JP2001089375A - Common cold composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for colds with an enhanced effect on nasal congestion among various symptoms caused by a cold, particularly rhinitis caused by a cold. SOLUTION: The composition for colds containing (a) emedastine or a pharmaceutically acceptable salt thereof and (b) acetaminophen or ibuprofen.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a composition for colds. In particular, the present invention relates to a common cold composition having an enhanced effect on nasal congestion (nasal congestion) among rhinitis symptoms caused by a cold.

[0002]

2. Description of the Related Art The cold syndrome is a viral respiratory tract infection, and is generally a disease accompanied by various systemic symptoms such as malaise and local inflammatory symptoms mainly in the upper respiratory tract. Therefore,
For the virus that causes a cold, administration of a drug that has an antiviral effect that suppresses the infection and proliferation of the virus is desirable as a causal therapy, but at present, no effective antiviral drug has been developed, and individual colds have not been developed. Symptomatic treatment aimed at improving symptoms has been the mainstay of cold treatment.

The improvement of inflammatory symptoms of the nasal mucosa due to a cold is no exception. A drug containing an antihistamine as a main component and a nasal secretion inhibitor or a sympathomimetic for removing nasal congestion is included. Symptomatic treatment by administration was central.

[0004] However, the ameliorating effects of these drugs on the inflammatory symptoms of the nasal mucosa caused by colds have not been sufficient.

On the other hand, emedastine or a pharmaceutically acceptable salt thereof is known to have a histamine release inhibitory action and an antihistamine action, and diseases caused by histamine, such as allergic skin disease and allergic rhinitis It has been used as a prophylactic and therapeutic agent. However, there has been no report that emedastine or a pharmaceutically acceptable salt thereof is applied to rhinitis due to a cold and has obtained an excellent ameliorating effect over a conventional antihistamine-based drug.

[0006]

DISCLOSURE OF THE INVENTION The present invention relates to various symptoms caused by a cold, particularly inflammatory symptoms of the nasal mucosa caused by a cold (such as nasal congestion).
It is an object of the present invention to provide a cold remedy composition in which the effect of improving cold is improved.

[0007]

Means for Solving the Problems The inventors of the present invention have conducted intensive studies to solve the above problems, and as a result, acetaminophen or ibuprofen, which is known as an antipyretic analgesic component, for emedastine or a pharmaceutically acceptable salt thereof. The present invention has been found to have a dramatic improving effect on the removal or alleviation of various symptoms caused by a cold, particularly inflammatory symptoms (such as nasal congestion) of the nasal mucosa, and have completed the present invention. That is, the present invention is a composition for colds comprising (a) emedastine or a pharmaceutically acceptable salt thereof and (b) acetaminophen or ibuprofen.

In the present invention, emedastine is a known compound (US Pat. No. 4,430,343), and pharmaceutically acceptable salts include hydrochloride, nitrate, sulfate, phosphate, oxalic acid. Salt, maleate, fumarate, hydrobromide and the like can be mentioned.

In the present invention, the amount of emedastine or a pharmaceutically acceptable salt thereof is the same as that of acetaminophen 1
It is usually 0.0001 to 0.01 parts by weight with respect to parts by weight.
004 to 0.005 parts by weight is preferred. It is usually 0.0005 to 0.01 part by weight with respect to 1 part by weight of ibuprofen.
It is preferably from 0008 to 0.007 parts by weight.

The acetaminophen and ibuprofen in the present invention both have antipyretic analgesic action,
It is used as a common cold medicine. These may be blended alone or in combination of two types.

[0011]

BEST MODE FOR CARRYING OUT THE INVENTION The cold-sensitive composition of the present invention comprises a tablet,
It can be provided as various oral administration forms such as capsules, granules, fine granules, powders, chewables, foaming agents, drops, mouth dissolving agents, dry syrups, and oral liquids. These preparations can be prepared by a conventional method.

[0012] In the case of solid preparations, as a carrier used for preparing a preparation, excipients such as lactose, starch, sugar, mannitol, crystalline cellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, gelatin,
There are binders such as PVP, disintegrators such as carboxymethylcellulose calcium and low-substituted hydroxypropylcellulose, and lubricants such as magnesium stearate, hydrogenated castor oil, and talc. , Preservatives, flavors, pigments, flavoring agents and the like can be used.

[0013] In the oral liquid preparation, a carrier used for preparation of the preparation includes surfactants such as sucrose fatty acid esters, polyoxyl stearate, polyoxyethylene polyoxypropylene glycols and polyoxyethylene mono fatty acid esters. , Synthetic aluminum silicate,
Thickeners such as magnesium silicate, magnesium carbonate, magnesium oxide, magnesium metasilicate aluminate,
There are organic acid-based and inorganic acid-based pH adjusters such as citrate buffer, phosphate buffer, etc.
Buffers, preservatives, flavors, dyes, sweeteners and the like can be used.

The composition for colds of the present invention may contain, if necessary, other nonsteroidal anti-inflammatory drugs, anti-inflammatory enzymes, bronchodilators, central nervous stimulants, antitussives, expectorants in addition to the above-mentioned components. And at least one drug selected from antihistamines, other antiallergic drugs, anticholinergic drugs, vitamins, antacids, crude drugs and the like. These components can be used alone or as a mixture with each other. Usually, these components are blended in accordance with the cold medicine standards and the like described in the Pharmaceutical Manufacturing Guideline (1995 edition of Pharmaceutical Times).

[0015]

The present invention will be described below in more detail with reference to Examples and Test Examples. (Example 1) Ibuprofen 600g noscapine 48g phosphoric acid dihydrocodeine 24g fumarate emedastine 1g ambroxol hydrochloride 45g phenylpropanolamine 60g theophylline 150g Lysozyme chloride 90 g (potency) of anhydrous caffeine 75g Vitamin B ₁ nitrate 8g vitamin B ₂ 4g Lactose 300g Microcrystalline cellulose 275 g Hydroxypropyl cellulose 100 g Magnesium stearate 10 g Hardened castor oil 10 g After weighing and uniformly mixing the above components, the resulting mixed powder was tabletted to obtain a tablet weighing 200 mg per tablet.

Example 2 Acetaminophen 900 g Noscapine 48 g Dihydrocodeine phosphate 24 g Emedastine fumarate 2 g Bromhexine hydrochloride 12 g Lysozyme chloride 90 g (titer) Lactose 300 g Microcrystalline cellulose 300 g Hydroxypropyl cellulose 105 g Magnesium stearate 10 g Hardened castor oil 10 g After weighing and uniformly mixing the above components, a tablet weighing 200 mg was obtained according to Example 1.

Example 3 Ibuprofen 400 g Emedastine fumarate 1.5 g Dihydrocodeine phosphate 24 g Ambroxol hydrochloride 45 g Lysozyme chloride 90 g (titer) Lactose 100 g Hydroxypropylcellulose 50 g Low-substituted hydroxypropylcellulose 60 g Magnesium stearate 15 g Curing Castor oil 15 g After weighing and uniformly mixing the above components, a tablet weighing 100 mg was obtained according to Example 1.

(Example 4) Acetaminophen 900 g Dihydrocodeine phosphate 24 g Emedastine fumarate 1 g dl-methylephedrine hydrochloride 60 g Ambroxol hydrochloride 45 g Anhydrous caffeine 75 g Vitamin B ₁ nitrate 8 g Vitamin B ₂ 4 g Sucrose fatty acid ester 15 g Mannitol 15 g Stevia 10 g Ethyl aminobenzoate 5 g Orange flavor 0.8 g Preservative (ethyl aminobenzoate), sweetener (mannitol, stevia), flavoring agent (orange flavor) in an aqueous solution in which a pH adjuster (phosphate buffer) is dissolved. Was added and completely dissolved, and after the sucrose fatty acid ester was uniformly dispersed in the solution, emedastine fumarate and other drugs were added and dissolved, and purified water was added to make the total volume 1000 ml to prepare an oral liquid preparation. .

[Test Example 1] [Effect of Combination Formulation on Olfactory Intensity] << Test Method >> Five subjects in each of six groups A to F, targeting 30 subjects having a nasal congestion (nasal congestion) due to a cold. To prepare tablets containing the components shown in Table 1,
The administration was performed three times a day for three days, and the results were compared. The judgment method is 2
This was done by measuring the olfactory intensity of the volatile aroma using a paper soaked with a 0% menthol solution. According to the following criterion, the change was 3 based on the olfactory intensity before administration.
Judgment was made on each day until the day after, and comparison was made using the average score of each group. The results are shown in Table 2. Judgment criteria 4 points: Feel the irritating odor of menthol 3 points: Feel the irritating odor of menthol 2 points: Hardly feel the irritating odor of menthol 1 point: Don't feel the irritating odor of menthol

[0020]

[Table 1]

[0021]

[Table 2]

Regarding the degree of olfactory intensity, the combination prescription group of groups A and B is superior to the control group of groups C to E, and it has been proved that the above-mentioned combination drugs have an excellent effect of improving rhinitis. Was.

[Test Example 2] An olfactory intensity test similar to that of Test Example 1 was carried out on 10 subjects having normal rhinitis symptoms other than a cold. The results are shown in Table 3.

[0024]

[Table 3]

[Test Example 3] Tablets containing the components shown in Table 4 were prepared, and the same odor test as in Test Example 1 was carried out on 30 subjects with nasal congestion (stuffy nose) due to a cold. . Table 5 shows the results.

[0026]

[Table 4]

[0027]

[Table 5]

From the results of Test Examples 1 and 2, the composition for colds according to the present invention exerts a remarkable effect on the improvement of rhinitis due to a cold, and the results of Test Examples 1 and 3 show that the composition for colds according to the present invention is effective. It has been found that the composition for use is superior to the conventional formulation containing an antihistamine as a main ingredient in improving the rhinitis caused by a cold.

[0029]

Industrial Applicability The present invention is a common cold composition which has a dramatic effect on the elimination and reduction of nasal congestion symptoms in order to enhance and improve the anti-inflammatory effect on inflammation of the nasal mucosa. It has become possible to provide a remarkably useful drug for nasal congestion (congestion of the nose).

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI theme coat ゛ (Reference) (A61K 31/551 (A61K 31/551 31: 192) 31: 192)

Claims (4)

[Claims] 1. A composition for colds comprising (a) emedastine or a pharmaceutically acceptable salt thereof and (b) acetaminophen or ibuprofen. 2. The cold-sensitive composition according to claim 1, wherein the component (a) is contained in an amount of 0.0001 to 0.01 part by weight based on 1 part by weight of acetaminophen. 3. An amount of (a) per 1 part by weight of ibuprofen
2. The composition according to claim 1, comprising 0.0005 to 0.01 parts by weight of the component.
The composition for colds as described. 4. The composition for colds according to claim 1, which is a composition for rhinitis.