JPS58128310A - Skin conditioner - Google Patents

Abstract

PURPOSE:A skin conditioner that contains pantethine as an active ingredient, thus being useful for improvement in changes caused by abnormality of lipid metabolism and for treatment of chromatosis. CONSTITUTION:The objective skin conditioner contains pantethine by 0.01-5, preferably 0.1-1wt%. The product is directly applied to skins for external purpose to improve the abnormality of lipid metabolism causing skin roughening, hypersteatosis, further improve fine wrinkles, skin texture and springiness. Pantethine is very stable to heat and light, causing no discoloration, smell change, decomposition and deactivation with time and can be combined with a variety of base materials for external use, further used safely without toxicity and skin troubles.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a cosmetic or pharmaceutical skin quality improving agent containing pantethine.

Pantethine is found in living organisms along with pantethine, and is reduced to form pantethine, a component of acetyl coenzyme, acedel carrier protein, etc.
It is known to have a wide range of physiological actions, including involvement in carbohydrate metabolism, fatty acid decomposition, synthesis, etc. Pantethine has recently attracted attention for its pharmacological effects, and its effects on fat metabolism and prevention and repair effects on arteriosclerosis are currently being elucidated, but there are no known examples of it being applied to the skin as an external drug. Air.

Abnormalities in the skin, particularly abnormalities in lipid metabolism, are generally thought to be caused by dysfunction in the sebaceous glands, and may appear as dry symptoms such as rough skin or rashes, or conversely, may be caused by excessive sebum secretion. Symptoms such as acne formation are seen. Other skin abnormalities include hyperpigmentation, such as age spots, freckles, and dark skin.

Until now, placenta preparations and vitamins have been mainly used to normalize rough skin and rough skin, but they have not been effective in a substantial sense.

Other methods include the use of male hormones, but excessive use of these can alter the balance of sebum secretion and may even interfere with normal metabolism. In addition, the use of female hormones can be considered to treat excessive sebum secretion, but unlike male hormones, dryness symptoms tend to become excessively obvious, so neither method is satisfactory.

As a result of intensive research into the effects of external use of pantethine, the present inventors found that pantethine can regulate lipid metabolism in the skin according to the symptoms, and has shown that pantethine can regulate skin roughness,
Based on abnormalities in lipid metabolism such as rough skin and excessive sebum secretion (
The present invention was completed after discovering that it is effective for improving skin changes and treating skin abnormalities such as hyperpigmentation.

Pantethine, which is an active ingredient of the lipid improving agent of the present invention, is a compound represented by the following formula, and is a substance produced by disulfide bonding between two molecules of pantethine and less than 2 mercapto groups. As methods for obtaining this, for example, a synthetic method using pantothenic acid as a starting material, a method in which coenzyme A is synthesized in a single stage, and various other methods are known. (Refer to each publication No. 3324).

According to the invention, pantethine is used in the form of creams, lotions, powders, ointments, etc. together with excipients, diluents, adjuvants, etc. These cosmetics and pharmaceutical preparations can be manufactured by conventional methods.

The content of pantethine contained in the skin quality improving agent of the present invention is usually 0.01 to 5% by weight, preferably 0.1 to 1% by weight.
It is. If the amount is less than 0.01% by weight, sufficient effects cannot be obtained. Moreover, if the amount exceeds 5% by weight, the effect will not be enhanced and it will be uneconomical.

Pantethine, the active ingredient of the skin quality improving agent of the present invention, is extremely stable against heat and light, and does not undergo changes over time such as discoloration, odor, or decomposition and inactivation even when made into a preparation. It is extremely advantageous in that it can be easily blended into the base. Furthermore, there is no concern about toxicity or skin damage (it can be used safely).

The skin quality improving/nourishing agent of the present invention is far more effective than those using vitamins and hormones, which are said to be effective in improving lipid metabolism. When applied directly to the skin as an external preparation, this agent not only improves abnormalities in lipid metabolism such as rough skin and chapped skin, but is also effective in improving fine wrinkles, skin texture, firmness, etc.

The effects of improving lipid metabolism and treating hyperpigmentation using the skin quality improving agent of the present invention were investigated, and compared with a commercially available cream containing vitamin E. The method of application was to apply the products of Examples 1 to B to the affected areas of the face of 18 women aged 20 to 40 with skin abnormalities such as rough skin, rough skin, acne, and age spots twice a day, once in the morning and before going to bed. The treatment was applied continuously for 6 months, and the treatment status of the affected area was observed and reported. The result is the first
Shown in the table. It is known that the skin quality improving agent of the present invention is significantly superior to commercially available products.

In particular, the skin quality improving agent of the present invention showed excellent effects on four women with considerably worsened symptoms.

(A) The degree of improvement is self-assessed. 1: No change 2: I feel like it has improved somewhat. 6: Slightly improved 4: Clearly improved The average value is shown in the table.

(B) Comparisons with commercially available products are made using the half-face comparison method. 6: The main rule is extremely good. 2: The main rule is slightly better. 1: Equivalent to the main rule. The average value is shown. Shown inside.

Table 1 Parts in the examples below refer to weight.

Example 1 (skin cream) FA>Squalane 10.0 parts Vaseline
10.0 parts beeswax 6.0 parts micro wax 90 parts whale wax
6,0 parts isopropyl myristate
12. Part o Sorbitan monostearate 5.0 parts Methyl paraoxybenzoate 0.1 part (B) 1
．． 3-Butanediol 10.0 parts Pantethine
o, part i Distilled water 62.8 parts (C) Perfume 0.5 parts The oil component (A) and the aqueous component CB) are separately heated to 80° C. and dissolved, and both are mixed and emulsified. Next, fragrance (C) is added while cooling, and the product is cooled to 60°C.

Example 2 (skin cream) FA) Cetanol 6.5 parts spermaceti
6.0 parts Lanolin 2.0 parts Liquid paraffin 20.0 parts Antioxidant 0.1 part Sorbitan monooleate 2.0 parts Pantethine 0.5 parts CB) Glycerin 10.0 parts Distilled water
52.0 parts (C) Fragrance 0.4 parts (A) and CB) were separately heated to 80°C and dissolved, and both were mixed and emulsified. , cool, add fragrance, and uniformly disperse to form a product.

7 Example 6 (Skin powder) (A) Talc 95 parts Zinc white
. Part Zinc stearate 2 parts (B) Pantethine 1 part (C) Fragrance
After dissolving an appropriate amount of pantethine (B) in a solvent and thoroughly mixing and dispersing it in the powder component of (A), the solvent was distilled off and the fragrance (C) was dissolved.
) and then dried to form a product.

Example 4 (lotion for acne) 1-Menthol 0.05 parts Propylene glycol 5.0 parts Pantethine
0.5 parts Alcohol 15.0 parts Fragrance 0.5 parts 8- Add distilled water to the above ingredients to make a total amount of 100 parts.

Example 5 (skin ointment) (A) Pantethine 1.0 parts isopropyl myristate 10.0 parts cetanol
10.0 parts Carbowax 5.0 parts (B) Liquid paraffin 59.0 parts Paraffin wax
5.0 parts (A) component is dissolved by heating to make it homogeneous,
A mixture of component (B) is added to this, and after cooling, the mixture is mixed to form a product.

Example 6 (skin ointment) (A) Sperm wax 12.5 parts White wax
12.0 parts Liquid paraffin 60.0 parts Vaseline 26.0 parts Pantethine 2.0 parts (B) Sodium borate 0.5 parts Distilled water
After heating and dissolving 17.0 parts (A) component at 70 to 80°C, (
B) Ingredients are gradually added and mixed, and the mixture is cooled to 30° C. or lower to form a product.

Test Example Stability tests of pantethine aqueous solution and vitamin C aqueous solution against heat, light, and changes over time were conducted.

The test method is as follows (a) to (C), and the sample is pantethine and vitamin C1'
(adjusted with N-hydrochloric acid) was used.

(a) Thermal stability = left at 100°C for 3 hours (b) Photostability: irradiated with sunlight for 3 days (C) Aging stability = 3 months at 40°C
Shown in the table. Pantethine has better stability than vitamin C in all respects, and can be advantageously used especially in the weak acidity required for the skin surface, and is expected to be effective as a preparation.

Table 2 Residual rate 2 〇: 90% or more ○: 8o~9o%Δ: 60~
80%×: Less than 6o% change Odor: None Professional: Slightly +: Yes Applicant Daiichi Pharmaceutical Co., Ltd. 1A representative Patent attorney ratio Masao Hayashi

Claims (1)

[Claims] A skin quality improving agent characterized by containing pantethine as an active ingredient.