JP2001199882A - Composition for cold and rhinitis - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for cold and rhinitis having excellent effect against congested nose among the rhinitis symptoms caused by the cold or the like. SOLUTION: The objective cold and rhinitis composition is obtained by formulating the following components (a) and (b): (a) loxoprofens and (b) at least one selected from the group of allergic drugs and the group of antihistaminic drugs.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a common cold symptom having an enhanced effect on nasal congestion (congestion of the nose).
It relates to a composition for rhinitis.

[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.

[0003] Drugs having antiviral activity are desired as causal treatments for the cold syndrome, but effective drugs have not been developed yet, and symptomatic treatments are mainly used to improve the cold syndrome. The focus of symptomatic treatment is antipyretic fever due to antipyretic analgesic components and analgesia at the onset of pain symptoms, and drugs such as loxoprofen have been used to improve these symptoms.

[0004] However, in performing daily life, among various symptoms caused by a cold, nasal inflammation, particularly nasal congestion (nasal congestion) causes respiratory failure, and must be compensated by mouth respiration. The direct ingestion of fresh air into the lungs has led to the infection of new viruses and bacteria, which has led to the inconvenience of prolonged symptoms.

[0005] Therefore, by improving the symptoms of nasal congestion (nasal congestion) at an early stage of a cold, remission of the symptoms or promotion of healing can be expected.

Hitherto, antihistamines have been mainly used to improve the inflammatory symptoms of the nasal mucosa, and in addition to these, those containing a nasal secretion inhibitor, a sympathomimetic for the purpose of removing nasal congestion, and the like are also known. Although they were mainly used, all of them had insufficient effects on inflammatory symptoms of the nasal mucosa caused by colds and the like.

[0007]

SUMMARY OF THE INVENTION An object of the present invention is to provide a composition for colds and rhinitis which is specialized in eliminating or alleviating inflammatory symptoms (such as nasal congestion) of nasal mucosa among various symptoms of colds. And

[0008]

Means for Solving the Problems The present inventors have conducted various studies in order to achieve the object. As a result, the simultaneous incorporation of loxoprofen and an antiallergic or antihistamine as active ingredients simultaneously allows the inflammation of the nasal mucosa to occur. The present inventors have found that a dramatic effect is exerted on the removal or reduction of nasal congestion and the like, and completed the present invention.

That is, the present invention is a composition for cold and rhinitis comprising (a) loxoprofen, and (b) an antiallergic or antihistamine.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, loxoprofen is loxoprofen and a pharmaceutically acceptable salt thereof, and they can be used as a mixture. The compounding amount of loxoprofen is 9 per day for adult.
0-180 mg is preferred.

As the antiallergic or antihistamine in the present invention, carbinoxamine, chlorpheniramine, ketotifen, mequitazine, epinastine and salts thereof are preferred. Here, the salt means a hydrochloride,
Nitrate, sulfate, phosphate, oxalate, maleate, fumarate, hydrobromide, potassium salt, sodium salt, calcium salt, magnesium salt and the like can be mentioned.

The amount of the antiallergic drug or antihistamine drug is 5 to 10 mg per day for carbinoxamine or a salt thereof, 2 to 10 mg for chlorpheniramine or a salt thereof, and 2 for mequitazine or a salt thereof.
~ 12 mg, in the case of ketotifen or its salts 0.5 ~
3 mg, and preferably 2 to 25 mg in the case of epinastine or a salt thereof.

The amount of the antiallergic drug or antihistamine drug to 1 part by mass of loxoprofen is 0.01 to 0.1 part by weight for carbinoxamine or a salt thereof, and 0.00 for chlorpheniramine or a salt thereof.
5 to 0.1 part by weight, 0.005 to 0.05 part by weight for ketotifen or a salt thereof, 0.01 to 0.1 part by weight for mequitazine or a salt thereof, 0.05 to 0.1 part by weight of epinastine or a salt thereof 0.5 parts by weight are each preferred.

The composition for colds and rhinitis of the present invention can usually be orally administered to an adult once or several times a day, and the dosage may be appropriately adjusted according to age, weight, and medical condition. Can be.

The composition for colds and rhinitis of the present invention may be in the form of tablets, capsules, granules, fine granules, chewables,
Foaming agent, dropping agent, dissolving agent in mouth, dry syrup,
The preparation can be made into an oral administration form such as an oral solution and can be produced by a conventional method.

When manufacturing the composition for colds and rhinitis of the present invention, if necessary, other nonsteroidal anti-inflammatory drugs, anti-inflammatory enzymes, bronchodilators, central nervous stimulants, antitussives,
It may also contain expectorants, other antihistamines, other antiallergic drugs, anticholinergic drugs, vitamins, antacids, crude drugs, and the like.

[0017]

According to the present invention, a composition for colds and rhinitis having a dramatic effect on the elimination and alleviation of nasal congestion symptoms is obtained, which is useful as an effective cold medicine for early treatment of colds.

[0018]

The present invention will be described in more detail with reference to the following Examples and Test Examples. Example 1 The following components and amounts were weighed and uniformly mixed, and a tablet of 200 mg was obtained according to a conventional method. Loxoprofen sodium 90 g Noscapine 48 g Dihydrocodeine phosphate 24 g Ketotifen fumarate 4 g Ambroxol hydrochloride 45 g Phenylpropanolamine 60 g Theophylline 150 g Lysozyme chloride 90 g (titer) Anhydrous caffeine 75 g Vitamin B ₁ nitrate 8 g Vitamin B ₂ 4 g Vitamin B ₂ 4 g Magnesium stearate 16g Hardened castor oil 16g

Example 2 The following components and amounts were weighed and uniformly mixed, and a tablet of 200 mg was obtained according to a conventional method. Loxoprofen sodium 180 g Noscapine 48 g Dihydrocodeine phosphate 24 g Mequitadine 6 g Bromhexine hydrochloride 12 g Lysozyme chloride 90 g (titer) Lactose 710 g Microcrystalline cellulose 710 g Magnesium stearate 10 g Hardened castor oil 10 g

Example 3 After the following components and amounts were weighed and uniformly mixed, the resulting mixed powder was tableted by a direct compression method so that the weight of each tablet became 100 mg, to give tablets. Loxoprofen sodium 120 g Carbinoxamine maleate 7.5 g Dihydrocodeine phosphate 24 g Ambroxol hydrochloride 45 g Lysozyme chloride 90 g (titer) Lactose 55 g Low-substituted hydroxypropylcellulose 30.5 g Magnesium stearate 18 g Hardened castor oil 10 g

Example 4 An aqueous solution in which a pH adjuster (phosphate buffer) was dissolved (pH =
To 4.5), a preservative, a sweetener and a flavor were added and completely dissolved. After the sucrose fatty acid ester was uniformly dispersed in the solution, naproxen and other chemicals were added and dissolved, and purified water was added to make the total volume 1000 ml to obtain a liquid. Loxoprofensodium 120g phosphate dihydrocodeine 24g epinastine hydrochloride 20 g dl-methylephedrine hydrochloride ephedrine 60g ambroxol hydrochloride 45g of anhydrous caffeine 75g Vitamin B ₁ nitrate 8g vitamin B ₂ 4g sucrose fatty acid ester 15g Mannitol 15g stevia 10g ethyl benzoate 5g orange flavor 0.8g

Test Example 1 [Effect of Combination Formulation on Olfactory Intensity] << Test Method >> The effect on the olfactory intensity of each of the formulations shown in Table 1 was determined.

[0023]

[Table 1] 60 patients with nasal congestion (congestion of the nose) were assigned to one of the A to L groups.
Each group was divided into 5 groups of 5 persons. The test drugs of the formulations shown in Table 1 were administered to each subject three times a day for three days, and the improvement effects were compared. The determination was performed by measuring the olfactory intensity of the volatile fragrance using a paper soaked with a 20% menthol solution. The transition was determined up to 3 days later based on the olfactory intensity before administration.

The judgment criteria are: 4 points: strong, 2 points: felt, 1 point: slightly felt, 0 points: no feeling
Each group was compared with the average score.

The results are shown in Table 2.

[0026]

[Table 2] Regarding the degree of olfactory intensity, the combination prescription group of the groups A to E was superior to the control group of the groups F to L, which proved that the combination drug of the present invention had an excellent effect.

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Claims (7)

[Claims] 1. A composition for cold and rhinitis comprising the following (a) and (b): (A) loxoprofens (b) at least one selected from the group consisting of antiallergic drugs and antihistamines 2. The cold or cold according to claim 1, wherein the antiallergic drug or antihistamine is at least one selected from carbinoxamine, chlorpheniramine, ketotifen, mequitazine, epinastine, or salts thereof.
Rhinitis composition. 3. The cold according to claim 1, wherein the component (b) is carbinoxamine or a salt thereof, and the amount of the component (b) is 0.01 to 0.1 part by weight per 1 part by weight of the component (a). -A composition for rhinitis. 4. The component (b) is chlorpheniramine or a salt thereof, and the amount of the component (b) is 0.005 to 0.1 part by weight per 1 part by weight of the component (a).
The composition for cold and rhinitis according to the description. 5. The cold according to claim 1, wherein the component (b) is ketotifen or a salt thereof, and the amount of the component (b) is 0.005 to 0.05 part by weight per 1 part by weight of the component (a). -A composition for rhinitis. 6. The cold according to claim 1, wherein the component (b) is mequitazine or a salt thereof, and the compounding amount of the component (b) is 0.01 to 0.1 part by weight based on 1 part by weight of the component (a). -A composition for rhinitis. 7. The cold according to claim 1, wherein the component (b) is epinastine or a salt thereof, and the compounding amount of the component (b) is 0.05 to 0.5 part by weight based on 1 part by weight of the component (a). -A composition for rhinitis.