JP2002241310A - Locally applying composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a locally applying composition good in feeling when applied, without unpleasant feeling including the irritant feeling of a locally applying agent formulated with an anti-influenza virus ingredient. SOLUTION: This locally applying composition is characterized by being obtained by formulating an anti-influenza virus ingredient having unpleasant feeling when applied locally and a volatile essential oil ingredient; wherein, particularly, the anti-influenza virus ingredient is one kind selected from zanamivir and salts thereof, and the volatile essential oil ingredient is selected from menthol, camphor, peppermint oil and eucalyptus oil. The above composition is in the form of inhalation such as a nasal drop, being a means for treating or preventing cold symptoms.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to providing a composition for topical application which is excellent in use feeling against unpleasant sensation or unpleasant sensation of an agent for topical application of an anti-influenza virus drug. Specifically, a topically applied composition comprising a menthol, camphor, peppermint oil, eucalyptus oil, or one or more volatile essential oil components blended with an anti-influenza virus component and having a significantly improved feeling in use. is there.

[0002]

2. Description of the Related Art Influenza is a viral infectious disease mainly involving respiratory mucosal cells. Influenza virus is an RNA virus.
It is known that the epidemic remarkably prevails in winter in conjunction with the decrease of the immune activity on the living body side in the cold season, and this is why it is also called epidemic cold. There are two glycoprotein spikes, hemagglutinin and neuraminidase, on the surface of the influenza virus, and these spikes are greatly involved in invading and multiplying target cells. Zanamivir, an anti-influenza virus drug, is a nasal inhalation form drug that inhibits the activity of neuraminidase, thereby blocking the progress of a series of viral multiplication processes, and is known to infect humans. It has the feature of acting non-selectively on both type B and type B. Since influenza virus mainly infects the living body through the nasal cavity, this agent used particularly for nasal inhalation is a very rational agent not only in function but also in form of use. In other words, this anti-influenza virus drug is significant in having a direct effect on the infection and propagation of the virus that is the root cause of the onset.

[0003] On the other hand, when the influenza is infected, the virus damages the respiratory mucosa when the virus infects and proliferates the cells of the mucosa of the respiratory mucosa and presents an inflammatory state of the mucous membrane. Nevertheless, because of its chemical composition, it presents unpleasant sensations such as irritating sensations, which hinders the use of the drug, and even if it is a highly useful drug with enhanced efficacy, there is a problem in use. Unless compliance is maintained or improved, the purpose of causal therapy cannot be achieved.

[0004] Volatile essential oil components such as menthol, camphor, peppermint oil and eucalyptus oil are widely used widely in general foods and quasi-drugs. However, the mechanism related to nerve information transmission represented by feeling of use has not yet been elucidated so far.

[0005]

SUMMARY OF THE INVENTION An object of the present invention is to provide a composition for topical application in which the feeling of use of an anti-influenza virus component having an unpleasant feeling such as irritation is improved.

[0006]

Means for Solving the Problems The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, menthol,
It has been found that volatile essential oil components such as camphor, peppermint oil, and eucalyptus oil inhibit or significantly reduce the transmission of unpleasant sensations of anti-influenza virus components, and significantly improve the feeling of use of various drugs. The present invention has been completed. That is, the present invention is a topically applied composition characterized by blending an influenza virus component having an unpleasant feeling of use when applied topically and a volatile essential oil component.

The anti-influenza virus component according to the present invention is, for example, zanamivir or a salt thereof, and examples of the salt include a hydrochloride, a sulfate, a nitrate, a citrate, a maleate and a fumarate. The volatile essential oil components include menthol, camphor, peppermint oil, eucalyptus oil and the like, and it is preferable to mix one or more of them.

[0008] The composition for topical application of the present invention may further comprise, if necessary, an antiallergic drug, an antihistamine drug, an anti-inflammatory enzyme, a bronchodilator, a sympathomimetic drug, an anticholinergic drug, a vitamin drug. Components such as a disinfectant, an astringent, a local anesthetic, a herbal medicine, a fragrance, and the like can be appropriately blended. In addition, these components can be used alone or mixed with each other. The composition for topical application of the present invention can be used in a form of inhalation such as nasal drops, and can be used in a wide range of quasi-drugs and sundries as needed.

The topical composition of the present invention, when zanamivir or a salt thereof is used as an active ingredient, is used in an amount of 5 to 30 mg, preferably 10 to 20 mg per day for an adult. This is a concentration of 1 to 20% by weight based on the whole preparation.
And preferably 5 to 10% by weight. Menthol, camphor, peppermint oil and eucalyptus oil, which are volatile essential oil components, each have a concentration of 0.0 with respect to the whole preparation.
0.01 to 1.0% by weight, preferably 0.01 to 0.7% by weight.
5% by weight.

The mixing ratio of the anti-influenza virus component to the volatile essential oil component is such that the volatile essential oil component is 0.0005 to 1 part by weight, preferably 0.001 to 0.001 part by weight, per 1 part by weight of the anti-influenza virus component. 15 parts by weight. The compounding concentration can be appropriately increased or decreased depending on the use subject such as age, weight, and medical condition.

The topical composition of the present invention can be prepared by a conventional method. If necessary, a surfactant, a solubilizing agent, a buffer, a preservative, an osmotic pressure regulator and the like can be used. In addition, other fragrances, coloring agents, other refreshing agents and the like can be used.

[0012]

EFFECTS OF THE INVENTION As constituents, zanamivir or one of its salts and menthol, camphor, peppermint oil,
By blending one of the eucalyptus oils, for the purpose of inhibiting or significantly reducing various unpleasant sensations against unpleasant irritations caused when using the anti-influenza virus drug topical application agent, A topical composition has been obtained which can be provided in inhalation form.

[0013]

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

Example 1 After weighing out the components and the amounts of the following components except for sodium chloride and mixing them homogeneously, they were dissolved in 80 mL of sterile purified water together with a phosphate (100 mg) buffer solution. After adjusting the pH to 6.8 by adding an appropriate amount of sodium hydroxide and an appropriate amount of sodium hydroxide, sterilized purified water was added to dissolve the solution to a total volume of 1 L. The lysate was divided into 100 mL containers to make nasal drops. Zanamivir 50,000mg Mint oil 100mg Sodium chloride 9000mg Methyl parahydroxybenzoate 50mg

Example 2 The following components except for sodium chloride and their amounts were weighed and uniformly mixed, and then a phosphate (100 mg) buffer solution,
Dissolve in 80 mL of purified water together with 10 mg of sodium edetate (preservative), and further add sodium chloride (isotonizing agent)
900 mg, an appropriate amount of sodium hydroxide was added to adjust the pH to 7.0.
Then, purified water was added and dissolved to make the total volume 1 L. The lysate was divided into 100 mL containers to make nasal drops. Zanamivir 100000mg l-menthol 5000mg Sodium chloride 9000mg Glycerin 20,000mg Polyoxyethylene hydrogenated castor oil 2000mg Methyl paraoxybenzoate 50mg

Example 3 According to Example 2, it was dissolved in purified water to give a nasal drop. Zanamivir 50,000mg dl-Camphor 5000mg Tetrahydrozoline hydrochloride 1000mg Benzethonium chloride 200mg Lidocaine 3000mg Dipotassium glycyrrhizinate 1500mg Sodium chloride 9000mg Glycerin 20,000mg Polyoxyethylene hydrogenated castor oil 2000mg

Example 4 The following components except for benzalkonium chloride and the amounts thereof were weighed and uniformly mixed, and then dissolved together with 10 mg of benzalkonium chloride (preservative) in 80 mL of purified water.
After re-mixing uniformly, purified water was added and dissolved to bring the total volume to 1 L. The solution was divided into 100 mL containers to prepare nasal sprays. Zanamivir 100000mg Eucalyptus oil 100mg Suplatast tosilate 5000mg Propylene glycol 25000mg Glycerin 25000mg Benzalkonium chloride 100mg Polyoxyethylene hydrogenated castor oil 2000mg Saccharin sodium 500mg

Test Example 1 Investigation on Improving the Usability The composition of Example 2 was applied to 10 users (5 men and 5 women) in a nasal spray container having a spray amount of about 50 μL per application to 10 panelists (5 men and 5 women). An in-use feeling test was conducted. As a comparative composition, one containing various concentrations of l-menthol,
The test was carried out in the same container. The feeling of use was evaluated on a scale of 10 points per person (a total of 100 points), and the total points of the evaluations of all panelists were obtained. As a guide for the distribution of points, 10 points: no problem in usability at all, 7 points: less discomfort and good usability, 5 points: slight irritation, but no major problem in usability 2 Points: There was discomfort and the usability was not good, and the 0 point usability was bad and unacceptable. In this range, an intermediate score (however, an integer of 0 to 10) was evaluated. The results are shown in FIG. As a result, the l-menthol concentration of 0.1 to 1.0% by weight was particularly high.

[0019]

[Brief description of the drawings]

FIG. 1 is a graph showing the degree of improvement in the usability of a test example.

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 47/44 A61K 47/44 A61P 31/16 A61P 31/16 (72) Inventor Joji Nakagami Tokyo 3-24-1, Takada, Toshima-ku Taisho Pharmaceutical Co., Ltd. (72) Inventor Katsuyoshi Aikawa 3-24-1, Takada, Toshima-ku, Tokyo Taisho Seiyaku Co., Ltd. F-term (reference) 4C076 AA11 AA24 AA93 BB21 BB25 CC35 DD37 DD40 EE53 FF68 4C084 AA17 AA27 BA44 CA59 MA13 MA59 NA10 ZB331 ZB332 ZC801 ZC802 4C086 AA01 AA02 BA07 GA17 MA05 MA08 MA13 MA59 NA10 ZB33 ZC80

Claims (6)

[Claims] 1. A topically applied composition comprising an anti-influenza virus component and a volatile essential oil component having an unpleasant feeling of use when applied topically. 2. The composition for topical application according to claim 1, wherein the anti-influenza virus component is any one selected from zanamivir or a salt thereof. 3. The topical composition according to claim 1, wherein the volatile essential oil component is one or more selected from the group selected from menthol, camphor, peppermint oil, and eucalyptus oil. 4. The composition for topical application according to claim 1, wherein the dosage form is an inhalation form. 5. The composition for topical application according to claim 4, which is in the form of nasal drops. 6. A method for treating or preventing cold symptoms using the composition for topical application according to any one of claims 1 to 5.