JP2002316927A - Composition for common cold - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for common cold effective against tussal symptoms due to common cold symptoms. SOLUTION: This composition for the common cold is characterized as comprising (a) one or more kinds selected from the group consisting of naproxen, ketoprofen, loxoprofen, isopropylantipyrin, ibuprofen, acetaminophen and salts thereof and (b) pseudoephedrine.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a composition for colds. More specifically, the present invention relates to a composition for colds with an improved antitussive effect against cough symptoms caused by cold syndrome.

[0002]

2. Description of the Related Art In general, the cold syndrome is mostly caused by a virus, and is a respiratory tract infection which is cured in about 3 to 7 days with various systemic or local symptoms. At present, the fact is that the causative viruses are susceptible to mutation, and the development of antiviral agents against these viruses has not been able to keep up and resort to symptomatic treatment. In particular, coughing symptoms mainly appear in the late to late stages of the cold illness, and the load on the chest muscles and the like cause a great loss of physical strength, and prolonged prolongation of the cold symptoms.
Therefore, how to reduce or eliminate cough symptoms is one of the therapeutic points.

[0003] In recent years, the relationship between the cold syndrome and allergic predisposition has been attracting attention, and suppression of the frequency of occurrence of airway irritable coughing has also become a new therapeutic issue.

Under these circumstances, as a cough medicine for colds corresponding to the cough symptom of the cold syndrome, narcotic drugs such as codeines and drugs mainly having a central respiratory depressant action are commonly used. Although the efficacy of these drugs has been demonstrated, the addictive nature of the narcotic component includes drowsiness and hallucinations. It has also been confirmed that there are serious side effects such as urine. Thus, its usage and dosage are strictly limited. This has been widely used by consumers and has acted as a factor inhibiting use of the drug in the field of over-the-counter drugs for the purpose of self-medication.

[0005]

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide a composition for colds which has no side effects and which is effective for cough symptoms caused by cold syndrome.

[0006]

Means for Solving the Problems Accordingly, the present inventors have:
We were investigating the effects of reducing and eliminating cough symptoms with non-steroidal anti-inflammatory drugs such as naproxen and ketoprofen.By combining these non-steroidal anti-inflammatory drugs with sympathomimetics, the antitussive effect was enhanced. ,And,
The inventors have found that the side effects are also within an acceptable range, and have completed the present invention. That is, the present invention comprises (a) one or more selected from the group consisting of naproxen, ketoprofen, loxoprofen, isopropylantipyrine, ibuprofen, acetaminophen and salts thereof, and (b) pseudoephedrine. This is a characteristic composition for colds.

The component (a) of the present invention, naproxen,
Ketoprofen, loxoprofen, isopropylantipyrine, ibuprofen, and acetaminophen are one type of nonsteroidal anti-inflammatory drugs, and these may be salts or hydrates. In addition to using one kind,
Two or more kinds may be used in combination.

[0008] Pseudoephedrine, which is the component (b) of the present invention, is a kind of sympathomimetics and may be a salt or a hydrate. The following is an example of the daily amount of the component (a) for an adult. In naproxen, it is usually 100 to 750 mg, preferably 1 to 500 mg.
50-600 mg. Usually 50 for ketoprofen
３００300 mg, preferably 75-200 mg. For loxoprofen, the amount is 15 to 200 mg, preferably 60 to 180 mg. In the case of isopropylantipyrine, the amount is usually 50 to 450 mg, preferably 7 to 450 mg.
5 to 300 mg. For ibuprofen 50 ~
It is 1200 mg, preferably 100-600 mg. 150 ~ 1500m for acetaminophen
g, preferably 300 to 900 mg.

The amount of the pseudoephedrine as the component (b) is usually 0.05 parts by mass or more, preferably 0.25 to 15 parts by mass, per 1 part by mass of the component (a).

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION The anti-cold composition of the present invention comprises (a)
It can be prepared by blending a fixed amount of the component (b) with the components. In addition, various drugs can be appropriately compounded as needed to make the drug applicable to cold symptoms other than cough symptoms.

The composition for colds of the present invention may further comprise tablets, granules, fine granules, powders, capsules, chewables, foaming agents, drops, instant dissolving agents in mouth, dry syrups,
Various preparations such as an oral solution, an inhalant, and a stream, and a dosage form can be appropriately selected.

These preparations can be prepared by a conventional method. Carriers used in the preparation of formulations include lactose,
Excipients such as starch, sugar, mannitol, crystalline cellulose, binders such as hydroxypropylcellulose, hydroxypropylmethylcellulose, gelatin, PVP, disintegrants such as carboxymethylcellulose calcium, low-substituted hydroxypropylcellulose, magnesium stearate, hardening Lubricants such as castor oil and talc can be used. In addition, if necessary, solubilizers, buffers, preservatives, flavors, dyes, flavoring agents, and the like can be used.

[0013] Carriers used for the preparation of a preparation in a liquid preparation for internal use include 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, sweeteners and the like can be used.

[0014]

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

Example 1 After weighing and thoroughly mixing the following components, the mixed powder was tableted with a tableting machine (Collect 19, manufactured by Kikusui Seisakusho) to produce a tablet weighing 200 mg per tablet. did. Naproxen 450 g Dihydrocodeine phosphate 24 g dl-Chlorpheniramine maleate 12 g Pseudoephedrine hydrochloride 240 g Lactose 250 g Microcrystalline cellulose 182 g Magnesium stearate 12 g

Example 2 The following components were weighed and thoroughly mixed, and then a tablet weighing 200 mg per tablet was produced in accordance with Example 1. Ketoprofen 100 g d-Chlorpheniramine maleate 6 g dextromethorphan 24 g pseudoephedrine hydrochloride 160 g guaifenesin 200 g lactose 340 g microcrystalline cellulose 300 g magnesium stearate 15 g hardened castor oil 15 g

Example 3 The following components were weighed and thoroughly mixed, and a tablet weighing 230 mg was produced according to Example 1. Loxoprofen sodium 90 g d-Chlorpheniramine maleate 6 g pseudoephedrine hydrochloride 200 g theophylline 450 g guaifenesin 200 g lactose 400 g microcrystalline cellulose 375 g magnesium stearate 20 g hardened castor oil 19 g

Example 4 The following components were weighed and mixed well, and then a tablet having a tablet weight of 250 mg was produced according to Example 1. Isopropylantipyrine 150 g Carbinoxamine maleate 12 g Noscapine 48 g Potassium guaiacol sulfonate 125 g Pseudoephedrine hydrochloride 240 g Proxyfilin 210 g Anhydrous caffeine 75 g Lactose 300 g Microcrystalline cellulose 290 g Magnesium stearate 20 g Hardened castor oil 17 g

Example 5 The following components were weighed and mixed well, and then a tablet weighing 250 mg per tablet was produced in accordance with Example 1. Ibuprofen 450g maleic carbinoxamine 12g citric tipepidine 45g guaiacol sulfonic acid potassium 125g pseudoephedrine hydrochloride 120g proxy Villingen 210g anhydrous caffeine 75g Vitamin _{B 1} nitrate 8g Lactose 300g Microcrystalline cellulose 290g Magnesium stearate 20g hardened castor oil 17g

(Test Example) [Effect of Combination Preparation on Cough Symptoms] Hartley guinea pigs weighing 300 to 400 g were used.
The animals were allowed to freely ingest feed and drinking water in an environment at room temperature of 24 ± 1 ° C., and were subjected to preliminary breeding before the experiment.

[0021] Non-anesthesia guinea pigs are treated with body plethysmogra
ph. The body plethysmograph is a transparent acrylic cylindrical box (about 1.2L) for the head and body
And acrylic neck restra covered with two rubber films
It consists of iner.

The method of Kohrogi et al. (J. Clin. Invest. 82,2063)
According to -2068), capsaicin was sprayed from the top of the container with an ultrasonic nebulizer (TUR-3200, Nihon Kohden) for 2 minutes (2.2 mL / min), and the presence or absence of cough, cough reflex strength and frequency were examined. Was. While checking the coughing sound with a microphone, the change in the internal pressure of the closed body box
Recording was performed on a pen recorder via a flow 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 is 2
Set to 5 ° C.

As a comparison drug, a formulation shown in Table 1 dissolved in 50 mL of purified water was used. Each group consisted of 5 mice, and each group was orally administered 3 mL of the drug 30 minutes before spraying capsaicin. The control group had 3 m of purified water.
L was given. Table 2 shows the results.

[0024]

[Table 1] List of prescriptions for test drugs (unit: mg in 50 mL)

[0025]

[Table 2] [Number of cough symptoms and suppression rate for control group (H group)]

The degree of the inhibitory effect of the Hartley guinea pig on the coughing reaction was superior in the groups A to C, and it was confirmed that the drugs in these groups had excellent effects.

[0027]

Industrial Applicability According to the present invention, it has become possible to provide a common cold medicine effective for cough symptoms caused by cold syndrome.

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61P 11/14 A61P 11/14 (72) Inventor Joji Nakagami 3- 24-1, Takada, Toshima-ku, Tokyo No. Taisho Pharmaceutical Co., Ltd. (72) Katsuyoshi Aikawa, Inventor 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. (72) Inventor Yasushi Nakagawa 3-24-1, Takada, Toshima-ku, Tokyo F term (reference) 4C086 AA01 AA02 BC36 MA02 MA03 MA04 MA09 MA10 NA05 ZA59 ZA62 ZC75 4C206 AA01 AA02 DA22 DA23 DA24 DA25 FA10 GA02 GA31 KA01 KA03 MA02 MA03 MA04 NA05 ZA59 ZA62 ZC75

Claims (1)

[Claims] (A) naproxen, ketoprofen,
A composition for colds comprising one or more members selected from the group consisting of loxoprofen, isopropylantipyrine, ibuprofen, acetaminophen and salts thereof, and (b) pseudoephedrine.