JPH09110677A - Aerosol preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an aerosol preparation having excellent antipruritic effect to immediate reaction of pruritus by getting stung by an insect and also having excellent antipruritic effect to delayed reaction of pruritus. SOLUTION: This aerosol preparation is composed of a raw solution and a propellant obtained by blending a mixed solvent of water and a lower alcohol with following components (A)-(C): (A) one kind or more than two kinds of surfactant selected from the group comprising of polyoxyethylene fatty sorbitates and fatty sorbitates; (B) 0.5-8wt.% menthol and (C) 1-0.5 pt.wt. of camphor based on 1 pt.wt. of menthol.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an aerosol agent having an excellent antipruritic effect against pruritus caused by insect bites and athlete's foot.

[0002]

2. Description of the Related Art Skin reactions caused by insect bites include itching and redness, and there are an immediate reaction several minutes to one hour after the bite and a delayed reaction after ten and several hours to one day. Among them, the itching of delayed reaction can be suppressed by applying a drug such as a general ointment containing a local anesthetic or an antipruritic. On the other hand, itching of the immediate reaction could not be sufficiently suppressed not only by applying the above-mentioned chemicals but also by cooling by evaporation of the stock solution components such as ethanol or simply by spraying a propellant.

[0003]

SUMMARY OF THE INVENTION An object of the present invention is to provide a preparation having an excellent antipruritic effect against itching of immediate reaction caused by insect bites and pruritus of athlete's foot.

[0004]

As a result of intensive studies, the inventors of the present invention found that an aerosol formulation containing menthol and camphor at a certain ratio in a specific surfactant can solve the above-mentioned problems. The present invention has been completed. That is, the present invention is an aerosol agent comprising a stock solution and a propellant in which the following components (A) to (C) are mixed in a mixed solvent of water and a lower alcohol. (A) one or more surfactants selected from the group consisting of polyoxyethylene sorbitan fatty acid esters and sorbitan fatty acid esters (B) menthol 0.5 to 8 wt% (C) to 1 part by weight of menthol 1 to 0.5 parts by weight camphor.

The surfactant used in the present invention, which is selected from the group consisting of polyoxyethylene sorbitan fatty acid esters and sorbitan fatty acid esters, is a paste or a semisolid at room temperature when preparing a stock solution. Oxyethylene (6) sorbitan monostearate alone or polyoxyethylene (20)
Sorbitan monostearate, polyoxyethylene (2
0) Mixtures of sorbitan tristearate and sorbitan monostearate are preferred. The blending amount of these is 0.
5 to 8% by weight, preferably 0.5 to 4% by weight.

Further, the solvent is a mixture of water and a lower alcohol, and the weight ratio thereof is preferably in the range of 30:70 to 70:30. A liquefied gas is used as the propellant, and dimethyl ether, n-butane, isobutane, propane or a mixture thereof can be used as the liquefied gas. Among these, a propellant containing 80% by weight or more of dimethyl ether is preferable. The compounding amount of the propellant is 40 to 80% by weight, preferably 50 to 70% by weight, based on the whole preparation.

In the aerosol composition of the present invention, the components usually contained in antipruritic agents and antifungal agents, for example, antipruritic agents (crotamiton, ictamol, moctamol, thymolic acid, etc.), antifungal agents (tornaftate, miconazole nitrate, etc.) ), Antihistamines (diphenhydramine, diphenhydramine hydrochloride, isothipendyl hydrochloride, chlorpheniramine maleate, etc.), local anesthetics (lidocaine, dibucaine hydrochloride, etc.), bactericides (potassium iodide, chlorhexidine gluconate, acrinol chloride, benzalkonium chloride) Etc.), anti-inflammatory agents (allantoin, glycyrrhetinic acid, methyl salicylate, etc.), antioxidants (dibutylhydroxytoluene, etc.), solubilizers (diisopropyl adipate, isopropyl myristate, lactic acid, sodium hydroxide, etc.), fragrances, etc. Effect of invention It can be added in amounts not detrimental to the.

The aerosol of the present invention is prepared by heating, mixing, stirring and dissolving or uniformly dispersing components other than the propellant to prepare a liquid, and then filling the liquid with the propellant in an aerosol container. It can be manufactured.

[0009]

EFFECTS OF THE INVENTION By using the aerosol composition having the above composition, the stock solution becomes sherbet-like at the time of spraying the aerosol, and the cooling effect more than that obtained by simply spraying alcohol or propellant can be obtained, and further menthol and camphor can be specified. A specific antipruritic effect can be obtained by mixing in a ratio. Therefore, according to the present invention, it is possible to provide an aerosol agent which can immediately and continuously relieve the itch of immediate reaction due to insect bites and the itch of athlete's foot.

[0010]

EXAMPLES The present invention will be described in more detail below with reference to examples and test examples. Example 1 stock Ingredients Amounts (g) Lidocaine 0.6 Diphenhydramine 0.3 Menthol 0.6 Camphor 0.6 Nikkol TS-10 [polyoxyethylene (20) Soruhi Keypad tradename monostearate] 0.9 Nikkor TS -30 [Product name of polyoxyethylene (20) sorbitan tristearate] 0.6 Nikkor SS-10 [Product name of sorbitan monostearate] 0.9 Ethyl alcohol 10.5 Purified water Total 30 ml Propellant dimethyl ether 70 ml Undiluted solution Each component of (1) was heated, mixed and stirred to make it uniform, and a stock solution was prepared, and then this stock solution was filled in an aerosol container together with a propellant to produce an aerosol agent.

Examples 2 and 3 and Comparative Examples 1 to 3 Using the formulations shown in Table 1, an aerosol agent was produced in the same manner as in Example 1. Comparative Example 4 A stock solution was prepared using the formulation shown in Table 1 and used as it was as a liquid agent.

[0012]

[Table 1]

Test Example (Test Method) Wear rubber gloves with a 5 mm diameter hole on the back of the hand,
Insert your hand into the gauge containing Aedes albopictus. Make one mosquito suck blood. When you have sufficiently sucked blood, remove your hands and remove the rubber gloves. If the degree of itching becomes unbearable, the sample (Examples 2 and 3)
And an appropriate amount of the aerosol agent produced in Comparative Examples 1 to 3 (3
Apply from a distance of 1 to 3 seconds). Further, the liquid agent produced in Comparative Example 4 is applied in an appropriate amount. Immediately after application, the degree of itching is self-determined every minute (see Table 2). The control is 0 minutes when the degree of itchiness becomes intolerable, and no treatment is performed.

[0014]

[Table 2]

(Results) The results are shown in FIGS. 1 and 2 as an average value of five subjects. It was found that with the aerosol preparations of the present invention prepared in Examples 2 and 3, the pruritus score peak was 1 or less, that is, there was almost no pruritus, and an effective pruritus-suppressing effect for consumers was obtained.

[Brief description of the drawings]

FIG. 1 is a diagram showing the antipruritic effect of the aerosol of the present invention and the liquid preparation of Comparative Example 4, in which the vertical axis represents the itch score and the horizontal axis represents the time (minutes).

FIG. 2 is a graph showing the antipruritic effect of an aerosol agent compared with the aerosol agent of the present invention, in which the vertical axis represents the pruritus score and the horizontal axis represents time (minutes).

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification number Reference number within the agency FI technical display location // (A61K 31/045 31: 125) (72) Inventor Fumiki Kimura 3 Takada, Toshima-ku, Tokyo No. 24-1 Taisho Pharmaceutical Co., Ltd. (72) Inventor Keiko Kato 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd.

Claims (3)

[Claims] 1. An aerosol agent comprising a stock solution and a propellant in which the following components (A) to (C) are mixed in a mixed solvent of water and a lower alcohol. (A) one or more surfactants selected from the group consisting of polyoxyethylene sorbitan fatty acid esters and sorbitan fatty acid esters (B) menthol 0.5 to 8 wt% (C) to 1 part by weight of menthol 1 to 0.5 parts by weight camphor 2. The aerosol composition according to claim 1, wherein the propellant has a dimethyl ether content of 80% by weight or more. 3. The compounding amount of the propellant is 50 to 70 of the whole preparation.
The aerosol composition according to claim 1 or 2, which is contained in a weight percentage.