JPH11279061A - Antipruritic solution - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an antipruritic solution which gives excellent refreshing feeling and decreased irritation to skin by blending a specific antipruritic component with a preparation containing a high concentration of menthol to prepare the solution. SOLUTION: This solution comprises (A) menthol of 3 w/v% or more based on the whole preparation, (B) chloropheniramine or its salt (preferably chlorpheniramine meleate) and (C) water of 20-45 w/v% based on the whole preparation. Further, the component B is preferably blended in an amount of 0.01-2 w/v% based on the whole preparation in terms of the amount of chlorpheniramine. For example, the solution is obtained by dissolving 0.3 g of chlorpheniramine meleate and 3.5 g of d,1-menthol into about 40 ml of ethanol, adding 40 g of purified water and adjusting the total volume to 100 ml by adding ethanol. By this process, the antipruritic solution which gives improved refreshing feeling and causes no stimulation can be provided and the use as a medicine or the like is expectable.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an antipruritic solution, and more particularly, to an antipruritic solution having improved refreshing feeling and reduced skin irritation.

[0002]

2. Description of the Related Art Conventionally, various external preparations have been marketed as an antipruritic for insect bites and the like. Usually, antihistamines such as diphenhydramine and isothibenzyl hydrochloride are compounded as antipruritic components. The dosage form of these preparations is generally a liquid preparation or a gel preparation, but the gel preparation has a sticky feeling after application, and the liquid preparation is more preferable in terms of usability. In addition, since such preparations are often used in the summer, it is necessary to increase the refreshing sensation at the time of use in order to improve the feeling of use and improve the product properties.

[0003] Generally, menthol, camphor, methyl salicylate and the like are known as cooling agents used for external preparations. These cooling agents are significantly involved in the refreshing sensation that persists after several minutes of application.

[0004]

DISCLOSURE OF THE INVENTION The present inventors have studied various refreshing agents to improve the refreshing feeling of an antipruritic solution. Undesirably, it was found that increasing the amount of methyl salicylate causes a reduction in product properties due to a specific odor. Therefore, menthol is most preferred as a cooling agent used for improving the refreshing feeling.

Conventionally, even if the amount of menthol to be added to obtain a refreshing feeling is small, the refreshing feeling has been supplemented by further adding another cooling agent. However, the feeling of use as the whole preparation may be impaired due to the irritating feeling and burning sensation.

On the other hand, it has been found that in the case of a liquid preparation, if the amount of menthol is increased in order to improve the refreshing feeling, skin irritation may occur when applied.

An object of the present invention is to provide an antipruritic solution which improves the refreshing sensation and reduces skin irritation.

[0008]

As a result of various studies, the present inventors have found that, when a liquid preparation is prepared by adding chlorpheniramine as an antipruritic component to a preparation containing a high concentration of menthol, a refreshing feeling and a low refreshing feeling can be obtained. The present invention was found to be a stimulant antipruritic solution and completed the present invention.

That is, the present invention relates to A) 3 W / V% of the whole preparation
An antipruritic solution comprising the above menthol, B) chlorpheniramine or a salt thereof, and (C) water of 20 to 45 W / V% of the whole preparation.

[0010]

DESCRIPTION OF THE PREFERRED EMBODIMENTS In the present invention, menthol is dl
-Menthol or l-menthol. In the present invention, the amount of menthol must be 3 W / V% or more of the whole preparation. If the amount is less than 3 W / V%, the refreshing feeling is not sufficient.

In the present invention, the salt of chlorpheniramine is a salt with a pharmaceutically acceptable acid, most preferably chlorpheniramine maleate.

The amount of chlorpheniramine or a salt thereof in the present invention is preferably 0.01 to 2 W / V% of the whole preparation in terms of the amount of chlorpheniramine.

The liquid preparation of the present invention must be in a liquid form at the time of application, for example, a liquid preparation, a lotion preparation, an emulsion preparation, an aerosol preparation and the like. Jelly-like dosage forms such as gels and ointments
This is because it is not preferable in terms of usability such as stickiness after coating.

In the liquid preparation of the present invention, it is necessary to mix water in the preparation from the viewpoint of refreshing feeling. The amount of water at that time is 20-
45 W / V% is preferred. If the content is less than 20 W / V%, a refreshing feeling cannot be sufficiently obtained, and if the content is more than 45 W / V%, the solubility of the blended components is reduced, so that it becomes difficult to produce a preparation.

The liquid preparation of the present invention can be produced by a usual production method by blending components generally used in the liquid preparation.

[0016]

EFFECT OF THE INVENTION The present invention makes it possible to obtain an antipruritic solution which improves the refreshing sensation and does not cause irritation.
It can be used for medicines and the like.

[0017]

The present invention will be described in more detail with reference to the following Examples and Test Examples.

Embodiment 1

[0019]

Table 1 Chlorpheniramine maleate 0.3 g dl-menthol 3.5 g Purified water 40 g ethanol Total 100 ml Chlorpheniramine maleate and dl-menthol were dissolved in about 40 ml of ethanol. Purified water was added, and the total volume was adjusted to 100 ml with ethanol to obtain a liquid preparation.

Comparative Example 1 A liquid formulation for comparison was obtained in the same manner as in Example 1 except that chlorpheniramine maleate of Example 1 was changed to 2 g of diphenhydramine hydrochloride (an antipruritic effect similar to that of Example 1).

Test Example 1 The liquid preparations obtained in Example 1 and Comparative Example 1
z method ("New skin physiology and safety", Seiji Shoin, 176
P.) Was evaluated for primary skin irritation. Japanese white rabbits were used as test animals, and the test was performed with three of each liquid. The primary irritability index (PII) was determined for each test animal, and the average of the three animals was used as the PII value of each solution.

As a result, the liquid preparation of Example 1 was 0.5, and the liquid preparation of Comparative Example 1 was 3.0.

Claims (2)

[Claims] 1. An antipruritic liquid comprising: A) menthol of 3 W / V% or more of the whole preparation; B) chlorpheniramine or a salt thereof; and (C) 20 to 45 W / V% of water of the whole preparation. (2) menthol, chlorpheniramine maleate of 3 W / V% or more of the whole preparation, and 20 to 30% of the whole preparation;
An antipruritic solution comprising 45 W / V% water.