JPH0469124B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a moisturizer containing pantetheine-S-sulfonic acid and its salt as an active ingredient. Humectants are included in various cosmetics and medicines for treating diseases for the purpose of preventing skin dryness. In particular, treatments for senile skin pruritus are attracting attention because it is difficult to treat. In general, pruritus skin refers to a disease in which there is no primary rash and only pruritus. Later, as the skin is itchy, epidermal exfoliation occurs, which increases skin sensitivity and becomes a cause of skin diseases such as eczema. In some cases, it may develop over time and lead to pigmentation. The disease can occur anywhere in the body, and is particularly likely to occur in the elderly, in which case it is called senile pruritus. In many cases, the cause is dryness and atrophy of the skin due to a decrease in the moisturizing ability associated with skin aging, and metabolic abnormalities such as liver damage, kidney damage, and diabetes are also cited as the root cause. Conventionally, the only treatments used have been the application of antipruritic agents as local therapy, and the administration of antihistamines and vitamins as systemic therapy. However, the current situation is that it is difficult to treat, has irritation problems when applied externally, and has side effects associated with long-term oral administration. The present inventor focused on the fact that the cause of senile skin pruritus is dryness of the skin associated with aging, and that it is more likely to occur in the winter. After various studies on pantetheine,
It has been discovered that S-sulfonic acid and/or its salts have extremely good moisture retention properties. This pantetheine-S-sulfonic acid and/or its salt has the following formula: (In the formula, M represents hydrogen, alkali metal, or 1/2 alkaline earth metal.) It is derived from edible carrots and has an extremely safe LD ₅₀ (rat) of 10 g/Kg or more when administered orally. It not only has a high level of irritation when applied locally, but also has the characteristic of reducing the irritation of compounded drugs.
(Japanese Patent Application Laid-Open No. 58-4721) Therefore, the effects of pantetheine-S-sulfonic acid and its salts in the present invention are recognized to be due to their strong moisturizing and water-retaining effects, and are highly expected from a clinical perspective. The moisturizing agent of the present invention is preferably administered parenterally, and in the case of parenteral administration, it can also be used as an external preparation or a patch. Further, the dosage of the active ingredient according to the present invention varies depending on the symptoms, but for external administration, an external preparation containing 0.1 to 10%, preferably 2 to 10% is suitable. Furthermore, the active ingredient of the present invention can be used in combination with commonly used antihistamines such as chlorpheniramine maleate and crotamiton, itch agents, vitamins, corticosteroids, sex hormones, etc., and a synergistic effect can be expected. It is something. To formulate the active ingredient of the present invention, surfactants, excipients, lubricants, flavoring agents, coloring and flavoring agents, preservatives, wetting agents, and other adjuvants are appropriately used in accordance with conventional methods. Next, Test Examples 1 to 3 in which the above compounds exhibit outstanding moisturizing effects will be shown. Test example 1 Hygroscopicity test Glycerin, sorbitol and pantetheine-S
− Dry sample of calcium sulfonate salt at relative humidity
81%, placed in a desiccator at a temperature of 25°C, and weighed over time. As an indicator of hygroscopicity, % weight increase was used. The results are shown in Figure 1. In FIG. 1, A represents pantetheine-S-sulfonic acid calcium salt, B represents glycerin, and C represents sorbitol. As a result, pantetheine-S-sulfonic acid calcium salt shows a moisture absorption effect superior to that of sorbitol, although it is inferior to that of glycerin. Test example 2 Moisture retention test Glycerin, sorbitol and pantetheine-S
- A dry sample of sulfonic acid sodium salt was mixed with about 10% water, left in a silica gel desiccator at a temperature of 25°C comparable to the dry season in winter, and weighed over time. Note that the moisture residual rate was used as an indicator of moisture retention. The results are shown in Figure 2. While glycerin and sorbitol release moisture quickly, pantetheine-S-sulfonic acid sodium salt has a very slow tendency to release moisture. It was revealed that it has moisturizing properties even under such conditions. In FIG. 2, A' represents pantetheine-S-sulfonic acid sodium salt, B represents glycerin, and C represents sorbitol. Test Example 3 Water retention effect The water retention effect of the sodium salt of pantetheine-S-sulfonate of the present invention was tested by attaching sodium salt of pantetheine-S-sulfonate and urea as a comparison to keratin powder, which is a component of the stratum corneum of the skin. Ivy. That is, test solution and comparison solution of each concentration were added dropwise to approximately 0.25 g of keratin powder, thoroughly absorbed into the keratin, dried in a standard desiccator to obtain a constant weight, and then left in a desiccator at a relative humidity of 79% and a temperature of 25°C to obtain a constant weight. shall be. This was weighed to determine the water retention amount of keratin (mg/100mg). The results are shown in Table 1.

[Table] As is clear from Table 1, sodium pantetheine-S-sulfonate has a value that can cause a significant increase in water absorption as the concentration increases, potentially causing the opposite effect of dehydration from the skin. Salt has little concentration dependence, indicating that it provides a sufficient water retention effect even at low concentrations. As is clear from the above test examples, the moisturizer according to the present invention not only has no safety problems, but also clearly shows that the concentration in actual use is even higher than that of urea, which is a typical moisturizer currently in use. It has strong water-retaining properties, and has stronger moisturizing properties than sorbitate and glycerin, making it an excellent moisturizing agent. In addition, considering that it has an anti-inflammatory effect, it is effective against the secondary increase in skin sensitivity associated with itching in senile skin pruritus, and it also has a strong melanin formation inhibiting effect. is also effective for pigmentation. Furthermore, even if only the moisturizing effect is considered, it can also be applied to progressive keratoderma and dry skin diseases. Therefore, the moisturizer according to the present invention can be said to be an ideal drug having excellent therapeutic effects as a symptomatic treatment agent for external use in a social environment where the number of elderly people will increase in the future. Next, examples of the present invention will be shown. Example 1 1 Ethanol 5.0g 2 Vegetable oil 0.1g 3 Polyoxyethylene hydrogenated castor oil 0.5g 4 Propylene glycol 5.0g 5 Sodium pantetheine-S-sulfonate
5.0g 6 Preservatives, fragrances Appropriate amount 7 Add purified water to make a total volume of 100ml. Dissolve 1, 2, and 3 and add this to the solution of 4 to 7 to obtain an aqueous solution type external preparation product. Example 2 1 Polyvinyl alcohol 20.0g 2 Ethanol 20.0g 3 Propylene glycol 3.0g 4 Sodium pantetheine-S-sulfonate
3.0g 5 Preservatives, fragrances Appropriate amount 6 Add purified water to make a total amount of 100g. 2 is moistened with 1, and this is added to a solution of the remaining ingredients in 6 while heating and dissolved under stirring to prepare a patch-type external preparation product. Example 3 1 Vaseline 2.5g 2 Liquid paraffin 10.0g 3 Cetostearyl alcohol 12.0g 4 Polyoxyethylene sorbitan monostearate 7.0g 5 Sorbitan monostearate 1.0g 6 Propylene glycol 5.0g 7 Pantetheine-S-calcium sulfonate
10.0g 8 Preservatives, fragrances Appropriate amount 9 Add purified water to make a total amount of 100g. 75 each for oil layers 1 to 5, water layers 6, 8, and 9.
Warm and emulsify at ℃. During cooling, add 7 to 30
Cool to ℃ and make a cream-type topical preparation (ointment-type product). Example 4 1 Microcrystalline wax 1.0g 2 Beeswax 2.0g 3 Lanolin 2.0g 4 Liquid paraffin 28.0g 5 Sorbitan sesquioleate 4.0g 6 Tween 80 1.0g 7 Aluminum stearate 0.2g 8 Glycerin 8.0g 9 Pantetheine-S- sodium sulfonate
5.0g 10 Crotamiton 10.0g 11 Preservatives, fragrances Appropriate amount 12 Add purified water to make a total of 100g. 70 each for oil layers 1 to 7, water layers 8, 11, and 12
Warm and emulsify at ℃. During cooling, add 9 and 10 and cool to 30°C to make an emulsion-type external preparation product.

[Brief explanation of drawings]

FIG. 1 is a diagram showing the results of the moisture retention test in Test Example, and FIG. 2 is a diagram showing the results of the moisture retention test in Test Example 2. A...Pantetheine-S-sulfonic acid calcium salt, B...Glycerin, C...Sorbit,
A'...Pantetheine-S-sulfonic acid sodium salt.

Claims (1)

[Claims] 1. (wherein M represents hydrogen, alkali metal or 1/2 alkaline earth metal)
A moisturizer containing S-sulfonic acid and/or a salt thereof.