DE20016125U1 - Vaseline-based nasal ointment with tannins - Google Patents

Description

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Phyt-Immun GmbH September 18, 2000

P34629GBM RI/peh

Nasal ointment based on Vaseline with tannins

The present invention relates to a nasal ointment comprising mixtures of predominantly saturated hydrocarbons which are gelatinous at room temperature and at least one tanning agent, and to the use thereof for the prophylaxis of inhalation allergic reactions, in particular atopic rhinitis in the form of "hay fever". In a preferred embodiment, the nasal ointment according to the invention also comprises at least one care additive suitable for ointments.

Inhalation allergies are now very common in western industrial civilizations, and the trend is continuing to rise. This is particularly the case with forms of atopic rhinitis triggered by inhalation of pollen, fungal spores, various types of dust (e.g. from wood, flour or house dust), chemical or animal irritants (feathers, hair), which, with their accompanying symptoms, can impair the patient's well-being to the point of being unable to work.

The excruciating itching of the nose, pharynx, roof of the throat and eyes, followed by tearing, sneezing and watery nasal discharge, is often accompanied by headache, irritability, loss of appetite, depression and insomnia. As the disease progresses, coughing fits and asthmatic wheezing may develop.

As a seasonal reaction triggered by pollen from trees, shrubs, grasses, wild or ornamental plants, the so-called "hay fever" is the most common atopic rhinitis.

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Most of the therapeutic and prophylactic measures used to date to control or eliminate inhalation allergic reactions have more or less serious disadvantages in terms of cost, efficiency, health side effects and comfort of use.

For example, treatments in which patients are removed from the exposure area for several weeks during the pollen season to areas with low pollen levels, such as high mountains or islands with little vegetation, or a change of residence or job in order to avoid exposure are difficult for many patients to cope with.

This avoidance is intended to achieve a large-scale removal of the disease-causing allergens from the patient's environment.
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It is not possible to completely remove inhaled allergens. There is only the possibility of eliminating the contact surfaces with the allergen, i.e. the mucous membrane as a reaction site. This is described as partial avoidance.

The installation of allergen filters in ventilation and air conditioning systems in homes, workplaces and cars can only prevent exposure in these specially protected areas and also involves non-negligible costs.

Wearing a breathing filter over the mouth and nose is inexpensive and effective, but uncomfortable.

Desensitization (hyposensitization, immunization) requires complex tests to select an effective antigen extract. However, it is not possible to predict with certainty whether the treatment will result in clinical improvement. This procedure is also not without the risk

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health-threatening side effects, such as asthmatic and urticarial complaints. Furthermore, the

Desensitization treatments involve a relatively high expenditure of time and money.

The symptomatic treatment of allergic reactions with oral antihistamines to reduce swelling of the mucous membranes is associated with the risk of a sedative effect with many of these preparations, which has a negative impact on the patient's well-being and ability to react. Side effects such as headaches, dry mouth and difficulty concentrating also occur quite frequently.

Furthermore, the use of sympathomimetics, cromoglycic acid-based preparations and glucocorticoids also has disadvantages due to numerous side effects and/or high costs.

For a detailed description of this state of the art, reference is made to DE-C 41 17 887. This relates to the use of saturated hydrocarbons, defined pharmaceutically/cosmetically as Vaseline, as a nasal ointment for the prophylaxis of inhalation allergic reactions, in particular of the "hay fever" type, whereby a Vaseline with the following properties was used:

Freezing point according to DIN 51 556: 49 to 52 ⁰ C;

Viscosity according to DIN 51 562: 6 mm ² /s (100 ⁰ C);

Cone penetration according to DIN 51 580: 150 to 170;

Average chain length of petrolatum hydrocarbons: 26 ± 1

C atoms;

C-number range of hydrocarbons: Ci5 to

Furthermore, the German utility model application DE 200 09 841.1 relates to a nasal ointment for the prophylaxis of inhalation allergic reactions comprising at least one mixture of saturated hydrocarbons with a viscosity according to DIN 51 562 of > 6 mm ² /s (100 ⁰ C), whereby this nasal ointment can additionally comprise at least one care additive as defined therein.

In view of this state of the art, the present invention was based on the object of providing a further improved nasal ointment for the effective prophylaxis of inhalation allergic reactions based on a further improved Vaseline. This nasal ointment should in turn not pose any health risks for the patient, have a broad spectrum of activity against various allergens in the air, be pleasant to use and ultimately only cause low treatment costs.

These and other objects are achieved by the nasal ointment according to patent claim 1, namely by a nasal ointment for the prophylaxis of inhalation allergic reactions comprising at least one mixture of saturated hydrocarbons and at least one tanning agent.

There are no restrictions whatsoever with regard to the hydrocarbon mixture or Vaseline that can be used according to the invention, as long as it meets the purity requirements of the pharmaceutical/cosmetic quality according to the DAB purity regulation and has the parameters required according to the invention with regard to the usual properties.

Preferably, the Vaseline described in DE-C 41 17 887 with the following properties is used:

Freezing point according to DIN 51 556: 49 to 52 ⁰ C;

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Viscosity according to DIN 51 562: 6 mnVVs (100 ⁰ C);

Cone penetration according to DIN 51 580: 150 to 170;

Average chain length of petrolatum hydrocarbons: 26 ± 1

C atoms;

C-number range of hydrocarbons: Ci5 to

Further preference is given to using the Vaseline described in DE 200 09 841.1, which is a mixture of saturated hydrocarbons with a viscosity according to DIN 51 562 of > 6 mm ² /s (100 ⁰ C). The Vaseline used particularly preferably according to the invention thus has a viscosity at 100 ⁰ C according to DIN 51 562 of > 6 mm ² /s, preferably > 8 mmVs and in particular a viscosity of 8.5 to 15 mm ² /s.

In a further preferred embodiment, a Vaseline is used which has at least one of the following properties (a) to (e):

(a) Freezing point (DIN 51556) 47 to 56 ⁰ C

(b) cone penetration according to DIN 51 5 80 from 15 5 to 185;

(c) a maximum of 5 wt.% of the saturated hydrocarbons have a chain length of < 25 ± 2;

(d) C number range of saturated hydrocarbons (determination by GC): covers C19 to C52, ± 2 in each case;

and

(e) Number average molecular weight: >400, preferably >480 and in particular >500 g/mol.

In the context of the present invention, both technical tannins, such as those obtained from bark and wood, leaves, fruits and galls, as well as therapeutic, mineral and synthetically produced tannins can be used as tanning agents. The following can be mentioned in detail:

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Crops (technical tanning agents) barks and woods:

Quercus robur L. (Fagaceae) Quercus petraea (Matt.) Liebl.

Quercus cerris L.

Quercus sylvestris L.

Picea abies (L.) Karst. (Pinaceae) Tsuga canadensis (L.) Carr. (Pinaceae) Larix decidua Mill. (Pinaceae) Betula pendula Roth (Betulaceae) Alnus glutinosa (L.) (Salicaaceae) Castanea sativa Mill. (Fagaceae) Castanea dentata Borkh.

Acacia mearnsii De Wild. (Mimosaceae) Acacia catechu Willd.

Acaica dealbata Link Eucalyptus wandoo Blakley (Myrtaceae) Eucalyptus occidentalis Endl.

Rhizophora mucronata Lam. (Rhizophoraceae) Rhizophora mangle L.

Ceriops candolleana Arn. (Rhizophoraceae) Braguiera gymmnorrhiza Lam. (Rhizophoraceae) Carapa molucensis Lam. (Meliaceae) Sonneratia caseolaris Druce (Sonneratiaceae) Avicennia tomentosa Jacq. (Verbenaceae) Schinopsis quebracho-colorado Barkl. et T. Mey. (Anacardiaceae) Schinopsis balanese Engl. Aspidosperma quebacho-blanco Poor. (Apocynaceae)

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Rhus coriaria L. (Anacardiaceae) Rhus glabra L.

Cotinus coggygia Scop. (Anacardiaceae) Coriaria myrtifolia L.
Uncaria gambir (Hunter) Roxb. (Rubiaceae)

Fruit:

Caesalpina coriaria (Jacq.) Willd. (Caesalpinaceae) Kigelia africana (Lam.) Benth. (Bignoniaceae) Terminalia chebula Retz. (Combretaceae) Areca catechu L. (Arecaceae)

Gallen:

Quercus robur L. (Fagaceae) Quercus petraea (Matt.) Liebl. (Fagaceae) Quercus infectoria Oliver (Fagaceae) Pistacea spec. (Anacardiaceae)

Tannins from gall and albumin

Medicinal plants (therapeutically used tannins)

Acacia catechu (L. f.) Willd. [Mimosaceae] Acacia suma Kurz [Mimosaceae] Agrimonia eupatoria L. [Rosaceae] Alchemilla xanthochlora Roth. [Rosaceae] Camellia sinensis (L.) O. Kuntze [Theaceae] Crataegus monogyna, laevigata, azarolus, pentagyna, nigra [Rosaceae] Fragaria vesca L [Rosaceae]

Hamamelis virginiana L. [Hamamelidaceae] Juglans regia L [Juglandaceae] Krameria lappacea (Dombey) Bürdet et Simpson Potentilla anserina L. [Rosaceae] Potentilla erecta (L.) Raeusch. [Roasaceae] Pterocarpus marsupium Roxb. [Fabaceae] Quercus infectoria Olivier [Fagaceae] Quercus pubescens Willd. [Fagaceae] Quercus robur L. [Fagaceae] Rhus chinensis Mill. [Anacardiaceae] Rubus fruticosus L[Rosaceae] Vaccinium myrtillus L. [Ericaceae] Depsides (ester-like linked phenolic carboxylic acids) Rosmarinus officinalis L. [Lamiaceae] Melissa officinalis L.

Origanum vulgaris L.

Sanicula europaea L. [Apiaceae] Lihospermum officinale L. [Boraginaceae] Rheum palmatum
Rheum officinale

mineral tannins:

Alum salts, such as potassium, ammonium or chrome alum 25

organic synthetic tanning agents:

Condensation products of phenolsulfonic acid, cresolsulfonic acid, urea and formaldehyde

The tannins are used in particular in the form of aqueous extracts. In this embodiment, the tannin extract is mixed with a

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Emulsifier, such as lecithin, is mixed with the Vaseline. It is also possible to use the tanning agent in the form of a suspension or emulsion (without emulsifier) mixed with the Vaseline. It is also possible to incorporate the tanning agent in powder form into the Vaseline.
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The proportion of tanning agent used is generally 10% by weight or less, preferably 5% by weight or less and in particular 1 to 2% by weight, in each case based on the total weight of the nasal ointment according to the invention.

In addition, the nasal ointment according to the invention can comprise proteins, such as albumins.

Furthermore, the nasal ointment according to the invention can comprise caring additives. All additives known for this purpose can be used as caring additives for ointments, preferably silicones, panthenol, lanolin, lecithin, dexpanthenol, provitamin B5, pantothenic acid, panthenyl ethyl ether, panthenyl ethyl ether acetate, panthenyl triacetate, allantoin, vegetable (algae, lichen) oils such as almond oil, wheat germ oil, avocado oil, waxes such as paraffins, extracts, preferably CO2 extracts such as chamomile, sea buckthorn and calendula.

To produce the nasal ointment according to the invention, the ingredients are mixed together using methods known to those skilled in the art.

The nasal ointment according to the invention can be applied with the finger or with an application aid. However, the place of application in the nose is important for the protective effect against inhalation allergic reactions. In order to achieve reliable prophylaxis, it must be ensured that the inner walls of the nose in the area of the two nasal valves are covered with the nasal ointment.

If the nasal ointment according to the invention is only applied to the lower end of the nasal vestibule in the area of the external nostrils, an inhalation allergic reaction cannot be ruled out. However, if used correctly, it is possible to achieve partial avoidance of inhalation allergens with the help of the nasal ointment according to the invention. Since the nasal ointment according to the invention cannot penetrate the nasal mucous membranes due to its special physical properties and is not absorbed, but rather forms a protective film, a mechanical barrier is created for the allergen carriers absorbed and transported with the respiratory stream. This can largely prevent the allergic reaction.

A significant advantage of the present invention is that allergic reactions are avoided without the patient's metabolism being burdened by systemic active substances. The main components of the nasal ointment, the saturated hydrocarbons mentioned above, are inert and are not absorbed. This means that the nasal ointment according to the invention can be used without risk. In addition, the effect does not diminish as the patient's organism becomes accustomed to it. The ability to smell and the associated sense of taste remain unaffected.

Further advantages of the nasal ointment according to the invention include:

comparatively low costs;

Patient can carry out the preventive treatment himself;

the application of the nasal ointment according to the invention with additive

at the same time a nourishing effect.

In addition, the nasal ointment according to the invention is not only able to prevent swelling, secretion and itching inside the nose when exposed to allergens, but also to eliminate irritation reactions in the eye and throat area.

Accordingly, the present invention also relates to the use of at least one pharmaceutically/cosmetically defined mixture of saturated hydrocarbons as defined herein as Vaseline in or as nasal ointment(s) for the prophylaxis of inhalation allergic reactions, whereby in particular atopic rhinitis of the "hay fever" type can be positively influenced.

Finally, it should be mentioned that due to the high efficiency of the nasal ointment according to the invention or the use according to the invention, a long-lasting, reliable protective effect is achieved, although very small amounts are sufficient. With amounts of just a few milligrams spread in front of the nasal valves, freedom from symptoms can be achieved for several hours even in the case of heavy pollen flight, without the need to reapply the nasal ointment according to the invention.

Claims (8)

1. Nasal ointment for the prophylaxis of inhalation allergic reactions comprising at least one mixture of saturated hydrocarbons and at least one tanning agent. 2. Nasal ointment according to claim 1, wherein the at least one mixture of saturated hydrocarbons has a viscosity according to DIN 51 562 of > 6 mm ² /s (100°C). 3. Nasal ointment according to claim 1 or 2, wherein the at least one mixture of saturated hydrocarbons comprises less than 20% by weight of linear saturated hydrocarbons (n-paraffins). 4. Nasal ointment according to one of claims 1 to 3, wherein the at least one mixture of saturated hydrocarbons has at least one of the following properties: a) Freezing point (ISO 2207) 47 to 56°C b) Cone penetration according to DIN S 1580 from 155 to 185; c) a maximum of 5 wt.% of the saturated hydrocarbons have a chain length of ≤ 25 ± 2; d) C number range of saturated hydrocarbons (determination by GC): includes C ₁₉ to C ₅₂ , each ±2; and e) Number average molecular weight: > 400, preferably > 480 and in particular > 500 g/mol. 5. Nasal ointment according to one of claims 1 to 4, wherein the at least one tanning agent is selected from: tannins from bark and wood, leaves, fruits, galls and medicinal plants; synthetic tannins and mineral tannins. 6. Nasal ointment according to one of claims 1 to 5, which additionally contains at least one care additive. 7. Nasal ointment according to claim 5, wherein the care additive is selected from silicones, panthenol, lanolin, lecithin, dexpanthenol, provitamin B5, pantothenic acid, panthenyl ethyl ether, panthenyl ethyl ether acetate, panthenyl triacetate, allantoin, almond oil, wheat germ oil, avocado oil, paraffins and CO ₂ extracts of chamomile, sea buckthorn or calendula, and mixtures of two or more thereof. 8. Nasal ointment according to one of claims 1 to 7, which further contains at least one protein.