JPH11302184A - Nasal composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a nasal composition especially having an effect for inhibiting or reducing the excitation of pituita secretion (snot) by the inflammation of nasal mucosa among the various syndromes of cold by adding zinc and a polyphenol compound. SOLUTION: This nasal composition contains (A) zinc and (B) a polyphenol compound in an amount of 10-150 pts.wt. per pt.wt. of the component A. The component A is exemplified by zinc gluconate, zinc sulfate, zinc chloride, zinc nitrate, zinc citrate, and zinc 2-oxoglutarate. The component B is exemplified by epicatechin, epigallocatechin, gallotannin, tannic acid, geraniin and leuoanthocyanidin. The composition is preferably administered with one to several portions as a preparation of topical administration form to nasal mucosa. The composition may be prepared as a solid aerosol or a liquid aerosol.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for nasal drops intended to remove or alleviate nasal mucus secretion due to inflammation of the nasal mucosa among various symptoms of colds.

[0002]

2. Description of the Prior Art Runny nose is directly a hyperfunction of the secretory line due to inflammation of the nasal mucosa. In recent years, the cause is thought to be mainly related to cold syndrome or allergy due to viral infection.

[0003] As a treatment method for allergy, a causative treatment of identifying an allergen-causing substance (allergen) and removing it is known. However, for allergic reactive rhinitis, performing causal treatments in daily life to identify and remove a very large number of allergens for each individual,
Generally very difficult. In addition, desensitization therapy for reducing sensitivity to allergens has problems such as a long treatment period and frequent hospital visits.

[0004] For allergic rhinitis, therefore, symptomatic treatment is regarded as important both in treatment and in daily life. In particular, nasal discharge symptoms due to inflammation of the nasal mucosa include QOL (qual
From the viewpoint of ity of life) and from the viewpoint of prevention of respiratory infections such as colds, it is important to improve the drug at an early stage, and nasal compositions containing antiallergic drugs have been developed.

[0005]

However, while some antiallergic drugs generally have side effects such as sleepiness, nasal congestion and nasal discharge often occur frequently.
Therefore, development of a composition for nasal drops suitable for repeated administration regardless of time for symptomatic treatment has been awaited.

[0006]

Means for Solving the Problems The inventors of the present invention have been studying the development of a composition for nasal drops, and found that a composition for nasal drops containing zinc and polyphenols is effective in increasing nasal secretion. The present inventors have found that they exhibit a dramatic inhibitory effect, and have completed the present invention.

[0007] That is, the present invention is a nasal composition containing zinc and polyphenols.

[0008] Zinc is a trace element that is contained in all human tissues and body fluids and has the second highest content after iron. As its physiological activity, it has been reported that growth and skeletal development and activation of metabolism of the skin and its accessory organs are reported. Also, it has been reported that the function of immune system organs such as the thymus decreases when zinc is deficient.

[0009] The polyphenols in the present invention are phenylpropanoid compounds contained in plants.
And a generic term for flavonoid compounds. Among them, tannin and epigallocatechin are known to have effects of promoting excretion of fat and cholesterol, normalizing lipids in blood, and reducing infectivity of viruses.

However, the effect of the combined use of zinc and polyphenols synergistically suppresses the hyperactivity of the secretory line due to inflammation of the nasal mucosa, which is a symptom after suffering from a cold or allergy. Was not known until then.

According to the present invention, since zinc and polyphenols can drastically suppress hypersecretion due to inflammation of the nasal mucosa, chlorpheniramine maleate and the like commonly used in nasal drops are generally used. A nasal composition can be prepared with no or all anti-allergic agents.

In the present invention, the mixing ratio of zinc to polyphenols is such that the polyphenols are added to 1 part by weight of zinc in order to achieve a synergistic effect of suppressing the secretory line hyperfunction caused by inflammation of the nasal mucosa. 10 parts by weight to 150
It is preferable to use parts by weight.

In the present invention, zinc is preferably incorporated into the composition in the form of a compound of an inorganic acid salt or an organic acid salt. Examples of such a compound include zinc gluconate, zinc sulfate, zinc chloride, zinc nitrate, zinc citrate, and zinc 2-oxoglutarate.

The polyphenols that can be used in the present invention include the hydrolyzable tannins such as gallic acid, tannin, tannic acid and geraniin, and the condensed tannins such as catechin, epigallocatechin, epicatechin gallate and m-glycan. Galloylgallic acid, luteoic acid, elagic acid, hexahydroxy diphenic acid, Chinese gallotannin, morrisacacidin, melacacidin, leucocyanidin, leucoanthocyanidin and the like can be exemplified.

[0015]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, various medicinal ingredients can be added, if necessary, for the purpose of improving the symptoms of a cold. For example, antihistamines such as diphenhydramine or salts thereof, antiallergic drugs such as mequitazine, sympathomimetics such as phenylpropanolamine or salts thereof, parasympathomimetics such as isopropamide iodide, inflammation enzymes such as lysozyme chloride and bromelain. Drugs, anti-inflammatory drugs such as tranexamic acid and glycyrrhizic acid, vitamins such as vitamin B1 or derivatives thereof, and the like.

Also, spicy, garlic, (dried) ginger, licorice, saiko, cinnamon bark (branch), mao, river kyu, ground yellow, bellflower, wheat gate winter,
Herbal powders such as Xinyi, Tingji, scented scent, eucalyptus, lavender, light load, etc., and extracts thereof can also be incorporated at the same time.

The composition for nasal drops of the present invention is preferably administered once or several times as a preparation for topical administration to the nasal mucosa. In addition, the dose can be appropriately increased or decreased depending on the age, body weight, and medical condition.

The nasal composition of the present invention can be prepared as a solid spray or a liquid spray. As an additive used in the preparation of these preparations, in the case of a solid spray, an excipient such as crystalline cellulose, a binder such as hydroxypropylcellulose, hydroxypropylmethylcellulose, gelatin, PVP, magnesium stearate, Lubricants such as hardened castor oil and talc, preservatives, and the like. In the case of a liquid spray, a surfactant, a solubilizing agent, a buffer, and the like, a preservative, a fragrance (menthol, camphor, etc.) ), Dyes, preservatives and the like can be used.

[0019]

The composition for nasal drop of the present invention can exert an extremely excellent symptomatic effect on hyperactivity of secretory glands due to inflammation of the nasal mucosa among various symptoms of cold. .

[0020]

EXAMPLES Hereinafter, the present invention will be described in more detail by way of examples and test examples, but the present invention is not limited to these examples.

Example 1 50 mg of zinc gluconate (the same applies to the following units) Catechin 500 Ipratropium bromide 100 Lidocaine hydrochloride 250 After weighing and uniformly mixing each of the above components and amounts, dissolving in 100 ml of purified water and dissolving the liquid agent Prepared.

Example 2 Zinc sulfate 15 mg (the same applies to the following units) Tannic acid 250 Lysozyme chloride 250 Lidocaine hydrochloride 300 The above components and amounts are weighed and uniformly mixed, and then dissolved in 100 ml of purified water to prepare a liquid preparation. did.

Example 3 Zinc Gluconate 10 mg (the same applies to the following units) Tannin 150 Tetrahydrozoline hydrochloride 100 Ketotifen fumarate 35 Oxytropium bromide 450 Lysozyme chloride 250 Lidocaine hydrochloride 250 Benzethonium chloride 20 The above components and amounts are weighed. After uniform mixing, the mixture was dissolved in 100 ml of purified water to prepare a solution.

<Example 4> Zinc gluconate 20 mg (same unit below) Catechin 200 Oxymetazoline hydrochloride 25 Ketotifen fumarate 50 Belladonna total alkaloids 50 Fluticasone propionate 50 Lysozyme chloride 250 Lidocaine hydrochloride 250 l-Menthol 10 Benzethonium chloride 20 After weighing and uniformly mixing the components and amounts of the above, the resulting mixture was dissolved in 100 ml of purified water to prepare a liquid preparation.

<Test Example> The components and amounts shown in Table 1 were diluted in 100 ml of purified water for each group, and 0.2 ml of each ddY male rat was intranasally administered to 5 male ddY rats in each group. Two hours after the administration, the nasal cavity was incised, the amount of secretion fluid on the nasal mucosa was measured, and the average value was calculated.
Each 2 ml was administered intranasally. ).
Table 2 shows the results.

The degree of suppression of the amount of nasal secretion is enhanced in the group as compared with the other groups, and it is clear that the remedy for cold symptoms combined with the active ingredient of the present invention exhibits an excellent inhibitory effect on secretory gland response. Proven.

[0027]

[Table 1]

[0028]

[Table 2]

[0029]

Claims (4)

[Claims] 1. A nasal composition comprising zinc and polyphenols. 2. The nasal composition according to claim 1, wherein the polyphenols are mixed in an amount of 10 to 150 parts by weight with respect to 1 part by weight of zinc. 3. The nasal drop according to claim 1, wherein the polyphenol is at least one selected from the group consisting of epicatechin, epigallocatechin, gallotannin, tannic acid, geraniin, and leukoantocyanidin. Composition. 4. The method according to claim 1, wherein the zinc is derived from one or more compounds selected from the group consisting of zinc gluconate, zinc sulfate, zinc chloride, zinc nitrate, zinc citrate and zinc 2-oxoglutarate. The nasal composition according to claim 1, 2, or 3.