CZ14266U1 - Pharmaceutical composition intended for treating nasal cavity - Google Patents

Description

(54) Utility model name:

A pharmaceutical composition for treating the nasal cavity

WHAT

WHAT

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CZ 14266 Ul

A pharmaceutical composition for treating the nasal cavity

Technical field

The invention relates to a novel composition, in particular drops and a spray, for treating the nasal cavity. The composition is particularly useful for treating rhinitis and acute or chronic sinusitis. BACKGROUND OF THE INVENTION

For the treatment of rhinitis and other nasal cavity problems, topical formulations acting directly on the nasal mucosa are widely used. The form of these preparations is primarily droplet, but very often may be ointments, creams or gels.

At present, these preparations contain either substances reducing the nasal congestion (decongestant effect), according to a mechanism of action called sympathomimetics, or substances with a healing, anti-inflammatory or antimicrobial effect, or substances preventing the nasal mucosa from drying out. The proportion of local antiallergic drugs is significant.

The decongestant effect is the main cause of the elimination of subjective problems associated with the cold. The State Institute for Drug Control (SUKL) has registered a number of substances suitable for this use.

Sympathomimetics intended for nasal applications registered at the Czech SUKL:

Cyclopentamine

Ephedrine

Fenylefrin

Oxymetazoline

Tetryzoline

Xylometazoline

Nafazolin

Tramazoline

Metizoline

Tuaminoheptan

Fenoxazoline

Tymazolin

Epinephrine (adrenaline).

This is undoubtedly the broadest group of drugs for local treatment of the nasal cavity.

Of these, oxymetazoline, tetryzoline, naphazoline and xylometazoline are the most used. A variety of rhinitis products are sold with these active substances in adults and children.

A disadvantage of preparations containing this group of substances is the simultaneous irritation of the nasal mucosa. It is typical of conventional sympathomimetic agents that, after a favorable decongestant effect, an adverse irritation effect occurs and subjective problems increase again (rebound effect).

On the other hand, another type of healing, anti-desiccant, has a lower effect against subjective complaints and thus does not provide the necessary rapid relief to the extent that sympathomimetics.

The essence of the solution

The subject of the invention is a pharmaceutical composition comprising both a sympathomimetic having a decongestant effect and a substance which removes or at least alleviates irritation of the nasal mucosa associated with the action of the former. Such a substance may be, for example, panthenol, dexpanthenol or pantothenic acid. These substances, in particular dexpanthenol, reduce the toxic effect of the sympathomimetic (oxymetazoline) and improve the growth of the ciliary epithelial cells, reduce the mucosal dryness, reduce the healing effect and hence the secretion from the nose. Accordingly, the present invention provides a pharmaceutical composition for treating the nasal cavity comprising a substance having a sympathomimetic effect in an amount of 0.005 to 0.2% by weight. and at least one negative effect mitigant selected from the group consisting of pantothenic acid, panthenol and dexpanthenol, in an amount of 1 to 10 wt. based on the total volume of the composition.

The pharmaceutical composition of the present invention is a mixture of the active ingredients with at least one pharmaceutically acceptable excipient.

Thus, they may be aqueous solutions or suspensions in the form of drops or sprays, or so-called semi-solid formulations such as ointments, creams or gels. Typical excipients for ointments and creams are fatty bases, which often form an emulsion with an aqueous solution of the active ingredients. The gels may be formed on a fat or emulsion basis or on an aqueous basis.

The choice of pharmaceutical excipients is not essential for solving the problem.

In addition to the basic combination of two substances, the composition of the present invention may contain substances with a supportive effect. These may be substances which prevent the nasal mucosa from drying out, have an antimicrobial effect, have a healing effect or have an overall refreshing effect on the patient.

These are mainly etheric oils such as eucalyptus, pinus sylvestris or menthol. The healing effect can be further enhanced by the addition of vitamin E.

Examples

Example 1

Liquid nasal preparation, preferably drops

Oxymetazoline hydrochloride, dexpanthenol, a mixture of ethereal oils and vitamin E in the form of acetate (tocopherol acetate), was used as a sympathomimetic for the preparation of the liquid preparation. The specific composition is shown in the following table:

Substance amount in g / 100 ml oxymetazoline hydrochloride 0.05 dexpanthenol 5 pinus sylvestris 0.05 eucalyptus oil 0.02 menthol 0.02 tocopherol acetate 0.1

Further, other solubility enhancers, a preservative and so on have been used. All was transferred to an aqueous suspension. If necessary, the suspension was filled into vials (nasal drops) or spray applicators.

Claims (8)

PROTECTION REQUIREMENTS A pharmaceutical composition for the treatment of the nasal cavity, characterized in that it contains a substance having a sympathomimetic effect in an amount of 0.005 to 0.2% by weight. and at least one adverse effect reducing agent selected from the group consisting of pantothenic acid, panthenol and dexpanthenol, in an amount of 1 to 10% by weight based on the total volume of the composition. 2. The composition of claim 1 further comprising etheric oils selected from eucalyptus, pinus sylvestris, menthol, optionally a mixture thereof, and optionally vitamin E. Composition according to claim 1 or 2, characterized in that the substance with a sympathomimetic effect is selected from the group consisting of oxymetazoline, naphazoline, tetryzoline and xylometazoline. Composition according to claim 3, characterized in that oxymetazoline is selected as the sympathomimetic agent. Composition according to claim 4, characterized in that the oxymetazoline is present in an amount of 0.01 to 0.05% by weight, based on the total volume of the composition. Composition according to any one of the preceding claims, characterized in that the content of ether oils is selected in the range of 0.01 to 0.2% by weight, based on the total volume of the composition. 7. A composition for treating the nasal cavity comprising 0.01 to 0.075 wt. % oxymetazoline, 2 to 5 wt. % dexpanthenol, 0.02 to 0.1 wt. % pinus sylvestris, 0 to 0.05 wt. % eucalyptus oil, 0.005 to 0.05 wt. % menthol and 0.02 to 0.2 wt. vitamin E in the form of tocopherol acetate, based on the total volume of the composition. Composition according to any one of the preceding claims, characterized in that it is in liquid form, applicable as drops or sprays.