome. The inventive means fights in particular the symptoms listed below with the help of corticosteroids.  Durch die spezielle Salbengrundlage bleibt die Wirkung der Corticosteroide voll erhalten und gleichzeitig bleiben überraschenderweise die Schleimhäute während der Entfaltung der Wirkung feucht. The special ointment base the effect of corticosteroids is fully maintained and surprisingly the mucous membranes while remaining moist during deployment of the effect.  Die austrocknende Nebenwirkung der Corticosteroide wird durch die befeuchtende Wirkung der Salbengrundlage aufgehoben. The drying side effect of corticosteroids is canceled by the moisturizing effect of the ointment base.  Dadurch bleiben die physiologischen Zustände der Schleimhäute erhalten, was mit wässerigen Präparaten nicht immer der Fall ist. Thus, the physiological conditions of the mucous membranes remain intact, which is the case with aqueous preparations not always.



    Als Hauptbestandteil der Salbengrundlage dient eine bei Körpertemperatur flüssige oder halbflüssige die Oberflächenspannung herabsetzende Komponenente, die selbstverständlich physiologisch annehmbar sein muss. As a main component of the ointment base is a liquid at body temperature or semi-liquid, the surface tension-reducing serves Komponenente that must be physiologically acceptable, of course.  Verbindungen dieser Art, die allein oder im Gemisch verwendet werden können, sind z. Compounds of this type which can be used alone or in a mixture, z are.  B. Polyalkylenglykole, insbesondere Poly äthylenglykole. , Polyalkylene glycols, especially poly ethylene glycols.  Eine besonders bevorzugte Komponente besteht aus einem Gemisch von Polyäthylenglykolen von verschiedenem Molekulargewicht, zB Polyäthylenglykol 600, Polyäthylenglykol 1000, Polyäthylenglykol 2000, Polyäthylenglykol 3000 und Polyäthylenglykol 5000, die in verschiedenen Gemischen von zwei oder mehr Komponenten und in verschiedenen Mengenverhältnissen miteinander vermischt werden können. A particularly preferred component is a mixture of polyethylene glycols of different molecular weight, for example polyethylene glycol 600, polyethylene glycol 1000, polyethylene glycol 2000, polyethylene glycol 3000 and polyethylene glycol 5000, which can be mixed together in various mixtures of two or more components, and in various proportions.



    Es hat sich ferner als vorteilhaft erwiesen, der Salbe weitere, für Nasensalben bekannte Zusätze beizufügen, zB It has also proven to be advantageous for the ointment further to include additives known for nasal ointments, for example,



   Verbindungen mit einer gewissen Schmierwirkung, wie höhere Fettalkohole; Compounds having a certain lubricating effect, such as higher fatty alcohols;  Kochsalz, insbesondere in Form von Meersalz, sowie Konservierungsmittel, z. Sodium chloride, particularly in the form of sea salt, and preservatives, such.  B. Benzoesäuresalze oder -ester. As benzoic acid salts or esters.



    Als Wirkstoffe eignen sich bekannte Verbindungen der 16-Methyl-pregna-1,4-dien-3,20-dion-Reihe wie Dexamethason und Beclomethason und deren Derivate, insbesondere deren Ester. As active ingredients are known compounds of the 16-methyl-pregna-1,4-diene-3,20-dione series, such as dexamethasone and beclomethasone, and their derivatives, especially their esters are suitable.



    Geeignete Wirkstoffkonzentrationen liegen im allgemeinen bei etwa 0,1 - 2 Gew.%. Suitable drug concentrations are generally from about 0.1 to 2 wt.%.



    Patienten, welche auf Pollen oder andere Substanzen allergisch reagieren, leiden jährlich und in ständig steigendem Masse an den Folgen dieser Allergien mit Nasentropfen, tränenden und geschwollenen Augen, etc. In extremen Fällen sind diese Patienten so stark behindert, dass Arbeitsunfähigkeit auftritt. Patients who are allergic to pollen or other substances suffer annually and in ever increasing extent from the effects of these allergies with nasal drops, watery and swollen eyes, etc., these patients are so severely disabled that disability occurs in extreme cases.  Viele dieser Patienten werden mit Medikamenten behandelt, die als unerwünschte Nebenwirkung die Schleimhäute austrocknen lassen. Many of these patients are treated with drugs that can dry up as an unwanted side effect of the mucous membranes.  Dies wird durch das erfindungsgemässe Mittel verhindert. This is prevented by the inventive means.  Eine weitere Patientengruppe leidet an vasomotorischen Rhinitiden, deren Symptome den allergischen Rhinitiden ähnelt. Another group of patients suffering from vasomotor rhinitis whose symptoms similar to allergic rhinitis.



    Es besteht daher auch hier die Notwendigkeit, diese unangenehmen Symptome mit einem geeigneten Mittel zu behandeln, dessen Nebenwirkungen auf ein Minimum reduziert sind, was mit dem erfindungsgemässen Mittel auf einfache Weise ermöglicht wird. Therefore, there is also the need to treat these uncomfortable symptoms with an appropriate agent whose side effects are reduced to a minimum, which is made possible with the invention agent easily.  Durch die spezielle Salbengrundlage, zB auf Polyalkylenglykol-Basis, werden die Nebenwirkungen der Wirkstoffe aufgehoben und eine optimale Behandlung ist gewährleistet. Due to the special ointment base, eg polyalkylene glycol base, the side effects of the active compounds are released and an optimum treatment is ensured.



    Mit Hilfe dieses erfindungsgemässen Mittels wird die Austrocknung der Nasenschleimhäute erfolgreich verhindert und Erkrankungen, wie z. With the help of this inventive agent, the drying of the nasal mucosa is successfully prevented and diseases such.  B. Rhinitis allergica und vasomotorica, können innert kurzer Zeit erfolgreich behandelt werden, so dass nach wenigen Minuten schon subjektiv und objektiv eine wesentliche Besserung des Zustandes des Patienten festgestellt werden kann. As allergic and vasomotor rhinitis, within a short time can be successfully treated, so that even subjectively and objectively a significant improvement of the patient's condition can be detected after a few minutes.



    Nachstehend wird die Erfindung durch zwei Beispiele näher erläutert. The invention is further illustrated by two examples.



    Beispiel 1 example 1
 Aus den folgenden Bestandteilen wurde auf übliche Weise eine Nasensalbe hergestellt: Polyäthylenglykol 600 40 g Polyäthylenglykol 2000 20 g Cetylalkohol 10 g Sorbitol 5g Meersalz (NaCl + Spurenelemente) 1,3 g Methylparabenzoat 0,1 g Wasser 22,6 g Dexamethason (9-Fluoro- 1113,17,21 -tri- hydroxy- 1 6a-methylpregna- 1 ,4-dien- 3,20-dion) oder dessen Derivate, wie z. 40 g of polyethylene glycol 600 Polyethylene glycol 2000 20 g Cetyl alcohol 10 g sorbitol 5 g of sea salt (NaCl + trace elements) 1.3 g 0.1 g Water 22.6 g Methylparabenzoat dexamethasone (9-Fluoro: From the following components, a nasal ointment was prepared in usual manner - 1113,17,21 tri- hydroxy-1 6a-methylpregna-1, 4-diene-3,20-dione) or its derivatives, such as.  B. B.

   Dexamethason-tert.-butylacetat, etc. 1 g Dexamethasone tert.-butyl acetate, etc. 1 g
 100 g 100 g
 Beispiel 2 example 2
 Die folgenden Bestandteile wurden zu einer Nasensalbe verarbeitet: Wasser 25,2 g Polyäthylenglykol 600 30 g Polyäthylenglykol 1000 10 g Polyäthylenglykol 3000 10 g Polyäthylenglykol 5000 10 g Stearylalkohol 10 g Meersalz (NaCl + Spurenelemente) 0,6 g Sorbitol 4g Beclomethason (9-Chlor-l Iss,17,21-tri- hydroxy- 1 6ss-methylpregna- 1 ,4-dien- 3;20-dion) oder dessen Derivate, wie zB Beclomethason-21-acetat und Beclomethason-dipropionat 0,2 g The following ingredients were processed to a nasal ointment: Water 25.2 g Polyethylene glycol 600 30 g Polyethylene glycol 1000 10 g Polyethylene glycol 3000 10 g Polyethylene glycol 5000 10 g Stearyl alcohol 10 g sea salt (NaCl + trace elements) 0.6 g Sorbitol 4g beclomethasone (9-chloro Iss -l, 17,21-tri- hydroxy-1 6ss-methylpregna-1, 4-diene-3, 20-dione) or its derivatives, such as beclomethasone 21-acetate and beclomethasone dipropionate 0.2 g
 100 g 100 g
 Zur Anwendung des erfindungsgemässen Mittels wird es in geeigneten Zeitabständen auf die Nasenschleimhäute aufgetragen. For the application of the invention agent is applied at appropriate intervals on the nasal mucosa. 

   Zur Erzielung des gewünschten Effektes werden im allgemeinen Salbenmengen aufgetragen, die 10 bis 1000 mg Reinwirkstoff pro Applikation entsprechen. To achieve the desired effect, ointment amounts are generally applied corresponding to 10 to 1000 mg of pure active ingredient per application.



    Zur Applikation der Salbe geeignete Vorrichtungen, die auf dem Markt erhältlich sind, sind verlängerte Tubenkanülen oder Tubenöffnungen, die in die Nasenöffnungen eingeführt werden. For application of the ointment suitable devices that are available on the market, are elongated tubes cannulas or tube openings, which are introduced into the nostrils.  Das Mittel kann gegebenenfalls auch mit dem Finger oder einem Wattestäbchen auf die Nasenschleimhäute appliziert werden. The agent may optionally be applied with the fingers or a cotton swab to the nasal membranes.  Die Anwendung kann bei Bedarf mehrmals und über längere Zeit wiederholt werden, ohne dass unerwünschte Nebenwirkungen auftreten, wie klinische Versuche an Menschen gezeigt haben. The application can if necessary several times and for a long time be repeated without adverse side effects, as demonstrated by clinical tests on humans. 

Claims (8)

  1. PATENTANSPRÜCHE 1. Mittel in Salbenform, insbesondere zur Behandlung von allergischen und vasomotorischen Rhinitiden, dadurch gekennzeichnet, dass es mindestens eine Steroidverbindung der 16-Methylpregna-1,4-dien-3,20-dion-Reihe und eine Salbengrundlage, welche zur Hauptsache aus einer bei Körpertemperatur flüssigen oder halbflüssigen, die Oberflächenspannung herabsetzenden, physiologisch annehmbaren Komponente besteht, enthält. CLAIMS 1. A composition in ointment form, in particular for the treatment of allergic and vasomotor rhinitis, characterized in that it comprises at least one steroid compound of 16-methylpregna-1,4-diene-3,20-dione series and an ointment base, which mainly of is a liquid at body temperature or semi-liquid, the surface tension reducing physiologically acceptable component contains.
  2. 2. Mittel nach Patentanspruch 1, dadurch gekennzeichnet, dass die Salbengrundlage zur Hauptsache aus Polyalkylenglykolen besteht. 2. The composition according to claim 1, characterized in that the ointment base consists mainly of polyalkylene glycols.
  3. 3. Mittel nach Patentanspruch 1 oder 2, dadurch gekennzeichnet, dass die Polyalkylenglykole aus einem Gemisch von Polyäthylenglykolen von verschiedenem Molekulargewicht bestehen. 3. The composition according to claim 1 or 2, characterized in that the polyalkylene glycols of a mixture of polyethylene glycols of various molecular weight exist.
  4. 4. Mittel nach einem der Patentansprüche 1 bis 3, dadurch gekennzeichnet, dass die Salbengrundlage ausserdem mindestens einen höheren Fettalkohol wie zB Cetylalkohol und/oder Stearylalkohol enthält. 4. Composition according to one of the claims 1 to 3, characterized in that the ointment base also contains at least one higher fatty alcohol such as cetyl alcohol and / or stearyl alcohol.
  5. 5. Mittel nach einem der Patentansprüche 1 bis 4, dadurch gekennzeichnet, dass es ausserdem ein Konservierungsmittel enthält, zB ein Salz- oder einen Ester der Benzoesäure. 5. Agent according to one of the claims 1 to 4, characterized in that it further comprises a preservative, for example, a salt or an ester of benzoic acid.
  6. 6. Mittel nach einem der Patentansprüche 1 bis 5, dadurch gekennzeichnet, dass es ausserdem Natriumchlorid, vorzugsweise in Form von Meersalz, enthält. 6. A composition according to any one of the claims 1 to 5, characterized in that it is preferably in the form of sea salt further comprises sodium chloride.
  7. 7. Mittel nach einem der Patentansprüche 1 bis 6, dadurch gekennzeichnet, dass es als Wirkstoff 9-Fluor 1113, 17,21-trihydroxy-16z-methylpregna- 1 ,4-dien-3,20-dion oder einen Ester davon, zB das tert.-Butylacetat, enthält. 7. Composition according to one of the claims 1 to 6, characterized in that it contains as active ingredient 9-fluoro 1113, 17,21-trihydroxy-16z-methylpregna-1, 4-diene-3,20-dione or an ester thereof, for example contains the tertiary butyl acetate.
  8. 8. Mittel nach einem der Patentansprüche 1 bis 6, dadurch gekennzeichnet, dass es als Wirkstoff 9-Chlor -11 1 7,21-trihydroxy- 1 613-methylpregna-l ,4-dien-3,20-dion oder dessen Ester, zB das 21-Acetat oder das Dipropionat, enthält. 8. Composition according to one of the claims 1 to 6, characterized in that it contains as active ingredient 9-Chloro -11 1 7,21-trihydroxy-1 613 methylpregna-l, 4-diene-3,20-dione or its esters, for example, the 21-acetate or the dipropionate contains.
    BESCHREIBUNG DESCRIPTION
    Die Erfindung betrifft ein Mittel in Salbenform, insbesondere zur Behandlung von allergischen und vasomotorischen Rhinitiden, dessen wesentliche Bestandteile ein oder mehrere Wirkstoffe der 16-Methylpregna-1,4-dien-3,20dion-Reihe sowie eine Salbengrundlage auf der Basis von bei Körpertemperatur flüssigen oder halbflüssigen, die Oberflächenspannung herabsetzenden Verbindungen sind. The invention relates to a composition in ointment form, in particular for the treatment of allergic and vasomotor rhinitis, whose essential components liquid, one or more active ingredients of the 16-methylpregna-1,4-dien-3,20dion series and an ointment base based on at body temperature or semi-liquid, the surface tension releasing compounds are reduced.
    Die als Wirkstoffe verwendeten Corticosteroide üben eine ausgezeichnete antiallergische Wirkung auf die Nasenschleimhäute aus. The corticosteroids used as active ingredients exert an excellent anti-allergic effect on the nasal mucosa. Bisher wurden sie zu diesem Zweck als Nasensprays eingesetzt, wobei sie aber eine sehr unangenehme und unerwünschte Austrocknung der Schleimhäute hervorriefen. So far, they have been used for this purpose as nasal sprays, but where they caused a very unpleasant and undesirable drying of the mucous membranes.
    Aufgabe der Erfindung war es daher, ein Mittel zu entwickeln, welches die positiven Wirkungen der Corticosteroide ohne das Austrocknen der Nasenschleimhäute erzielt. It is an object of the invention to develop an agent which achieves the positive effects of corticosteroids without drying out the nasal mucous membranes.
    Das erfindungsgemässe Mittel ist in Patentanspruch 1 definiert. The inventive agent is defined in claim. 1
    Das erfindungsgemässe Mittel bekämpft mit Hilfe der Corticosteroide insbesondere die unten genannten Krankheitssymptome. The inventive means fights in particular the symptoms listed below with the help of corticosteroids. Durch die spezielle Salbengrundlage bleibt die Wirkung der Corticosteroide voll erhalten und gleichzeitig bleiben überraschenderweise die Schleimhäute während der Entfaltung der Wirkung feucht. The special ointment base the effect of corticosteroids is fully maintained and surprisingly the mucous membranes while remaining moist during deployment of the effect. Die austrocknende Nebenwirkung der Corticosteroide wird durch die befeuchtende Wirkung der Salbengrundlage aufgehoben. The drying side effect of corticosteroids is canceled by the moisturizing effect of the ointment base. Dadurch bleiben die physiologischen Zustände der Schleimhäute erhalten, was mit wässerigen Präparaten nicht immer der Fall ist. Thus, the physiological conditions of the mucous membranes remain intact, which is the case with aqueous preparations not always.
    Als Hauptbestandteil der Salbengrundlage dient eine bei Körpertemperatur flüssige oder halbflüssige die Oberflächenspannung herabsetzende Komponenente, die selbstverständlich physiologisch annehmbar sein muss. As a main component of the ointment base is a liquid at body temperature or semi-liquid, the surface tension-reducing serves Komponenente that must be physiologically acceptable, of course. Verbindungen dieser Art, die allein oder im Gemisch verwendet werden können, sind z. Compounds of this type which can be used alone or in a mixture, z are. B. Polyalkylenglykole, insbesondere Poly äthylenglykole. , Polyalkylene glycols, especially poly ethylene glycols. Eine besonders bevorzugte Komponente besteht aus einem Gemisch von Polyäthylenglykolen von verschiedenem Molekulargewicht, zB Polyäthylenglykol 600, Polyäthylenglykol 1000, Polyäthylenglykol 2000, Polyäthylenglykol 3000 und Polyäthylenglykol 5000, die in verschiedenen Gemischen von zwei oder mehr Komponenten und in verschiedenen Mengenverhältnissen miteinander vermischt werden können. A particularly preferred component is a mixture of polyethylene glycols of different molecular weight, for example polyethylene glycol 600, polyethylene glycol 1000, polyethylene glycol 2000, polyethylene glycol 3000 and polyethylene glycol 5000, which can be mixed together in various mixtures of two or more components, and in various proportions.
    Es hat sich ferner als vorteilhaft erwiesen, der Salbe weitere, für Nasensalben bekannte Zusätze beizufügen, zB It has also proven to be advantageous for the ointment further to include additives known for nasal ointments, for example,
    Verbindungen mit einer gewissen Schmierwirkung, wie höhere Fettalkohole; Compounds having a certain lubricating effect, such as higher fatty alcohols; Kochsalz, insbesondere in Form von Meersalz, sowie Konservierungsmittel, z. Sodium chloride, particularly in the form of sea salt, and preservatives, such. B. Benzoesäuresalze oder -ester. As benzoic acid salts or esters.
    Als Wirkstoffe eignen sich bekannte Verbindungen der 16-Methyl-pregna-1,4-dien-3,20-dion-Reihe wie Dexamethason und Beclomethason und deren Derivate, insbesondere deren Ester. As active ingredients are known compounds of the 16-methyl-pregna-1,4-diene-3,20-dione series, such as dexamethasone and beclomethasone, and their derivatives, especially their esters are suitable.
    Geeignete Wirkstoffkonzentrationen liegen im allgemeinen bei etwa 0,1 - 2 Gew.%. Suitable drug concentrations are generally from about 0.1 to 2 wt.%.
    Patienten, welche auf Pollen oder andere Substanzen allergisch reagieren, leiden jährlich und in ständig steigendem Masse an den Folgen dieser Allergien mit Nasentropfen, tränenden und geschwollenen Augen, etc. In extremen Fällen sind diese Patienten so stark behindert, dass Arbeitsunfähigkeit auftritt. Patients who are allergic to pollen or other substances suffer annually and in ever increasing extent from the effects of these allergies with nasal drops, watery and swollen eyes, etc., these patients are so severely disabled that disability occurs in extreme cases. Viele dieser Patienten werden mit Medikamenten behandelt, die als unerwünschte Nebenwirkung die Schleimhäute austrocknen lassen. Many of these patients are treated with drugs that can dry up as an unwanted side effect of the mucous membranes. Dies wird durch das erfindungsgemässe Mittel verhindert. This is prevented by the inventive means. Eine weitere Patientengruppe leidet an vasomotorischen Rhinitiden, deren Symptome den allergischen Rhinitiden ähnelt. Another group of patients suffering from vasomotor rhinitis whose symptoms similar to allergic rhinitis.
    Es besteht daher auch hier die Notwendigkeit, diese unangenehmen Symptome mit einem geeigneten Mittel zu behandeln, dessen Nebenwirkungen auf ein Minimum reduziert sind, was mit dem erfindungsgemässen Mittel auf einfache Weise ermöglicht wird. Therefore, there is also the need to treat these uncomfortable symptoms with an appropriate agent whose side effects are reduced to a minimum, which is made possible with the invention agent easily. Durch die spezielle Salbengrundlage, zB auf Polyalkylenglykol-Basis, werden die Nebenwirkungen der Wirkstoffe aufgehoben und eine optimale Behandlung ist gewährleistet. Due to the special ointment base, eg polyalkylene glycol base, the side effects of the active compounds are released and an optimum treatment is ensured.
    Mit Hilfe dieses erfindungsgemässen Mittels wird die Austrocknung der Nasenschleimhäute erfolgreich verhindert und Erkrankungen, wie z. With the help of this inventive agent, the drying of the nasal mucosa is successfully prevented and diseases such. B. Rhinitis allergica und vasomotorica, können innert kurzer Zeit erfolgreich behandelt werden, so dass nach wenigen Minuten schon subjektiv und objektiv eine wesentliche Besserung des Zustandes des Patienten festgestellt werden kann. As allergic and vasomotor rhinitis, within a short time can be successfully treated, so that even subjectively and objectively a significant improvement of the patient's condition can be detected after a few minutes.
    Nachstehend wird die Erfindung durch zwei Beispiele näher erläutert. The invention is further illustrated by two examples.
    Beispiel 1 Aus den folgenden Bestandteilen wurde auf übliche Weise eine Nasensalbe hergestellt: Polyäthylenglykol 600 40 g Polyäthylenglykol 2000 20 g Cetylalkohol 10 g Sorbitol 5g Meersalz (NaCl + Spurenelemente) 1,3 g Methylparabenzoat 0,1 g **WARNUNG** Ende CLMS Feld konnte Anfang DESC uberlappen**. Example 1 from the following ingredients was prepared in a conventional manner, a nasal ointment: polyethylene glycol 600 40 g Polyethylene glycol 2000 20 g Cetyl alcohol 10 g sorbitol 5 g of sea salt (NaCl + trace elements) 1.3 g 0.1 g ** WARNING ** Methylparabenzoat end of CLMS field could overlap the beginning of DESC **.
CH231686A 1986-06-09 1986-06-09 Corticosteroid ointment compsns. - comprise e.g. dexamethasone in poly:alkylene glycol base, and are used esp. for treating rhinitis CH668188A5 (en)

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CH231686A CH668188A5 (en) 1986-06-09 1986-06-09 Corticosteroid ointment compsns. - comprise e.g. dexamethasone in poly:alkylene glycol base, and are used esp. for treating rhinitis

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CH231686A CH668188A5 (en) 1986-06-09 1986-06-09 Corticosteroid ointment compsns. - comprise e.g. dexamethasone in poly:alkylene glycol base, and are used esp. for treating rhinitis

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