JPH0546323B2 - - Google Patents

Description

Detailed Description of the Invention (Field of Industrial Application) The present invention relates to ointments and liquids containing hyaluronic acid or its salts and an antihistamine, and more specifically to senile xeroderma, skin keratosis, and mild atopic dermatitis. The present invention relates to ointments and liquids useful for the treatment of sexual dermatitis, etc.

(Prior art and problems) Conventionally, due to various causes such as improvement of housing environment and reduction of green areas in urban environments, the humidity in winter has progressed and the condition of human skin has become dry, especially in the elderly. As the skin ages, cases of senile xeroderma and skin keratosis are increasing due to low humidity.

As a countermeasure against xeroderma, etc., it is important to supply sufficient moisture to the skin surface and retain moisture in the skin. For these purposes, propylene glycol, 1,3-butylene glycol, pyrrolidone carboxylic acid Moisturizers containing hyaluronic acid, hyaluronic acid, etc. have been provided, and among these, external preparations containing hyaluronic acid etc. are the most favorable and have come to be widely used.

Although conventional moisturizers such as those mentioned above show good results in cosmetically protecting and beautifying the skin, they are not sufficiently effective in treating conditions such as senile xeroderma as mentioned above. The problem was that it had little effect on problems such as itchiness that may occur.

On the other hand, antihistamines are commonly used to treat skin itching, etc., but although these antihistamines can temporarily suppress skin itching, they cannot be expected to have a fundamental therapeutic effect on the affected area. However, there is a problem in that it lacks lasting effects.

Therefore, an object of the present invention is to provide a topical drug that is useful as a skin moisturizer and is particularly effective in treating xeroderma and the like in the elderly.

(Means for solving problems) The following objects are achieved by the present invention.

That is, the present invention provides an ointment characterized by blending hyaluronic acid or a salt thereof and an antihistamine in an ointment base material, and an ointment characterized by blending hyaluronic acid or a salt thereof and an antihistamine in a liquid base. It is a liquid agent.

(Action) By using hyaluronic acid or its salt as an active ingredient in an ointment or liquid together with an antihistamine, it provides a sufficient moisturizer for xeroderma in the elderly, and also relieves the itching characteristic of xeroderma. The effect of treating the affected area itself can be obtained.

(Preferred Embodiments) Next, the present invention will be described in more detail by citing preferred embodiments.

The hyaluronic acid or its salt used in the present invention is a type of complex polysaccharide having N-acetylglucosamine and D-glucuronic acid as repeating constituent units, and has high water absorption and water retention properties. Hyaluronic acid and its salts can be used as they are in the present invention.

In addition, the antihistamine used in combination with the above-mentioned hyaluronic acid or its salt in the present invention is known as a treatment for ginma, allergic rhinitis, gastrointestinal tract allergy, systemic anaphylaxis, itching associated with skin diseases, itching due to drug reactions, etc. Examples thereof include chlorpheniramine maleate, d-chlorpheniramine maleate, diphenhydramine and its salts, isothipendyl hydrochloride, clemizole sulfate, diphenylimidazole, and the like.

The ointment and liquid preparation of the present invention are characterized in that the above-mentioned hyaluronic acid or its salt and an antihistamine are dissolved or dispersed in an ointment base material or a liquid base material.
The ratio of use of both is also important; for example, 50 parts of antihistamine per 1 part by weight of hyaluronic acid or its salt.
It is preferable to use it in a proportion of 200 parts by weight.
If the amount of hyaluronic acid or its salt used is too small, the moisturizing properties during use will be insufficient and the effect of the antihistamine agent will not be fully exerted. Furthermore, even if the amount of hyaluronic acid or its salt used is too large, the moisturizing properties will be sufficient, but the effect of the antihistamine will not be sufficient.

In the present invention, when the target product is an ointment, conventionally known ointment base materials can be used as base materials for dissolving or dispersing the above-mentioned hyaluronic acid or its salts and antihistamines, such as carboxymethylcellulose sodium salt, polyethylene glycol, etc. water-soluble polymers such as, vegetable oils such as olive oil,
Any conventionally known ointment base containing mineral oil such as vaseline, lower alcohol such as cetyl alcohol, etc. as a main ingredient can be used. Particularly preferred is the sodium salt of carboxymethyl cellulose.

Further, when the composition of the present invention is in liquid form, conventionally known lotion base materials, liquid agent base materials, etc. can be used as they are.

Furthermore, in the present invention, the above-mentioned hyaluronic acid or a salt thereof,
It goes without saying that in addition to the antihistamine and the base material, additives such as various stabilizers and preservatives that are added to general medicines, ointments, liquids, etc., may also be contained, if necessary.

In the composition of the present invention, the concentration of hyaluronic acid or its salt and the antihistamine agent relative to the entire composition is also important;
The antihistamine is preferably used in an amount of 0.01 to 1% by weight based on 100 parts by weight, while the antihistamine is preferably used in an amount of 0.5 to 5% by weight.
If either one is too little or too much, the synergistic effect of the two will not be satisfactory.

(Effect) According to the present invention as described above, by using hyaluronic acid or its salt and an antihistamine together as the active ingredients of an ointment or a liquid, sufficient moisturizing properties can be achieved for xeroderma in the elderly. It eliminates the itching characteristic of xeroderma and provides a therapeutic effect on the affected area itself. Of course, the ointments and liquid preparations of the present invention are not limited to the treatment of xeroderma, etc., but are also effective for their prevention, skin beautification, and treatment and prevention of rough skin, razor burn, itching, etc.

(Example) Next, the present invention will be explained in more detail with reference to Examples.

Example 1 Hyaluronic acid or its sodium salt 0.1g Carboxymethylcellulose sodium salt 2g Chlorpheniramine maleate 1g Methyl p-hydroxybenzoate 0.02g Propyl p-hydroxybenzoate 0.01g Ethanol 2ml Purified water Amount to make the total volume 100ml Above According to the prescription, add hyaluronic acid or its sodium salt and chlorpheniramine maleate to approximately 80 ml of purified water, and also add methyl p-hydroxybenzoate and propyl p-hydroxybenzoate that have been dissolved in ethanol in advance. Stir to dissolve. After dissolving, carboxymethylcellulose sodium salt and the remaining water were added and the whole was thoroughly mixed and homogenized to obtain an ointment of the present invention.

Comparative Example 1 Example 1 except that hyaluronic acid or its sodium salt was not used in Example 1.
An ointment of a comparative example was obtained in the same manner as above.

Example 2 Hyaluronic acid or its sodium salt 0.1g Chlorpheniramine maleate 1g Glycerin 10ml Methyl p-hydroxybenzoate 0.02g Propyl p-hydroxybenzoate 0.01g Ethanol 2ml Purified water Amount to make the total volume 100ml According to the above recipe Add hyaluronic acid or its sodium salt and chlorpheniramine maleate to approximately 80 ml of purified water, and also add methyl p-hydroxybenzoate and propyl p-hydroxybenzoate, which have been previously dissolved in ethanol, and stir to dissolve. let After dissolving, the glycerin salt and the remaining water were added and the whole was thoroughly mixed and homogenized to obtain a liquid preparation of the present invention.

Comparative Example 2 Example 2 except that hyaluronic acid or its sodium salt was not used in Example 2.
A liquid formulation of a comparative example was obtained in the same manner as above.

Usage Example When the ointments and liquids of Examples and Comparative Examples were thinly applied to the dry skin area of a 63-year-old elderly man at a rate of approximately 5 g/m ² and the progress was observed for 5 days after application, the following results were obtained. I got it.

Example 1: Skin dryness and itching were significantly suppressed, and a clear therapeutic effect was observed on papules and erythema, for which conventional antihistamines are not expected to be very effective. In addition, the patient was significantly relieved from the mental stress caused by the itching sensation. Therefore, by using hyaluronic acid or a salt thereof in combination with an antihistamine, the effect of conventional antihistamines was enhanced several times (2 to 3 times).

Example 2: The same effect as in Example 1 was obtained, and the product also had a refreshing feeling when used in summer.

Comparative Example 1: Although there was an effect of suppressing itching sensation, the suppressive effect was about half that of the example. In addition, the dryness of the skin did not stop, and cracks appeared on the skin surface in some areas, which worsened the situation. Furthermore, it had almost no effect on papules and erythema.

Comparative Example 2: Same as Comparative Example 1.

As described above, according to the present invention, an excellent synergistic effect that cannot be obtained with either hyaluronic acid or antihistamine alone can be obtained.

Claims (1)

[Scope of Claims] 1. An ointment characterized by containing hyaluronic acid or its salt and an antihistamine in an ointment base material. 2. A liquid agent characterized by containing hyaluronic acid or its salt and an antihistamine agent in a liquid agent base material.