[go: up one dir, main page]

WO2002032460A1 - Use of biologically degradable substituted hydrocarbons, the esters, ethers and /or amides thereof for prophylaxis of allergic inhalation reactions and/or for treatment of the nasal mucosa - Google Patents

Use of biologically degradable substituted hydrocarbons, the esters, ethers and /or amides thereof for prophylaxis of allergic inhalation reactions and/or for treatment of the nasal mucosa Download PDF

Info

Publication number
WO2002032460A1
WO2002032460A1 PCT/EP2001/012101 EP0112101W WO0232460A1 WO 2002032460 A1 WO2002032460 A1 WO 2002032460A1 EP 0112101 W EP0112101 W EP 0112101W WO 0232460 A1 WO0232460 A1 WO 0232460A1
Authority
WO
WIPO (PCT)
Prior art keywords
use according
preparation
oil
preparation contains
nasal mucosa
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP2001/012101
Other languages
German (de)
French (fr)
Inventor
Rüdiger GRÖNING
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to AU2002210555A priority Critical patent/AU2002210555A1/en
Publication of WO2002032460A1 publication Critical patent/WO2002032460A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A61K31/231—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/201—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having one or two double bonds, e.g. oleic, linoleic acids
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • 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
    • A61K9/0043—Nose
    • 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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders

Definitions

  • Hydrocarbons their esters, ethers and / or amides for
  • the present invention relates to the use of biodegradable, substituted hydrocarbons, their esters, ethers and / or amides for the prophylaxis of inhalation-allergic reactions and for the care of the nasal mucosa.
  • allergenic substances such as Bee pollen, animal hair or house dust with the air we breathe etc. over the nose.
  • the corresponding substances come into contact with the mucous membrane and lead to allergic reactions.
  • allergic reactions too
  • a main component of petroleum jelly is liquid paraffin, which is also known as mineral oil.
  • mineral oil-containing nasal preparations are known that after their use, mineral oil granulomas or mineral oil pneumonia can develop in the lungs (Wagner, JC et al., 1955, Thorax, 10: 157-170; Bayer, PM et al., 1974, Wiener clinical weekly, 86 : 438-441 and Lauque, D. et al., 1990, Chest, 98: 1149-1155).
  • the object of the present invention is to use a preparation for the prophylaxis of inhalation allergic reactions or for the care of the nasal mucosa, which do not have the disadvantages mentioned above.
  • This object is achieved in an advantageous manner by the use of a preparation for the prophylaxis of inhalation-allergic reactions and / or for the care of the nasal mucosa containing hydrocarbons substituted with hydroxyl group and / or carboxylic acid groups, their derivatives and / or esters, ethers and / or amides thereof.
  • Chain lengths of at least 8 carbon atoms are advantageous according to the invention, since they have proven to be well tolerated when used on patients. According to the invention, chain lengths of 8 to 24 carbon atoms are particularly well tolerated. The chain length is not limited, however.
  • substituted hydrocarbons of the aforementioned type also include saturated or unsaturated hydrocarbons.
  • the preparation used according to the invention can contain natural, semi-synthetic and / or synthetic fats, oils, waxes and / or wax-like compounds, preferably mono-, di- and / or triglycerides of fatty acids.
  • esters, ethers and / or amides of fatty acids and / or fatty alcohols are also used in the preparation according to the invention. Examples include neutral oil, peanut oil, sesame oil, sunflower oil, safflower oil, olive oil, soybean oil, castor oil and / or lard.
  • a preparation is preferably used which, for. B. isopropyl palmitate and / or oleic acid.
  • hydrocarbons substituted with hydroxyl groups and / or carboxylic acid groups according to the invention is the enzymatic degradability of the hydrocarbons in the body due to their functional groups. That is, the hydrocarbons substituted according to the invention are enzymatically degradable in the nasal mucosa or generally in the body.
  • the preparations used according to the invention can have an ointment-like, gel-like or liquid consistency and in the form of a nasal ointment, a nasal gel, nasal sprays or as nasal drops be administered.
  • the preparations additionally contain a suitable gel-forming component, which can be lipophilic or hydrophilic. According to the invention, these can be macromolecular synthetic, semisynthetic and / or natural gel formers. Examples include magnesium stearate, aluminum stearate, zinc stearate and / or ethyl cellulose.
  • the ingredients mentioned are contained individually or in combination in the preparation used according to the invention.
  • the above-mentioned ingredients of the preparations used can be present as a solution or in the form of a dispersion.
  • the basis for the preparations used can be water.
  • a water / glycerol and / or a water / propylene glycol mixture can be the base solution, which is mixed and / or dispersed with the hydrophilic or lipophilic gel formers and / or hydrocarbons of the aforementioned type.
  • the preparations used can optionally contain at least one emulsifier.
  • the preparation can be produced, for example, by mixing or dispersing the components present, it being possible to carry out heating, heating, melting, cooling and / or combinations thereof. These procedures can be carried out before and / or during the filling (packaging) of the preparations, for example in tubes or atomizers.
  • the exact preparation of the preparations takes place according to methods known per se. They are familiar to the specialist and are therefore not listed any further.
  • the preparations can be applied well to the mucous membranes and can, for example, have a residence time of at least 5 hours. Samples can be taken to show that pollen grains, dust particles and / or hair have settled in and / or have been deposited in and / or on the preparation applied topically to the nasal mucosa.
  • a major advantage of using the aforementioned preparation is that it is enzymatically degradable in the nasal mucosa or in general in the body of humans and animals. Furthermore, the use of the preparations described is advantageous for the prophylaxis of inhalation-allergic reactions. In addition to inhalation-allergic reactions, hypersensitivities to inhaled substances are also included according to the invention. The invention also relates to the use of the preparation according to the invention for the care of the nasal mucosa.
  • Such an application can be particularly advantageous, for example, for the treatment of the symptom of the so-called “dry nose” or in general for drying out the nasal mucosa, for example when traveling by air or in the elderly or less severe water loss of the cells on the surface of the nasal mucosa is reduced, which means that the preparation according to the invention, due to its lipophilic properties, prevents natural evaporation on the surface of the mucous membranes or at least strongly counteracts them.
  • the present invention is characterized in more detail below by means of exemplary embodiments. However, these examples are not limitative of the invention.
  • Preparation 1 (Oleogel with medium-chain triglycerides) An ointment-like gel is produced as follows: Medium-chain triglycerides (EuAB) 45 parts aluminum stearate (EuAB) 5 parts
  • Aluminum stearate is evenly dispersed in the medium-chain triglycerides. The dispersion is heated to 115 ° C. The mixture is then cooled to 90 ° C and filled into tubes.
  • An ointment-like gel is made as follows:
  • Zinc stearate is dissolved in castor oil while heating.
  • the hot solution is passed through a sieve with a mesh size of 0.2 mm and filled into the tubes as a melt.
  • Medium-chain triglycerides are filled into a bottle for nasal preparations with a spray head and pump valve without any additional additives.
  • Medium-chain triglycerides are melted into a gel with the aluminum stearate.
  • the components pectin and carmellose sodium are dispersed in the melt in a finely powdered form.
  • the preparation is filled into tubes.
  • a hydrogel with good adherence to the nasal mucosa is made as follows:
  • Hydroxypropylmethylcellulose is dissolved in the Gyicerol / water mixture.
  • Cotton swabs are placed in each patient's nostril and distributed by gently massaging into the nose. By taking and examining a sample, it is shown that after 6 hours there is still a thin layer of oleogel on the mucous membranes. Microscopic examination shows that pollen grains from plants and dust particles have been deposited in the oleic layer.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention relates to the use of preparations for the prophylaxis of allergic inhalation reactions and/or for treatment of the nasal mucosa, comprising OH- and/or COOH-substituted hydrocarbons, the derivatives, esters, ethers and/or amides thereof, which are enzymatically degraded in the nasal mucosa or generally in the body and are physiologically acceptable.

Description

Verwendung von biologisch abbaubaren, substituierten Use of biodegradable, substituted

Kohlenwasserstoffen deren Ester, Ether und/oder Amide zurHydrocarbons their esters, ethers and / or amides for

Prophylaxe von inhalationsallergischen Reaktionen und/oder zurProphylaxis of inhalation allergic reactions and / or for

Pflege der NasenschleimhautCare of the nasal mucosa

Die vorliegende Erfindung betrifft die Verwendung von biologisch abbaubaren, substituierten Kohlenwasserstoffen, deren Ester, Ether und/oder Amide zur Prophylaxe von inhalationsallergischen Reaktionen sowie zur Pflege der Nasenschleimhaut.The present invention relates to the use of biodegradable, substituted hydrocarbons, their esters, ethers and / or amides for the prophylaxis of inhalation-allergic reactions and for the care of the nasal mucosa.

Menschen mit allergischen Erkrankungen nehmen allergen wirkende Stoffe, wie z.B. Blütenpollen, Tierhaare oder Hausstaub mit der Atemluft u.a. über die Nase auf. In der Nase treten die entsprechenden Substanzen mit der Schleimhaut in Kontakt und führen zu allergischen Reaktionen. Neben allergischen Reaktionen können auchPeople with allergic diseases take allergenic substances, such as Bee pollen, animal hair or house dust with the air we breathe etc. over the nose. In the nose, the corresponding substances come into contact with the mucous membrane and lead to allergic reactions. In addition to allergic reactions, too

Überempfindlichkeitsreaktionen bei den Patienten auftreten.Hypersensitivity reactions occur in patients.

In DE 411 78 87 ist die Verwendung von gesättigten, aliphatischen Kohlenwasserstoffen als Nasensalbe zur Prophylaxe von inhalationsallergischen Reaktionen beschrieben. Diese durch die Bezeichnung Vaselin definierten Kohlenwasserstoffe besitzen keinerlei funktioneile Gruppen. Die Möglichkeit eines enzymatischen Abbaus von Vaselin ist für einige spezialisierte Mikroorganismen beschrieben. Einem enzymatischen Abbau in der Nasenschleimhaut oder allgemein im Körper sind diese vaselinhaltigen Verbindungen jedoch nicht zugänglich.DE 411 78 87 describes the use of saturated, aliphatic hydrocarbons as a nasal ointment for the prophylaxis of inhalation-allergic reactions. The hydrocarbons defined by the name petroleum jelly do not have any functional groups. The possibility of enzymatic degradation of petroleum jelly has been described for some specialized microorganisms. However, these vaseline-containing compounds are not amenable to enzymatic degradation in the nasal mucosa or in general in the body.

Aus medizinischer und pharmazeutischer Sicht bestehen erhebliche toxikologische Bedenken gegen die Verwendung von vaselinartigenFrom a medical and pharmaceutical perspective, there are significant toxicological concerns about the use of vaseline-like

Kohlenwasserstoffen in Nasensalben. Ein Hauptbestandteil des Vaselins ist u.a. flüssiges Paraffin, das auch als Mineralöl bezeichnet wird. Von mineralölhaltigen Nasenzubereitungen ist bekannt, daß sich nach ihrer Anwendung Mineralölgranulome oder Mineralölpneumonien in der Lunge ausbilden können (Wagner, J.C. et al., 1955, Thorax, 10: 157-170; Bayer, P.M. et al., 1974, Wiener klinische Wochenschrift, 86: 438-441 und Lauque, D. et al., 1990, Chest, 98: 1149-1155).Hydrocarbons in nasal ointments. A main component of petroleum jelly is liquid paraffin, which is also known as mineral oil. Of mineral oil-containing nasal preparations are known that after their use, mineral oil granulomas or mineral oil pneumonia can develop in the lungs (Wagner, JC et al., 1955, Thorax, 10: 157-170; Bayer, PM et al., 1974, Wiener clinical weekly, 86 : 438-441 and Lauque, D. et al., 1990, Chest, 98: 1149-1155).

Salben und Gele auf der Grundlage von Fetten oder öligen Verbindungen sind zahlreich bekannt (Römpp, Lexikon der Chemie, Thieme Verlag, 9. Auflage, 1990). Allerdings sind diese Zubereitungen als Grundlage für Arzneimittel oder in einer rein pflegenden Funktion für die Haut allgemein oder die Nasenschleimhaut insbesondere beschrieben. Eine Verwendung zum Schutz und/oder zur Linderung von inhalationsallergischen Reaktionen ist nicht beschrieben.Numerous ointments and gels based on fats or oily compounds are known (Römpp, Lexikon der Chemie, Thieme Verlag, 9th edition, 1990). However, these preparations are described as the basis for pharmaceuticals or in a purely nourishing function for the skin in general or for the nasal mucosa in particular. Use for the protection and / or relief of inhalation allergic reactions is not described.

Aufgabe der vorliegenden Erfindung ist die Verwendung einer Zubereitung zur Prophylaxe von inhalationsallergischen Reaktionen oder zur Pflege der Nasenschleimhaut, welche die zuvor genannten Nachteile nicht aufweisen.The object of the present invention is to use a preparation for the prophylaxis of inhalation allergic reactions or for the care of the nasal mucosa, which do not have the disadvantages mentioned above.

Diese Aufgabe wird in vorteilhafter Weise gelöst durch die Verwendung einer Zubereitung zur Prophylaxe von inhalationsallergischen Reaktionen und/oder zur Pflege der Nasenschleimhaut enthaltend mit Hydroxylgruppen- und/oder Carbonsäuregruppen substituierte Kohlenwasserstoffe, deren Derivate und/oder Ester, Ether und/oder Amide davon.This object is achieved in an advantageous manner by the use of a preparation for the prophylaxis of inhalation-allergic reactions and / or for the care of the nasal mucosa containing hydrocarbons substituted with hydroxyl group and / or carboxylic acid groups, their derivatives and / or esters, ethers and / or amides thereof.

Hierbei sind im Sinne der vorliegenden Erfindung unter „mitFor the purposes of the present invention, “with

Hydroxylgruppen- und/oder Carbonsäuregruppen substituierte Kohlenwasserstoffe" mittel- und/oder langkettige substituierte Kohlenwasserstoffe zu verstehen. Erfindungsgemäß vorteilhaft sind Kettenlängen von wenigstens 8 C-Atomen, da sie sich bei der Anwendung am Patienten als gut verträglich erwiesen haben. Erfindungsgemäß besonders gut verträglich sind Kettenlängen von 8 bis 24 C-Atomen. Die Kettenlänge ist nach oben jedoch nicht begrenzt.Hydroxyl group and / or carboxylic acid groups substituted hydrocarbons "medium and / or long chain substituted Understand hydrocarbons. Chain lengths of at least 8 carbon atoms are advantageous according to the invention, since they have proven to be well tolerated when used on patients. According to the invention, chain lengths of 8 to 24 carbon atoms are particularly well tolerated. The chain length is not limited, however.

Ferner sind im Sinne der vorliegenden Erfindung in den substituierter Kohlenwasserstoffen der zuvor genannten Art auch gesättigte oder ungesättigte Kohlenwasserstoffe umfaßt.Furthermore, for the purposes of the present invention, the substituted hydrocarbons of the aforementioned type also include saturated or unsaturated hydrocarbons.

Hierbei kann die erfindungsgemäß verwendete Zubereitung natürliche, halbsynthetische und/oder synthetische Fette, Öle, Wachse und/oder wachsartige Verbindungen enthalten, bevorzugt Mono-, Di- und/oder Triglyceride von Fettsäuren. Erfindungsgemäß finden ferner Ester, Ether und/oder Amide von Fettsäuren und/oder Fettalkoholen Einsatz in der erfindungsgemäßen Zubereitung. Als Beispiele hierfür sind Neutralöl, Erdnussöl, Sesamöl, Sonnenblumenöl, Safloröl, Olivenöl, Sojaöl, Ricinusöl und/oder Schweinefett zu nennen. Bevorzugt wird eine Zubereitung eingesetzt, die z. B. Isopropylpalmitat und/oder Ölsäureoleylester enthält.The preparation used according to the invention can contain natural, semi-synthetic and / or synthetic fats, oils, waxes and / or wax-like compounds, preferably mono-, di- and / or triglycerides of fatty acids. According to the invention, esters, ethers and / or amides of fatty acids and / or fatty alcohols are also used in the preparation according to the invention. Examples include neutral oil, peanut oil, sesame oil, sunflower oil, safflower oil, olive oil, soybean oil, castor oil and / or lard. A preparation is preferably used which, for. B. isopropyl palmitate and / or oleic acid.

Ein weiterer Vorteil der erfindungsgemäßen „mit Hydroxylgruppen- und/oder Carbonsäuregruppen substituierten Kohlenwasserstoffe" ist die enzymatische Abbaubarkeit der Kohlenwasserstoffe im Körper aufgrund ihrer funktioneilen Gruppen. D.h., daß die erfindungsgemäß substituierten Kohlenwasserstoffe in der Nasenschleimhaut oder allgemein im Körper enzymatisch abbaubar sind.Another advantage of the hydrocarbons substituted with hydroxyl groups and / or carboxylic acid groups according to the invention is the enzymatic degradability of the hydrocarbons in the body due to their functional groups. That is, the hydrocarbons substituted according to the invention are enzymatically degradable in the nasal mucosa or generally in the body.

Die erfindungsgemäße verwendeten Zubereitungen können eine salbenartige, gelartige oder flüssige Konsistenz aufweisen und in Form einer Nasensalbe, eines Nasengels, Nasensprays oder als Nasentropfen verabreicht werden. Dabei enthalten die Zubereitungen zusätzlich eine geeignete Gel-bildende Komponente, die lipophil oder hydrophil sein kann. Erfindungsgemäß können dies makromolekulare synthetische, halbsynthetische und/oder natürliche Gelbildner sein. Beispiele hierfür sind u.a. Magnesiumstearat, Aluminiumstearat, Zinkstearat und/oder Ethylcellulose.The preparations used according to the invention can have an ointment-like, gel-like or liquid consistency and in the form of a nasal ointment, a nasal gel, nasal sprays or as nasal drops be administered. The preparations additionally contain a suitable gel-forming component, which can be lipophilic or hydrophilic. According to the invention, these can be macromolecular synthetic, semisynthetic and / or natural gel formers. Examples include magnesium stearate, aluminum stearate, zinc stearate and / or ethyl cellulose.

Erfindungsgemäß sind die genannten Inhaltstoffe einzeln oder in Kombination in der erfindungsgemäß verwendeten Zubereitung enthalten.According to the invention, the ingredients mentioned are contained individually or in combination in the preparation used according to the invention.

Ferner können die zuvor genannten Inhaltsstoffe der verwendeten Zubereitungen als Lösung oder in Form einer Dispersion vorliegen. Grundlage für die verwendeten Zubereitungen kann Wasser sein. In einer Variante der verwendeten Zubereitungen kann beispielsweise ein Wasser/Glycerol- und/oder ein Wasser/Propylenglycol-Gemisch die Basislösung sein, die mit den hydrophilen oder lipophilen Gelbildner und/oder Kohlenwasserstoffen der zuvor genannten Art vermischt und/oder dispergiert ist. In einer Variante der vorliegenden Erfindung können die verwendeten Zubereitungen ggf. wenigstens einen Emulgator enthalten.Furthermore, the above-mentioned ingredients of the preparations used can be present as a solution or in the form of a dispersion. The basis for the preparations used can be water. In a variant of the preparations used, for example a water / glycerol and / or a water / propylene glycol mixture can be the base solution, which is mixed and / or dispersed with the hydrophilic or lipophilic gel formers and / or hydrocarbons of the aforementioned type. In a variant of the present invention, the preparations used can optionally contain at least one emulsifier.

Allgemein kann die Herstellung der Zubereitung beispielsweise durch Mischen oder Dispergieren der enthaltenen Komponenten erfolgen, wobei eine Erwärmung, Erhitzung, ein Schmelzen, eine Abkühlung und/oder Kombinationen davon durchgeführt werden kann. Diese Vorgehensweisen können vor und/oder während der Abfüllung (Konfektionierung) der Zubereitungen, z.B. in Tuben oder Zerstäuber erfolgen. Die genaue Herstellung der Zubereitungen erfolgt nach an sich bekannten Methoden. Sie sind dem Fachmann vertraut und werden deshalb nicht weiter aufgeführt. Die Zubereitungen lassen sich gut auf die Schleimhäute auftragen und können beispielsweise eine Verweildauer von wenigstens 5 Stunden aufweisen. Durch Probeentnahmen kann gezeigt werden, daß sich Pollenkörner, Staubpartikel und/oder Haare in und/oder auf die oberflächlich (topisch) auf die Nasenschleimhaut aufgebrachte Zubereitung ein und/oder aufgelagert haben.In general, the preparation can be produced, for example, by mixing or dispersing the components present, it being possible to carry out heating, heating, melting, cooling and / or combinations thereof. These procedures can be carried out before and / or during the filling (packaging) of the preparations, for example in tubes or atomizers. The exact preparation of the preparations takes place according to methods known per se. They are familiar to the specialist and are therefore not listed any further. The preparations can be applied well to the mucous membranes and can, for example, have a residence time of at least 5 hours. Samples can be taken to show that pollen grains, dust particles and / or hair have settled in and / or have been deposited in and / or on the preparation applied topically to the nasal mucosa.

Ein wesentlicher Vorteil der Verwendung der zuvor genannten Zubereitung ist, daß sie in der Nasenschleimhaut oder allgemein im Körper von Mensch und Tier enzymatisch abbaubar ist. Ferner zeichnet sich die Verwendung der beschriebenen Zubereitungen in vorteilhafter Weise zur Prophylaxe von inhalationsallergischen Reaktionen aus. Neben inhalationsallergischen Reaktionen sind erfindungsgemäß auch Überempfindlichkeiten gegenüber eingeatmeten Stoffen erfindungsgemäß umfaßt. Darüber hinaus ist auch eine Verwendung der erfindungsgemäßen Zubereitung zur Pflege der Nasenschleimhaut Gegenstand der Erfindung. Eine solche Anwendung kann beispielsweise zur Behandlung des Symptoms der sogenannten „Trockenen Nase" oder allgemein beim Austrocknen der Nasenschleimhaut z. B. bei Flugreisen oder bei älteren Menschen besonders vorteilhaft sein. Hierbei wird durch ein Auftragen der erfindungsgemäßen Zubereitung auf die Nasenschleimhaut der natürlicher Weise mehr oder weniger stark auftretende Wasserverlust der Zellen an der Oberfläche der Nasenschleimhaut reduziert. Das heißt, daß die erfindungsgemäße Zubereitung aufgrund ihrer lipophilen Eigenschaften eine natürlichen Verdunstung an der Oberfläche der Schleimhäute verhindert oder dieser zumindest stark entgegenwirkt. Nachfolgend ist die vorliegende Erfindung durch Ausführungsbeispiele näher charakterisiert. Diese Beispiele sind jedoch nicht limitierend für die Erfindung.A major advantage of using the aforementioned preparation is that it is enzymatically degradable in the nasal mucosa or in general in the body of humans and animals. Furthermore, the use of the preparations described is advantageous for the prophylaxis of inhalation-allergic reactions. In addition to inhalation-allergic reactions, hypersensitivities to inhaled substances are also included according to the invention. The invention also relates to the use of the preparation according to the invention for the care of the nasal mucosa. Such an application can be particularly advantageous, for example, for the treatment of the symptom of the so-called “dry nose” or in general for drying out the nasal mucosa, for example when traveling by air or in the elderly or less severe water loss of the cells on the surface of the nasal mucosa is reduced, which means that the preparation according to the invention, due to its lipophilic properties, prevents natural evaporation on the surface of the mucous membranes or at least strongly counteracts them. The present invention is characterized in more detail below by means of exemplary embodiments. However, these examples are not limitative of the invention.

Die Bezeichnung EuAB steht als Abkürzung für „Europäisches Arzneibuch".The name EuAB stands for "European Pharmacopoeia".

Zubereitung 1 : (Oleogel mit mittelkettigen Triglyceriden) Ein salbenartiges Gel wird wie folgt hergestellt: Mittelkettige Triglyceride (EuAB) 45 Teile Aluminiumstearat (EuAB) 5 TeilePreparation 1: (Oleogel with medium-chain triglycerides) An ointment-like gel is produced as follows: Medium-chain triglycerides (EuAB) 45 parts aluminum stearate (EuAB) 5 parts

Aluminiumstearat wird in den mittelkettigen Triglyceriden gleichmäßig dispergiert. Die Dispersion wird auf 115 °C erhitzt. Die Mischung wird anschließend auf 90 °C abgekühlt und in Tuben gefüllt.Aluminum stearate is evenly dispersed in the medium-chain triglycerides. The dispersion is heated to 115 ° C. The mixture is then cooled to 90 ° C and filled into tubes.

Zubereitung 2: (Oleogel mit Ricinusöl)Preparation 2: (oleogel with castor oil)

Ein salbenartiges Gel wird wie folgt hergestellt:An ointment-like gel is made as follows:

Ricinusöl (EuAB) 45 TeileCastor oil (EuAB) 45 parts

Zinkstearat 7 TeileZinc stearate 7 parts

Zinkstearat wird unter Erwärmen in Ricinusöl gelöst. Die heiße Lösung wird durch ein Sieb mit einer Maschenweite von 0,2 mm gegeben und als Schmelze in die Tuben gefüllt.Zinc stearate is dissolved in castor oil while heating. The hot solution is passed through a sieve with a mesh size of 0.2 mm and filled into the tubes as a melt.

Zubereitung 3: (öliges Nasenspray)Preparation 3: (oily nasal spray)

Mittelkettige Triglyceride werden ohne weitere Hilfsstoffe in eine Flasche für Nasenzubereitungen mit Sprühkopf und Pumpventil gefüllt.Medium-chain triglycerides are filled into a bottle for nasal preparations with a spray head and pump valve without any additional additives.

Zubereitung 4: (Oleogel mit hydrophilen Hilfsstoffen) Ein Oleogel, das durch hydrophile Hilfsstoffe eine verbesserte Haftfähigkeit auf Schleimhäuten besitzt wird wie folgt hergestellt: Mittelkettige Triglyceride 45 TeilePreparation 4: (oleogel with hydrophilic auxiliary substances) An oleogel, which has an improved adhesion to mucous membranes due to hydrophilic additives, is produced as follows: Medium-chain triglycerides 45 parts

Aluminiumstearat 5 Teile Pectin 3 TeileAluminum stearate 5 parts pectin 3 parts

Carmellose-Natrium 2 TeileCarmellose sodium 2 parts

Mittelkettige Triglyceride werden mit dem Aluminiumstearat zu einem Gel geschmolzen. In der Schmelze werden die Bestandteile Pectin und Carmellose-Natrium in fein gepulverter Form dispergiert. Die Zubereitung wird in Tuben abgefüllt.Medium-chain triglycerides are melted into a gel with the aluminum stearate. The components pectin and carmellose sodium are dispersed in the melt in a finely powdered form. The preparation is filled into tubes.

Zubereitung 5: (Hydrogel für die Nase)Preparation 5: (hydrogel for the nose)

Ein Hydrogel mit guter Haftfähigkeit auf den Nasenschleimhäuten wird wie folgt hergestellt:A hydrogel with good adherence to the nasal mucosa is made as follows:

Hydroxypropylmethylcellulose 2 TeileHydroxypropylmethylcellulose 2 parts

Wasser 100 TeileWater 100 parts

Glycerol 1 TeilGlycerol 1 part

Hydroxypropylmethylcellulose wir im Gyicerol/Wasser-Gemisch gelöst.Hydroxypropylmethylcellulose is dissolved in the Gyicerol / water mixture.

Anwendungsbeispiel:Example of use:

Jeweils etwa 100 mg der Zubereitung 1 werden mit Hilfe einsApproximately 100 mg of preparation 1 are made using one

Wattestäbchens in jedes Nasenloch von Patienten gegeben und durch leichtes Einmassieren in der Nase verteilt. Durch Entnahme und Untersuchung einer Probe wird nachgewiesen, daß sich nach 6 Stunden noch eine dünne Schicht des Oleogels auf den Schleimhäuten befindet. Die mikroskopische Untersuchung zeigt, daß sich Pollenkörner von Pflanzen und Staubpartikel in der Oleogelschicht abgelagert haben. Cotton swabs are placed in each patient's nostril and distributed by gently massaging into the nose. By taking and examining a sample, it is shown that after 6 hours there is still a thin layer of oleogel on the mucous membranes. Microscopic examination shows that pollen grains from plants and dust particles have been deposited in the oleic layer.

Claims

Patentansprüche: claims: 1. Verwendung einer Zubereitung zur Prophylaxe von inhalationsallergischen Reaktionen und/oder zur Pflege der Nasenschleimhaut enthaltend mit Hydroxylgruppen- und/oder1. Use of a preparation for the prophylaxis of inhalation allergic reactions and / or for the care of the nasal mucosa containing with hydroxyl groups and / or Carbonsäuregruppen substituierte Kohlenwasserstoffe, deren Derivate und/oder Ester, Ether und/oder Amide davon.Carboxylic acid groups substituted hydrocarbons, their derivatives and / or esters, ethers and / or amides thereof. 2. Verwendung gemäß Anspruch 1 , wobei die Zubereitung mittel- bis langkettige mit Hydroxylgruppen- und/oder Carbonsäuregruppen substituierte Kohlenwasserstoffe enthält.2. Use according to claim 1, wherein the preparation contains medium to long-chain hydrocarbons substituted with hydroxyl groups and / or carboxylic acid groups. 3. Verwendung gemäß einem der Ansprüche 1 oder 2, ' wobei die Zubereitung substituierte Kohlenwasserstoffe mit einer Kettenlänge von wenigstens 8 C-Atomen enthält.3. Use according to one of claims 1 or 2, ' wherein the preparation contains substituted hydrocarbons with a chain length of at least 8 carbon atoms. 4. Verwendung gemäß einem der Ansprüche 1 bis 3, wobei die Zubereitung substituierte Kohlenwasserstoffe mit einer Kettenlänge von 8 bis 24 C-Atomen enthält.4. Use according to one of claims 1 to 3, wherein the preparation contains substituted hydrocarbons with a chain length of 8 to 24 carbon atoms. 5. Verwendung gemäß einem der Ansprüche 1 bis 4, wobei die Zubereitung natürliche, halbsynthetische und/oder synthetische Ester, Ether und/oder Amide von Fettsäuren und/oder Fettalkoholen enthält.5. Use according to one of claims 1 to 4, wherein the preparation contains natural, semi-synthetic and / or synthetic esters, ethers and / or amides of fatty acids and / or fatty alcohols. 6. Verwendung gemäß einem der Ansprüche 1 bis 5, wobei die Zubereitung natürliche, halbsynthetische und/oder synthetische Mono-, Di- und/oder Triglyceride von Fettsäuren enthält. 6. Use according to any one of claims 1 to 5, wherein the preparation contains natural, semi-synthetic and / or synthetic mono-, di- and / or triglycerides of fatty acids. 7. Verwendung gemäß einem der Ansprüche 1 bis 6, wobei die Zubereitung Neutralöl, Erdnussöl, Sesamöl, Sonnenblumenöl, Olivenöl, Safrolöl, Sojaöl, Ricinusöl und/oder Schweinefett enthält.7. Use according to one of claims 1 to 6, wherein the preparation contains neutral oil, peanut oil, sesame oil, sunflower oil, olive oil, saffron oil, soybean oil, castor oil and / or lard. 8. Verwendung gemäß einem der Ansprüche 1 bis 7, wobei die Zubereitung Isopropylpalmitat und/oder Ölsäureoleylester enthält.8. Use according to one of claims 1 to 7, wherein the preparation contains isopropyl palmitate and / or oleic acid oleyl ester. 9. Verwendung gemäß einem der Ansprüche 1 bis 8, wobei die Zubereitung zusätzlich synthetische, halbsynthetische und/oder natürliche Gelbildner enthält.9. Use according to one of claims 1 to 8, wherein the preparation additionally contains synthetic, semisynthetic and / or natural gelling agents. 10. Verwendung gemäß einem der Ansprüche 1 bis 9, wobei die Zubereitung Magnesiumstearat, Aluminiumstearat, Zinkstearat und/oder Ethylcellulose enthält.10. Use according to one of claims 1 to 9, wherein the preparation contains magnesium stearate, aluminum stearate, zinc stearate and / or ethyl cellulose. 11. Verwendung gemäß einem der Ansprüche 1 bis 10, wobei die Zubereitung in der im Körper, bevorzugt der Nasenschleimhaut enzymatisch abbaubar ist. 11. Use according to one of claims 1 to 10, wherein the preparation is enzymatically degradable in the body, preferably the nasal mucosa.
PCT/EP2001/012101 2000-10-19 2001-10-19 Use of biologically degradable substituted hydrocarbons, the esters, ethers and /or amides thereof for prophylaxis of allergic inhalation reactions and/or for treatment of the nasal mucosa Ceased WO2002032460A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002210555A AU2002210555A1 (en) 2000-10-19 2001-10-19 Use of biologically degradable substituted hydrocarbons, the esters, ethers and /or amides thereof for prophylaxis of allergic inhalation reactions and/or for treatment of the nasal mucosa

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10051858.3 2000-10-19
DE10051858A DE10051858A1 (en) 2000-10-19 2000-10-19 Use of biodegradable, substituted hydrocarbons, their esters, ethers and / or amides as nasal ointments or nasal drops for the prophylaxis of inhalation allergic reactions and for the care of the nasal mucosa

Publications (1)

Publication Number Publication Date
WO2002032460A1 true WO2002032460A1 (en) 2002-04-25

Family

ID=7660345

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2001/012101 Ceased WO2002032460A1 (en) 2000-10-19 2001-10-19 Use of biologically degradable substituted hydrocarbons, the esters, ethers and /or amides thereof for prophylaxis of allergic inhalation reactions and/or for treatment of the nasal mucosa

Country Status (3)

Country Link
AU (1) AU2002210555A1 (en)
DE (1) DE10051858A1 (en)
WO (1) WO2002032460A1 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2283805A1 (en) * 2009-07-28 2011-02-16 Sirvis BV Compositions comprising a zinc containing compound dissolved in a hydrophobic phase
EP2425842A1 (en) * 2010-09-02 2012-03-07 Lorentz, Eckart Composition for symptomatic local treatment of the nasal mucous membrane and nose drops containing this composition

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62209023A (en) * 1986-03-10 1987-09-14 Sunstar Inc Antiallergic agent
JPS62209016A (en) * 1986-03-10 1987-09-14 Sunstar Inc Antiallergic agent
EP0352412A2 (en) * 1988-05-04 1990-01-31 HERMES Fabrik pharmazeutischer Präparate Franz Gradinger GmbH & Co. Aerosols for inhalation containing esters of retinol and/or retinoic acid
JPH06256119A (en) * 1993-03-05 1994-09-13 Nippon Bayeragrochem Kk Bactericide composition for agricultural and horticultural use

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MC2204A1 (en) * 1989-10-31 1992-11-26 Columbia Lab Inc COMPOSITION AND METHOD FOR HUMIDIFYING TISSUE
DE4117887C2 (en) * 1990-06-09 1993-12-16 Siegfried Rochler Use of pharmaceutically / cosmetically defined petroleum jelly as a nasal ointment for the prophylaxis of inhalation allergic reactions

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62209023A (en) * 1986-03-10 1987-09-14 Sunstar Inc Antiallergic agent
JPS62209016A (en) * 1986-03-10 1987-09-14 Sunstar Inc Antiallergic agent
EP0352412A2 (en) * 1988-05-04 1990-01-31 HERMES Fabrik pharmazeutischer Präparate Franz Gradinger GmbH & Co. Aerosols for inhalation containing esters of retinol and/or retinoic acid
JPH06256119A (en) * 1993-03-05 1994-09-13 Nippon Bayeragrochem Kk Bactericide composition for agricultural and horticultural use

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
PATENT ABSTRACTS OF JAPAN vol. 012, no. 070 (C - 479) 4 March 1988 (1988-03-04) *
PATENT ABSTRACTS OF JAPAN vol. 018, no. 651 (C - 1285) 9 December 1994 (1994-12-09) *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2283805A1 (en) * 2009-07-28 2011-02-16 Sirvis BV Compositions comprising a zinc containing compound dissolved in a hydrophobic phase
EP2316415A2 (en) 2009-07-28 2011-05-04 Sirvis Lip compositions comprising a zinc containing compound dissolved in a hydrophobic phase
EP2316415A3 (en) * 2009-07-28 2012-06-20 Sirvis Lip compositions comprising a zinc containing compound dissolved in a hydrophobic phase
EP2425842A1 (en) * 2010-09-02 2012-03-07 Lorentz, Eckart Composition for symptomatic local treatment of the nasal mucous membrane and nose drops containing this composition

Also Published As

Publication number Publication date
DE10051858A1 (en) 2002-06-06
AU2002210555A1 (en) 2002-04-29

Similar Documents

Publication Publication Date Title
EP2504012B1 (en) Use of an oleo gel containing triterpene for healing wounds
EP1282446B1 (en) Pharmaceutical and/or cosmetic composition containing an organosiloxane and a phospholipid
DE69111821T2 (en) ACTIVE SUBSTANCE DELIVERY VEHICLE SUSPENDED IN A NON-AQUE PERFLUORED CARRIER MEDIUM.
DE69629988T2 (en) "Pharmaceutical base in ointment form and its use"
WO1994003156A1 (en) Pharmaceutical and/or cosmetic preparation and the use of the preparation
EP0135617B1 (en) Gel-like ointment containing indomethacin
EP2395973B1 (en) In situ preparations forming bonding gel, in particular for topical application to moistened skin/mucous membranes
WO2007118653A2 (en) Nanoparticle containing nicotine and/or cotinine, dispersions and use thereof
DE69524662T2 (en) Topical medication with a scarring effect
CH634994A5 (en) BASICS FOR EXTERNAL MEDICINAL PRODUCTS.
DE69635298T2 (en) Use of acetylsalicylic acids for the manufacture of a medicament for the treatment of skin injuries
DE19810655A1 (en) Pharmaceutical composition containing cyclosporin A suitable for topical administration for treating disorders of skin, mucosa and eyes
DE69804130T2 (en) USE OF A MIXTURE OF A DIOL AND ALPHA HYDROXYSIC ACID FOR THE TREATMENT OF HYPERKERATOTIC SKIN DISEASES
DE3411225C2 (en)
DE10064950A1 (en) Thixotropic nasal spray
EP2011504B1 (en) Skin cream for treatment and/or cleaning of skin for neurodermitis
WO2002032460A1 (en) Use of biologically degradable substituted hydrocarbons, the esters, ethers and /or amides thereof for prophylaxis of allergic inhalation reactions and/or for treatment of the nasal mucosa
AT414095B (en) Preparation useful e.g. to treat dry mucous membrane in oral and throat area comprises medical and/or food organic substance, flavor material, mucoadhesive substance, sugar (alcohol) and carrier substance e.g. fat and/or oil
DE60000658T2 (en) COMPOSITION FOR TREATING PSORIASIS
DE202022001251U1 (en) Pharmaceutical skin care product
EP3675814A1 (en) Composition for topical treatment of non-microorganism-caused inflammatory skin and mucous-membrane diseases
DE102013004199A1 (en) Pharmaceutical composition
EP0343406A2 (en) Use of lyzozyme in the preparation of an agent for the treatment of the mucous membrane of the nose
CH690023A5 (en) Local medicament for treating damage to cells of nasal mucosal, e.g. due to air pollution or smoking, contains capsaicin to improve mucociliary transport
DE4323174C2 (en) Pharmaceutical and / or cosmetic preparation

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PH PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP