JP2001172175A - Composition for the cold - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for the cold highly effective for tussive syndromes out of various syndromes caused by the cold and the like. SOLUTION: This composition for the cold is blended with an expectorant and loxoprofen or its salt.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for colds having an enhanced effect on coughing among various symptoms caused by colds.

[0002]

2. Description of the Related Art The cold syndrome causes fever, pain, swelling of mucous membranes, etc., and causes serious obstacles to actual daily life and social and economic losses.

[0003] Eliminating or alleviating the symptoms of colds is an important therapeutic point. In particular, in the field of over-the-counter medicines (OTC), how to effectively eliminate various symptoms of colds, etc., has become a point of drug (cold composition) development.

[0004]

SUMMARY OF THE INVENTION It is an object of the present invention to provide a composition for colds in which cough symptoms are eliminated or reduced.

[0005]

Means for Solving the Problems As a result of repeated studies to achieve the above object, the present inventors have found that the addition of loxoprofen to expectorants has a dramatic effect on the elimination and reduction of cough symptoms. He found something and completed the invention.

[0006] That is, the present invention is a cold composition comprising an expectorant and loxoprofen or a salt thereof.

In the present invention, expectorants include cold syndrome,
For drugs with excessive viscous airway fluid secreted from the respiratory tract during asthma, etc., drugs that suppress sputum by acting to stop secretion, reduce viscosity, or promote airway ciliary movement, etc. For example, bromhexine, ambroxol, lycorine, saponin and the like can be mentioned.

[0008] The amount of loxoprofen or a salt thereof is preferably 15 to 225 mg, preferably 30 to 200 mg, and more preferably 30 to 200 mg, and bromhexine or a salt thereof per day for adults. The amount is preferably 3 to 30 mg, more preferably 6 to 24 mg, and the amount of ambroxol or a salt thereof is 15 to 75 m.
g is good, and preferably 22.5 to 50 mg.

An excellent compounding ratio in terms of eliminating and reducing cough symptoms is that loxoprofen or a salt thereof is preferably 1 to 1 part by weight of bromohexine or a salt thereof in an amount of 0.01 to 2 parts by weight per day for an adult. The amount is preferably 0.03 to 0.8 parts by weight, and the amount of ambroxol or a salt thereof is preferably 0.06 to 5 parts by weight, more preferably 0.12 to 1.7 parts by weight.

[0010] The cold composition of the present invention may contain a nonsteroidal anti-inflammatory drug, an anti-inflammatory enzyme drug, a bronchodilator,
A central nervous system stimulant, an antitussive, an antihistamine or an antiallergic, an anticholinergic, a vitamin, an antacid, a crude drug and the like may be added.

The composition for a cold of the present invention may be in the form of tablets, capsules, granules, fine granules, powders, chewables, foaming agents, drops, dissolving agents in the mouth, dry syrups, jellies, oral liquids. And so on.

These preparations can be prepared by a conventional method. In solid preparations, carriers used for preparation of the preparation include lactose, starch, sugar, mannitol, excipients such as 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, the carrier used for preparing the preparation includes surfactants such as sucrose fatty acid esters, polyoxyl stearate, polyoxyethylene polyoxypropylene glycols and polyoxyethylene mono fatty acid esters; There are thickeners such as synthetic aluminum silicate, magnesium silicate, magnesium carbonate, magnesium oxide and magnesium aluminate metasilicate, and organic acid and inorganic acid pH adjusters such as citrate buffer and phosphate buffer. In addition, if necessary, a solubilizer, a buffer, a preservative, a flavor, a pigment, a sweetener, and the like can be used.

[0014]

According to the present invention, the effect on the cough reaction is remarkably improved, and as a result, a drug which is extremely useful for the cold syndrome can be provided.

[0015]

The present invention will be described in more detail with reference to the following examples and test examples, but the present invention is not limited to the following examples.

Example 1 The following components were weighed and uniformly mixed, and the resulting mixed powder was tableted by a direct compression method to a tablet weight of 100 mg to obtain tablets. Loxoprofen sodium 150 g Carbinoxamine maleate 7.5 g Dihydrocodeine phosphate 24 g Ambroxol hydrochloride 45 g Lysozyme chloride 90 g (titer) Lactose 35 g Low-substituted hydroxypropylcellulose 25.5 g Magnesium stearate 15 g Hardened castor oil 8 g.

Example 2 The following components were weighed and uniformly mixed, and a tablet of 200 mg was obtained according to Example 1. Loxoprofen sodium 180 g noscapine 48 g dihydrocodeine phosphate 24 g bromhexine hydrochloride 12 g lysozyme chloride 90 g (titer) lactose 720 g microcrystalline cellulose 700 g magnesium stearate 13 g hardened castor oil 13 g.

Example 3 The following components were weighed and uniformly mixed, and a tablet of 200 mg was obtained according to Example 1. Loxoprofen sodium 150 g Noscapine 48 g Dihydrocodeine phosphate 24 g Ketotifen fumarate 2 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 Milk sugar Magnesium stearate 22 g Hardened castor oil 22 g.

Example 4 A preservative, a sweetener, and a flavor are added to an aqueous solution in which a pH adjuster (phosphate buffer, pH 4.5) is dissolved, and the solution is completely dissolved. The sucrose fatty acid ester is uniformly dispersed in the solution. Thereafter, naproxen and other drugs were added and dissolved, and purified water was added to make the total amount to 1000 ml. Loxoprofen sodium 100 g dihydrocodeine phosphate 24 g epinastine hydrochloride 20 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 sweetener suitable amount preservative suitable amount .

Test Example [Effects of Combination Formulation on Cough Symptoms] Using a Hartley guinea pig weighing 300 to 400 g, feed and drinking water were freely taken under an environment of room temperature 24 ± 1 ° C., and preliminarily reared and subjected to experiments. . Anesthetized guinea pigs were placed in a body plethysmograph. The body plethysmograph consists of two transparent acrylic cylindrical boxes (about 1.2 L) of the head and body, and an acrylic n covered with two upper and lower rubber films.
It consists of an eck restrainer. K
ohlogi et al. (J. Clin. Invest.
82, 2063-2068 (1988)), capsaicin is sprayed from the top of the entire surface of the container with an ultrasonic nebulizer (TUR-3200, Nippon Koden) for 2 minutes (2.2 mL / min), the presence or absence of coughing, cough reflex The strength and frequency were examined. The coughing sound was confirmed with a microphone, and the change in the internal pressure of the sealed body box was measured by fl.
Recording was performed on a pen recorder via an ow meter (MEP-1100, Nihon Kohden). The evaluation was made based on the presence or absence of suppression of the number of 1-minute cough reactions that occurred. The room temperature was set at 25 ° C.

As a comparative drug, one prepared by dissolving the formulation shown in Table 1 in 50 mL of purified water was used. Each group consisted of 5 animals, and each group was treated with drug 3 30 minutes before exposure to capsaicin.
mL was administered orally. (Control group is 3m of purified water
L was given. )

[0022]

[Table 1] Table 2 shows the results. Groups A and B are superior in the degree of suppression of coughing reaction by Hartley guinea pigs, and it has been proved that drugs in these groups have excellent effects.

[0023]

[Table 2] Test results [Number of cough symptoms and suppression rate for control group]

Claims (2)

[Claims] 1. A cold composition comprising an expectorant and loxoprofen or a salt thereof. 2. The composition according to claim 1, wherein the expectorant is bromhexine or a salt thereof, or ambroxol or a salt thereof.