DE19517251A1 - Use of D-(+) pantothenyl-alcohol to treat dry nose - Google Patents

Abstract

The use of D-(+) pantothenyl alcohol ('Dex panthenol') (I) is claimed for the treatment of dry mucous membranes of the nose (rhinitis sicca).

Description

The present invention relates to the use of D - (+) - pantothenyl alcohol (dexpanthenol, especially as Solution in physiological saline, for treatment dry nasal mucous membranes.

For drug treatment of chronic rhino Pathies - in particular rhinitis sicca - have so far been identified no suitable and effective means available. Therapy attempts are at best with ointments Base of paraffin hydrocarbons or vegetable fats in front. This will dry out the nasal mucus at best made the skin supple again without it a healing effect on the mucous membranes is coming.

In addition, the use of fat by patients containing ointments due to the additional nasal breathing disability is perceived as unpleasant - with the result poor compliance.

Anti-inflammatory effect and increase in infection Defense against dexpanthenol are already known (for example Weise Weber, Deutsche Apotheker Zeitung 123, 1921 (1983) and accordingly it is already in shape pharmaceutical preparations on the market (Red List 1994).

EP-A 53 754 describes an agent for combating Snoring, which in physiological saline a surface-active substance and optionally also Contains dexpanthenol. For the desired effect there comes especially the surfactant  crucial to. To treat drier This remedy is not suitable for nasal mucous membranes, yes even prohibits it because surface-active substances Do not promote wound healing, but delay it.

From DE-A 38 32 401 is also already one pharmaceutical preparation containing dexpanthenol in physio contains logical saline, for treatment ent inflamed nasal mucous membranes.

It has now surprisingly been found that after topical Application of dexpathenol in patients with rhinitis sicca (dry nasal mucosa) compared to Placebo the bark formation is clearly reduced. The Clinical differences are found by the company toric analysis according to the initial hypothesis as statistically significant. The extent of bark formation improved by 1.04 during treatment with verum and with placebo only by 0.33 scores. With this preparation tion is now possible by proliferation of Fibroblasts cause rapid wound healing.

The present invention thus relates to the use of D - (+) - pantothenyl alcohol (dexpanthenol) for treatment lung dry mucous membranes.

For the use according to the invention, dexpanthenol advantageously in the form of pharmaceutical preparations applied.

These preparations can be liquid or viscous be semi-solid. You can e.g. B. as ointments, creams or Gels for introduction into the nose or as solutions for There are drops or sprays.

Suitable carriers for liquid dosage forms  especially aqueous systems with or without the addition of Glycerol, sorbitol and other polyols.

As carriers for viscous or semi-solid pharmaceuticals medicinal preparations such as B. ointments, creams or Gels are suitable for. B. paraffin hydrocarbons, Petroleum jelly, wool wax products and other pharmaceuticals usable viscosity-increasing raw materials at hydro phile gels e.g. As water, glycerol or sorbitol with suitable swelling agents, such as. B. polyacrylic acid, Cellulose derivatives, starch or tragacanth are gelled.

The pharmaceutical preparations contain dexpanthenol preferably in amounts of 0.2 to 20% by weight, particularly preferably 5 to 10% by weight.

Preferred pharmaceutical preparations are aqueous Solutions, especially solutions of dexpanthenol in physiological saline (i.e. 0.9% by weight cook salt solution), the dexpanthenol in an amount of 5% by weight contain.

In addition to the Active and carrier substances and any present Emulsifiers and other pharmaceutically acceptable and auxiliary and / or additive compatible with the active ingredients fabrics such as B. filling, stretching, binding, mesh, stabili sierungs-, dyes, buffers and fragrances contain. Furthermore, microbiologically active chemical ver bonds, such as B. preservatives or antisep tica, to improve microbial stability in the usual pharmaceutical concentrations in the preparation tions are included.

In addition, the preparations can also  or several other pharmacologically active substances contain. In particular, other connections can be made with pantothenic acid effect in free form and / or in Form of derivatives may be included.

The preparations are produced by mixing or dissolving the active substances in the pharmacological effective concentration, the auxiliary and / or additives as well as any other pharmacologically active seed substances in the intended carrier medium.

example 1

To prepare 100 g of a clear aqueous solution are mixed in a glass vessel with a stirring device 0.9 g Na trium chloride and 5 g dexpanthenol with 90 g purified Pour water and the substances thoroughly Stir clearly dissolved. The solution becomes 0.02 g benzalkoni added umchloride as a preservative and the same if dissolved with stirring. Finally, with more what water to the final weight of 100.0 g and homogeneous touched. If necessary, the solution must be neutral be filtered. The clear, odorless Liquid becomes 10 in narrow-necked amber glass bottles or 20 ml filled, which optionally with a drip pi pette or a spray metering pump can.

Use: One drop several times a day as needed or give a spray in each nostril and on pull.  

Example 2

For the preparation of 100 g of a clear buffered aq solution with an increased pantothenic acid effect in a glass jar with stirring device 0.9 g of table salt and Pour 85 g of purified water over 7.5 g of dexpanthenol and clearly dissolved by thorough stirring. For setting a stable pH of 5.3, the solution becomes 0.756 g of potassium dihydrogen phosphate and 0.024 g of sodium monohydro genphosphate dodecahydrate as buffer substances and Preservation 0.02 g benzalkonium chloride added and dissolved with stirring. The solution comes with more water filled up to the final weight of 100.0 g and homogeneously ge stirs. If necessary, over neutral cellulose fiber filtered. The clear, odorless liquid is in Bottled narrow-neck bottles made of amber glass of 10 or 20 ml, which either with a dropper or a Spray dosing pump can be equipped.

Use: 3 to 5 times a day or one as needed Put drops or sprays in each nostril and wind up.

Example 3

For the preparation of 100 g of a clear buffered aq solution with increased adherence becomes 0.9 g Koch salt and 5 g dexpanthenol and 0.02 g benzalkonium chloro rid as a preservative in a glass jar with stirring Pour 80 g of purified water over the device and clearly dissolved by stirring. To set a stable pH of 5.3, the solution 0.756 g of potassium diihy drug phosphate and 0.024 g sodium monohydrogen phosphate Dodecahydrate added and dissolved with stirring. To Her deposition of the surface tension and increase of the viscosity  5 g of sorbitol solution and 70% of the solution 5 g of glycerol 85% added and the mixture with further Replenished water to a final weight of 100.0 g. Last is stirred until streak-free and if necessary, filtered through neutral cellulose filters. The clear, odorless liquid is in narrow-neck bottles filled from amber glass to 10 or 20 ml, which either with a dropper or a spray Dosing pump can be equipped.

Use: One drop several times a day as needed or give a spray in each nostril and wind up.

Example 4

To prepare 100 g of a solution according to Example 3, however with an increased pantothenic acid effect, are in a glass vessel with a stirring device 0.9 g of table salt and 10 g dexpanthenol and 0.02 g benzalkonium chloride as Kon Pour 75 g of purified water over the dish and clearly dissolved by thorough stirring. To reduce increase in surface tension and increase in viscosity and the adhesive are added 5 g of sorbitol Solution and 5 g glycerol 85% added and the mixture with additional water to the final weight of 100.0 g fills. Then it is homogeneous until streak-free stirs and, if necessary, over neutral cellulose filters filtered. The clear, odorless liquid is in Bottled narrow-neck bottles made of amber glass of 10 or 20 ml, which either with a dropper or a Spray dosing pump can be equipped.

Use: 3 to 5 times a day or one as needed Put drops or a spray in each nostril and wind up.  

Example 5

To make 100 g of a viscous gel leaves one in a closable glass jar 0.625 g of polyacrylic Swell acid in 50 g of purified water to a sol. After about 24 hours, 0.1 g with intensive stirring Ammonia solution 10% entered, with gel formation puts. 0.9 g are then placed in a second glass vessel Table salt and 5 g dexpanthenol and 0.02 g benzalkonium chloride as a preservative in 40 g of purified Water dissolved and the clear solution in turn under active stirring slowly introduced into the polyacrylate gel. Finally, with further water, the final weight is 100.0 g filled up and the product stirred until homogeneous. You get an almost clear, colorless and odorless thick liquid gel, which is divided into small tubes of 5 or 10 g, with the application tip pulled out.

Application: If necessary, a small one several times a day Introduce the portion of gel as high as possible into both nostrils and raise.

Example 6

To make a creamy nose ointment are in one Glass jar with stir bar 0.9 g of table salt and 5 g Dexpanthenol and 0.02 g benzalkonium for preservation chloride dissolved in purified water to 30.0 g. In a Ointment grater with pestle is the aqueous active ingredient Solution incorporated in 70 g of wool wax alcohol ointment and finely emulsified with vigorous stirring. You get one white, soft nose ointment, which is in small tubes of 5 or 10 g, with the application tip pulled out becomes.  

Application: If necessary, a small por several times a day Pour ointment into each nostril and after softening by raising the body temperature.

Application example

47 patients with dry nasal mucosa became two up to three times a day in the form of a solution according to Example 1 sprayed into the nose (verum). For comparison, 48 patients received the same Conditions only physiological saline (Placebo).

The extent of bark formation was assessed by rhinoscopic examinations by a doctor. The results given in Table 1 (verum) and Table 2 (placebo) were obtained. In it, x stands for the mean and S _D for the standard deviation.

Table 1 (verum)

Extent of bark formation *

Table 2 (placebo)

Extent of bark formation *

Claims (5)

1. Use of D - (+) - pantothenyl alcohol (dexpanthenol) for the treatment of dry nasal mucous membranes. 2. Use according to claim 1, characterized in that dexpanthenol in the form of pharmaceutical preparation is applied. 3. Use according to claim 2, characterized in that that the preparations are liquid or viscous are semi-solid. 4. Use according to claim 2 and / or 3, characterized ge indicates that the preparations dexpanthenol in Quantities from 0.2 to 20% by weight, particularly preferably 5 to 10% by weight. 5. Use according to one or more of claims 2 to 4, characterized in that a 5 wt.% Solution of dexpanthenol in physiological common salt solution is used.