JPH10330252A - Improving agent for atopic dermatitis - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an improving agent for atopic dermatitis, having high safety and excellent in improving effects on xeroderma, pruritus, keratinous moisture content, epidermal lipid content and easy irritability by formulating a specific compound as an active ingredient therein. SOLUTION: This improving agent for atopic dermatitis contains diisopropylamine dichloroacetate represented by the formula as an active ingredient. The amount of the improving agent for the atopic dermatitis formulated in a skin preparation for external use which is a medicine or a quasi-drug is 0.01-20 wt.% based on the total amount of the composition. An oil and fat, a humectant, a pigment, a coloring matter, a surfactant, an antioxidant, an ultraviolet light absorber, a preservative, a water-soluble polymer, etc., can suitably be formulated in the skin preparation for external use which is the medicine or quasi-drug. Furthermore, the improving agent can be prepared as a dosage form such as an ointment, a lotion, a milky lotion, a cream, a pack or a granule.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention is highly safe and improves skin dryness, pruritus, keratin water content, skin surface lipid content and irritability (the property of being less resistant to external stimuli). The present invention relates to an atopic skin improving agent having excellent effects.

[0002]

2. Description of the Related Art Patients with atopic skin have a lower skin surface lipid amount and keratin water content and a lower sebum film-forming ability than healthy subjects.
A decrease in the threshold of resistance to external stimuli is observed. Also,
In atopic skin patients, the barrier function of the skin is destroyed,
Abnormal dryness and pruritus of the skin occur. Conventionally, topical steroids, non-steroidal external preparations and the like have been used for the treatment and prevention of pruritus, and their effects are excellent, but their application needs to be devised from the viewpoint of safety. In addition, in order to prevent skin dryness, a combination of moisturizing cream and the like has been devised.

[0003] Therefore, it is highly safe and has excellent effects of improving skin dryness, pruritus, keratin water content, skin surface lipid content, and irritability (the property of being less resistant to external stimuli). What is desired is an atopic skin improving agent that is easy to treat.

[0004]

In view of such circumstances, the present inventor has found that the present inventors have high safety, dry skin, pruritus, keratin water content, skin surface lipid content and irritability (for external stimuli). As a result of diligent investigations into the search for a material having an improved effect on properties such as weak resistance, etc., surprisingly, it was found that diisopropylamine dichloroacetate showed such effects, and the present invention was completed. Thing,
Its purpose is high safety, dry skin,
It is an object of the present invention to provide an atopic skin improving agent excellent in the effects of improving pruritus, pruritus, keratin water content, skin surface lipid content, and irritability (the property of being less resistant to external stimulation).

[0005]

The above-mentioned object is achieved by an atopic skin improving agent containing diisopropylamine dichloroacetate as an active ingredient.

[0006]

DESCRIPTION OF THE PREFERRED EMBODIMENTS The present invention will be described below in detail.

The diisopropylamine dichloroacetate used in the present invention is represented by the following formula, is in the form of a white crystalline powder, has almost no smell, and has a bitter taste.
Easy to dissolve in water, ethanol, etc.

Embedded image

The melting point is 5 to 118 ° C. to 122 ° C.
% Aqueous solution has a pH of 5.6 to 6.8. The acute toxicity of diisopropylamine dichloroacetate in mice is as follows.

[0009]

[Table 1] Remarks (Uncorrected pH) (pH 7.4)

The atopic skin improving agent of the present invention may be the above substance itself, but may also contain a solvent such as water, an excipient, and the like.

Since the atopic skin improving agent of the present invention has an excellent atopic skin improving effect, it can be incorporated into, for example, a pharmaceutical or quasi-drug skin external preparation.

The amount of the atopic skin-improving agent of the present invention to be added to the skin or external preparation of a drug or a quasi-drug varies depending on the application target and cannot be specified unconditionally. 0.01 to 20 on the basis of
% By weight, and particularly preferably 0.05 to 10% by weight.

The pharmaceutical or quasi-drug skin external preparations of the present invention include oils and fats, humectants, pigments, pigments, surfactants, antioxidants, ultraviolet absorbers, and preservatives. And water-soluble polymers can be appropriately blended.

[0014] Further, any dosage form can be appropriately selected depending on the subject applicable to the skin such as ointments, lotions, emulsions, creams, packs, granules and the like.

[0015]

EXAMPLES In order to clarify the effect of improving atopic skin according to the present invention, comparative examples and examples are shown below.

Example 1, Comparative Example 1 (Effect of improving atopic skin) (1) Test preparations were prepared using ointments having the compositions shown in Table 2.
In the table, diisopropylamine dichloroacetate used in the present invention is abbreviated as DADA. The ointment was prepared by mixing the components shown in Table 2 (B) while heating to 80 ° C in a hot water bath.
The mixture was gradually added to a mixture of the components shown in Table 2 (A) heated to 80 ° C. with stirring. Next, use a homogenizer.
After vigorously stirring (2500 rpm) for 5 minutes to sufficiently emulsify and disperse each component, the mixture was gradually cooled with stirring to obtain.

[0017]

[Table 2]

(2) Test subjects Among the atopic skin patients, 30 men and women who agreed to participate in this test were targeted, and 30 cases were divided into two groups.
The test was performed on each of two groups, with five groups as comparative examples and 10 examples as examples.

(3) Test Method The ointment (test preparation) of the example was applied to 10 atopic skin patient groups and the ointment of the comparative example (test preparation) was applied to 5 atopic skin patient groups twice a day. . Use period is 4 in principle
Weeks.

(4) Observation items and evaluation method Observation date The degree of skin symptoms and subjective symptoms were observed before the test was started and, in principle, after 4 weeks, and described in the record summary.

2. Observation items and their evaluation Dryness and pruritus of the skin were evaluated in three stages: improvement, no change, and deterioration, and the results were described in the record summary.

3. Measurement of keratin water content and skin surface lipid content At the start of the test and 4 weeks later, SKICON-20 (manufactured by IBS) was used to measure keratin water content at the same site (three places), and Sebummeter SM810 (COURA)
GE and KHAZAKA).

4. Irritability All incidents observed during the study period were described in the summary of the record, with their symptoms and severity and the causal relationship with the test product.

5. Evaluation of usefulness Changes in each observation item before and after the use of the test preparation, keratin water content, skin surface lipid amount measurement results, comprehensively evaluate the side effects, the usefulness is quite useful, somewhat useful, does not seem to be useful, It was rated on a four-point scale, which was not preferred.

6. result

[0026]

[Table 3]

[0027]

[Table 4]

[0028]

[Table 5]

[0029]

[Table 6]

In the evaluation of dryness and pruritus in Table 3, in Comparative Example 1, there was one unfavorable case that strongly felt pruritus, and four cases that did not seem to be useful reported skin irritation. There was one case. On the other hand, in Example 1 of Table 4, one case was quite useful and four cases were slightly useful, and there was no example showing easy irritation.

In Comparative Example 1, the difference in the amount of keratin water and the difference in the amount of skin surface lipid in Table 5 are low or negative. On the other hand, in Example 1 of Table 6, the values tended to be higher in the case of fairly useful cases and in the case of fairly useful cases.

From the above results, it was confirmed that Example 1 was superior to Comparative Example 1 in improving skin dryness, pruritus, keratin water content, skin surface lipid content and irritability.

[0033]

[Table 7]

[0034]

[Table 8]

[0035]

[Table 9]

[0036]

[Table 10]

In the evaluation of dryness, pruritus and irritability shown in Table 7, in Comparative Example 2, there were two unfavorable cases complaining of discomfort or pruritus, and three cases which were not considered useful. On the other hand, in Example 1 of Table 8, three cases were quite useful and four cases were slightly useful, and there was no example showing easy irritation.

In Comparative Example 2, the difference in the amount of keratin water or the difference in the amount of skin surface lipid in Table 9 is low or negative. On the other hand, in Example 2 of Table 10, the numerical values tended to be higher in the case of fairly useful cases and in the case of slightly useful cases.

From the above results, it was confirmed that Example 2 was superior to Comparative Example 2 in improving skin dryness, pruritus, keratin water content, skin surface lipid content and irritability.

Examples of the present invention will be further described, but the present invention is not limited to these examples.

Examples 3 to 5 (liquids)

[0042]

[Table 11]

Each of the above components is dissolved in purified water, and the mixture is stirred and homogenized to obtain a liquid preparation.

Examples 6 to 9 (cream)

[0045]

[Table 12]

After the component (A) was uniformly mixed and dissolved at 80 ° C., the component (B) was mixed and dissolved therein (mixture I). Separately, the component (D) was uniformly mixed and dissolved at 80 ° C., and then the component (C) was mixed and dissolved therein (mixture liquid II).
Next, the mixture II was gradually added to the mixture I, and the mixture was cooled to 30 ° C. with sufficient stirring to obtain a cream.

Examples 10 to 12 (Lotion)

[0048]

[Table 13]

Each component was mixed and dissolved to prepare a lotion.

[0050]

As described above, according to the present invention, safety is high, skin dryness, pruritus, keratin water content, skin surface lipid content and irritability (resistance to external stimuli are high). Weak nature)
It is clear that an atopic skin improving agent excellent in the effect of improving skin can be provided.

Claims (1)

[Claims] An atopic skin improving agent comprising diisopropylamine dichloroacetate as an active ingredient.