WO2002032460A1 - Utilisation d'hydrocarbures substitues, biodegradables, de leurs esters, ethers et/ou amides pour la prophylaxie de reactions allergiques par inhalation et/ou pour le traitement de la muqueuse nasale - Google Patents

Utilisation d'hydrocarbures substitues, biodegradables, de leurs esters, ethers et/ou amides pour la prophylaxie de reactions allergiques par inhalation et/ou pour le traitement de la muqueuse nasale Download PDF

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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
Application number
PCT/EP2001/012101
Other languages
German (de)
English (en)
Inventor
Rüdiger GRÖNING
Original Assignee
Beisel, Günther
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 Beisel, Günther filed Critical Beisel, Günther
Priority to AU2002210555A priority Critical patent/AU2002210555A1/en
Publication of WO2002032460A1 publication Critical patent/WO2002032460A1/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
    • A61K31/21—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.

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

Abstract

La présente invention concerne l'utilisation de préparations pour la prophylaxie de réactions allergiques par inhalation et/ou pour le traitement de la muqueuse nasale. Ces préparations contiennent des hydrocarbures, substitués par des groupes OH et/ou COOH, leurs dérivés et/ou esters, leurs éthers et/ou amides, enzymatiquement dégradables dans la muqueuse nasale ou dans la peau de façon générale et physiologiquement neutres.
PCT/EP2001/012101 2000-10-19 2001-10-19 Utilisation d'hydrocarbures substitues, biodegradables, de leurs esters, ethers et/ou amides pour la prophylaxie de reactions allergiques par inhalation et/ou pour le traitement de la muqueuse nasale WO2002032460A1 (fr)

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
DE10051858A DE10051858A1 (de) 2000-10-19 2000-10-19 Verwendung von biologisch abbaubaren, substituierten Kohlenwasserstoffen deren Ester, Ether und/oder Amide als Nasensalbe oder Nasentropfen zur Prophylaxe von inhalationsallergischen Reaktionen und zur Pflege der Nasenschleimhaut
DE10051858.3 2000-10-19

Publications (1)

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

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PCT/EP2001/012101 WO2002032460A1 (fr) 2000-10-19 2001-10-19 Utilisation d'hydrocarbures substitues, biodegradables, de leurs esters, ethers et/ou amides pour la prophylaxie de reactions allergiques par inhalation et/ou pour le traitement de la muqueuse nasale

Country Status (3)

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2283805A1 (fr) * 2009-07-28 2011-02-16 Sirvis BV Compositions comprenant un composé contenant du zinc dissout dans une phase hydrophobique
EP2425842A1 (fr) * 2010-09-02 2012-03-07 Lorentz, Eckart Composition pour la thérapie locale symptomatique de la muqueuse nasale et gouttes pour le nez contenant cette composition

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62209016A (ja) * 1986-03-10 1987-09-14 Sunstar Inc 抗アレルギ−剤
JPS62209023A (ja) * 1986-03-10 1987-09-14 Sunstar Inc 抗アレルギ−剤
EP0352412A2 (fr) * 1988-05-04 1990-01-31 HERMES Fabrik pharmazeutischer Präparate Franz Gradinger GmbH & Co. Aérosols pour l'inhalation contenant des esters du rétinol et/ou de l'acide rétinoique
JPH06256119A (ja) * 1993-03-05 1994-09-13 Nippon Bayeragrochem Kk 農園芸用殺菌剤組成物

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MC2204A1 (fr) * 1989-10-31 1992-11-26 Columbia Lab Inc Composition et methode d'humidification de tissus
DE4117887C2 (de) * 1990-06-09 1993-12-16 Siegfried Rochler Verwendung von pharmazeutisch/kosmetisch als Vaselin definierten gesättigten Kohlenwasserstoffen als Nasensalbe zur Prophylaxe von inhalationsallergischen Reaktionen

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62209016A (ja) * 1986-03-10 1987-09-14 Sunstar Inc 抗アレルギ−剤
JPS62209023A (ja) * 1986-03-10 1987-09-14 Sunstar Inc 抗アレルギ−剤
EP0352412A2 (fr) * 1988-05-04 1990-01-31 HERMES Fabrik pharmazeutischer Präparate Franz Gradinger GmbH & Co. Aérosols pour l'inhalation contenant des esters du rétinol et/ou de l'acide rétinoique
JPH06256119A (ja) * 1993-03-05 1994-09-13 Nippon Bayeragrochem Kk 農園芸用殺菌剤組成物

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 (fr) * 2009-07-28 2011-02-16 Sirvis BV Compositions comprenant un composé contenant du zinc dissout dans une phase hydrophobique
EP2316415A2 (fr) 2009-07-28 2011-05-04 Sirvis Compositions pour les lèvres comprenant un composé contenant du zinc dissout dans une phase hydrophobique
EP2316415A3 (fr) * 2009-07-28 2012-06-20 Sirvis Compositions pour les lèvres comprenant un composé contenant du zinc dissout dans une phase hydrophobique
EP2425842A1 (fr) * 2010-09-02 2012-03-07 Lorentz, Eckart Composition pour la thérapie locale symptomatique de la muqueuse nasale et gouttes pour le nez contenant cette composition

Also Published As

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

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