KR100525842B1 - Nicotinamide-containing ceramide liquid crystal and cosmetic composition comprising the same - Google Patents

Abstract

The present invention is a ceramide liquid crystal composed of ceramide, nonionic surfactant, cetostearyl alcohol, cholesterol and oil in a weight ratio of 2.0 to 6.0: 1.0 to 2.0: 1.0 to 2.0: 2.0 to 4.0: 1.0 to 2.0. The present invention relates to a nicotinamide-containing ceramide liquid crystal comprising 0.1 to 10% by weight of nicotinamide, and to a cosmetic composition comprising 0.1 to 20% by weight of the total weight of the cosmetic composition. It has superior retention and provides excellent dry skin improvement effect and provides excellent cosmetic composition in stability.

Description

Nicotinamide-containing ceramide liquid crystal and a cosmetic composition comprising the same {Nicotinamide-containing ceramide liquid crystal and Cosmetic composition comprising the same}

The present invention relates to a nicotinamide-containing ceramide liquid crystal and a cosmetic composition comprising the same, more specifically, ceramide (ceramide), nonionic surfactant, cetostearyl alcohol, cholesterol and oil, respectively 2.0 to 6.0: 1.0 to Nicotinamide-containing ceramide liquid crystal, characterized in that 0.1 to 10% by weight of nicotinamide is contained in the ceramide liquid crystal compounded in a weight ratio of 2.0: 1.0 to 2.0: 2.0 to 4.0: 1.0 to 2.0 and 0.1 per the total weight of the cosmetic composition It relates to a cosmetic composition comprising 20 to 20% by weight.

In general, the normal stratum corneum has a water content of about 10 to 30%, and thus the skin surface is smooth and soft, and maintains normal body protection. However, even healthy skin is prone to poor skin condition or lack of water due to the variable external environment. Thus, when the moisture content of the stratum corneum is less than 10%, the skin becomes rough and the body loses its protective function, causing aging.

On the other hand, according to the results of comparing and analyzing normal skin and dry skin to examine the moisture state in the stratum corneum, it is known that dry skin has less water content than normal skin. Dry skin has a weakening of the stratum corneum's cohesion, causing the scalp to peel off from the surface of the skin, resulting in scaling phenomenon. Drying the skin reduces the water content of the stratum corneum and prevents the barrier from functioning properly. Because.

According to a recent study, ceramide, a major component of intercellular lipids present in the stratum corneum, plays an important role in the stratum corneum retention, barrier function, and cohesion and adhesion of keratinocytes. Therefore, if the ceramide component is naturally generated in the intercellular lipids of the stratum corneum to maintain the moisture retention ability of the stratum corneum and strengthen the barrier function, and if this condition persists, there will be no skin dryness or aging.

However, with age, the ceramide content in the intercellular lipids naturally decreases, and as a result, the moisture content of the stratum corneum naturally decreases. Examples of patents related to such ceramides include US Pat. Nos. 5294444, 5368857, and Japanese Patent Laid-Open No. 81-123210. In this patent, ceramide is regarded as playing an important role in the stratum corneum and it was simply formulated into a formulation and applied to cosmetics. However, in the simple compounding as described in the patent, ceramide was difficult to be formulated in a concentration sufficient to exhibit the efficacy in the product because of poor compatibility with other raw materials. Therefore, it was confirmed that the amount of use is limited, so it does not contribute much to the water retention and barrier function of the stratum corneum.

Nicotinamide, on the other hand, is a type of vitamin B called Vitamin-PP (Pellagra Preventive) by preventing Pellagra, a skin disease. The nicotinamide is a component of two important hydrogen transfer coenzymes, Nicotinamide Adenine Dinucleotide (NAD) and NADP (Nicotinamide Adenine Dinucleotide Phosphate), which are known to be involved in various physiological functions of various enzymes. In addition, nicotinamide has been reported to heal wound healing, sedation, water retention, and ceramide synthesis (Pharmacol. Biochem. Behav., 1996-4; 53 (4). 783-90, Ann N. Y. Acad. Scio., 1996-6; 15; 786; 135-51). In addition, World Patent No.9625943A describes the growth effect of nicotinamide hair and nails, European Patent No. 36422A describes the whitening effect, and Japanese Patent Publication No. 92-2777540 describes the moisturizing effect.

However, the patent shows that nicotinamide has various effects on the skin, and it was confirmed that the effect was not so great because it was simply formulated into a formulation and applied to cosmetics. This is due to the low percutaneous absorption of nicotinamide, a water-soluble substance (Mem Rager, "Factors Affecting Sorption of Topically Applied Substances, in Skin Permeation", Edited by Jelle Zat, Wheaton: Allured Publishing Co. (JL Zatz, ed., 1993: 62-66).

As a result, there have been examples of increased transdermal absorption of nicotinamide using amphoteric surfactants, but this also increased the transdermal absorption to some extent, but had disadvantages in terms of skin irritation (Girido, RS Hinds, J. J. Ho). Styneck, G Ridout, RS Hinz, JJ Hostynek, AK Reddy and RH Guy, Fund. Appl. Toxicol, 1991 16:41.

Accordingly, the present invention has been made to solve the above problems, the ceramide to maintain and maintain the water retention ability of the stratum corneum and to enhance the water retention ability, promote the synthesis of ceramide, excellent moisturizing effect and other nicotinamide with other raw materials It is an object of the present invention to provide a nicotinamide-containing ceramide liquid crystal that can be well blended to promote transdermal absorption.

Another object of the present invention is to provide a cosmetic composition having excellent moisture retention and excellent skin stability by increasing the percutaneous absorption by containing the nicotinamide-containing ceramide liquid crystal at a predetermined ratio per total weight of the cosmetic composition.

Nicotinamide-containing ceramide liquid crystal according to the present invention for achieving the above object is a ceramide, nonionic surfactant, cetostearyl alcohol, cholesterol and oil is 2.0 to 6.0: 1.0 to 2.0: 1.0 to 2.0: 2.0 to 4.0: It is mix | blended in the weight ratio of 1.0-2.0, It is characterized by comprised by 0.1-10 weight% of nicotinamide in this ceramide liquid crystal.

Cosmetic composition according to the present invention for achieving the above another object is characterized in that the nicotinamide-containing ceramide liquid crystal is contained 0.1 to 20% by weight per total weight of the cosmetic composition.

Hereinafter, the present invention will be described in detail.

In the nicotinamide-containing ceramide liquid crystal according to the present invention, ceramide, nonionic surfactant, cetostearyl alcohol, cholesterol and oil have a constant ratio, that is, 2.0 to 6.0: 1.0 to 2.0: 1.0 to 2.0: 2.0 to 4.0: 1.0 to 2.0. In the non-aqueous solvent mixture blended in a weight ratio of 0.1 to 10% by weight of nicotinamide. This is because when the non-aqueous solvent mixture forms a ceramide liquid crystal, it does not cause swelling process unlike other liquid crystals, so that the water-soluble substance nicotinamide is effectively contained in the ceramide liquid crystal.

In addition, the cosmetic composition according to the present invention, the ceramide liquid crystal containing the nicotinamide is contained by 0.1 to 20% by weight based on the total weight of the cosmetic composition to increase the percutaneous absorption and provide a good skin safety formulation.

The ceramide according to the present invention is a ceramide of yeast origin represented by the animal and plant origin cerevide and the following general structural formula, that is, ceramide I (Formula 1), ceramide II (Formula 2), and ceramide III (Formula 3). ), Ceramide IV (Formula 4), ceramide V (Formula 5), ceramide VI (Formula 6) is preferably used at least one ceramide selected from.

[Formula 1]

[Formula 2]

[Formula 3]

[Formula 4]

[Formula 5]

[Formula 6]

In addition, the nonionic surfactant for forming the nicotinamide-containing ceramide liquid crystal according to the present invention is a sebum-15 oleate represented by the following formula (7), a sebum-15 stearate of the formula (8), and a formula (9). CETEARETH, i.e., Cearares-15, Cateares-16, Cateares-17, Cateares-18, Cateares-20, Cateares-22, Cateares-23, Cateares-24, Cateares- Preference is given to using at least one substance selected from the group consisting of 25.

[Formula 7]

[Formula 8]

[Formula 9]

In the above formula (9), the average value of n is the number in each of Ceteares-15, 16, 17, 18, 20, 22, 23, 24, 25, that is, Ceteares-15 is n is 15 and Ceteares-23 is n This coincides with the number of names, such as 23, where R is a mixture of alkyl groups derived from cetyl and stearyl alcohol.

In addition, as the oil according to the present invention, it is preferable to use one or more selected from the group consisting of octyldodecanol, squalane, octyldodecyl myristate, octyl palmitate and caprylic capric triglyceride.

In addition, the mixing ratio of each component constituting the non-aqueous solvent-based ceramide liquid crystal according to the present invention is 2.0 to 6.0: 1.0 to 2.0: 1.0 to 2.0: 2.0 to 4.0 for ceramide, nonionic surfactant, cetostearyl alcohol, cholesterol and oil. It is preferable that it is a weight ratio of 1.0-2.0. If it is out of this range, the melting point is low or high, it is difficult to stabilize in the formulation.

In addition, in order to form the most stable nicotinamide-containing ceramide liquid crystal, it is preferable to add nicotinamide in an amount of 0.1 to 10% by weight based on the total amount of the nonaqueous solvent-based ceramide liquid crystal. If the nicotinamide is used in less than 0.1% by weight, the promotion of ceramide synthesis is weak, and if it is used in more than 10% by weight, the solubility of the nicotinamide is poor and precipitated, and in this case, the structure of the ceramide liquid crystal is weak, which is applied to the cosmetic composition. Doing so may reduce the stability of the cosmetic.

Meanwhile, the nicotinamide-containing ceramide liquid crystal composition according to the present invention may be prepared by heating and dissolving the components in a non-aqueous solvent in the above ratio, followed by emulsification by adding nicotinamide and naturally cooling.

The cosmetic composition according to the present invention preferably contains 0.1 to 20% by weight of nicotinamide-containing ceramide liquid crystal per total weight of the cosmetic composition, and is preferably used as a cosmetic composition comprising a formulation such as lotion, cream, and essence. This is because the use of nicotinamide-containing ceramide liquid crystals less than 0.1% by weight is insignificant, and when used at 20% by weight or more, it is difficult to prepare a formulation such as lotion, cream, and essence.

Hereinafter, the present invention will be described in detail by Examples and Experimental Examples. However, these examples illustrate, but do not limit, the present invention.

Examples 1 to 3

Propylene glycol was used as a solvent according to the composition of Table 1 below, and the raw materials of 2 to 6 were heated and dissolved at 80 to 85 ° C. while stirring. Nicotinamide was added thereto at 70 to 75 ° C, and then emulsified for 3 to 4 minutes under the condition of a homomixer at 2000 to 2500 rpm, and then cooled to 45 to 50 ° C while stirring. Natural cooling to prepare a nicotinamide containing ceramide liquid crystal composition.

TABLE 1

The numerical unit used in Table 1 above is weight percent. In addition, Ceramide is a product of Ceramide LS3773, a product of Serobiologiques, France, Ceteares is Enmulgin B ₂ , a product of Henkel, Germany, and Octyldodecanol is a product of Henkel, Germany. Phosphorous ethanol-G (Eutanol-G) and nicotinamide were used as products of Roche, Switzerland.

Examples 4-6 and Comparative Examples 1-3

Oil-in-water emulsions were prepared with compositions as shown in Table 2 to investigate the effects of water retention, transdermal absorption measurement and dry skin improvement of the cosmetic composition including nicotinamide-containing ceramide liquid crystals. That is, in Examples 4 to 6, the nicotinamide-containing ceramide liquid crystal obtained in Example 3 was used, and in Comparative Examples 1 to 3, nicotinamide was simply mixed in a general manner to prepare an oil-in-water emulsion according to the following method.

First, the aqueous phase and the oil phase were dissolved by heating at 75 to 80 ° C., respectively, and then the oil phase was added to the aqueous phase. The mixture thus obtained was emulsified under homomixer 4000 to 6000 rpm for 4 to 6 minutes, and then nicotinamide-containing ceramide liquid crystal was added at 45 to 50 ° C. to obtain an oil-in-water emulsion.

TABLE 2a

TABLE 2

TABLE 2b

Table 2 continued

The unit of the numerical value used in Table 2 is weight%. Carboxyvinyl polymers are also available in US B.F. Carbopol 941, a product of BF Goodrich, was used as a 1% by weight aqueous solution.Solbitan monostearate was used with Arlacel 60, a product of ICI, USA, and Pioy (20). Tanmonostearate used Tween 60, a product of Isaiah, USA, and isocetyloctanoate, ICEH, a product of Nihon Kokyu Alcohol, Japan.

Experimental Example 1 transdermal absorption measurement test

To evaluate the transdermal absorption promoting effect of nicotinamide, three skin permeation tests were performed using the skin of hairless mice. 48 μl of samples were injected into the surface of 7.5 mm in diameter, and the amount of nicotinamide permeated after 24 hours using a transdermal absorption device (Microette, Hanson Co.) was analyzed by high-performance liquid chromatography. Quantification The results are shown in Table 3 as transmittance (%).

TABLE 3

As shown in Table 3, in Examples 4 to 6, which are cosmetic compositions containing nicotinamide-containing ceramide liquid crystals, transdermal absorption was significantly promoted as compared with Comparative Examples 1 to 3, and nicotine was increased as the content of the non-aqueous solvent-based ceramide liquid crystals increased. Transdermal absorption of amides increased proportionally. This is believed to be due to an increase in the concentration of nonionic surfactant and ceramide with increasing content of ceramide liquid crystal.

Experimental Example 2 skin primary irritation test

In order to examine the skin irritation properties of the samples prepared according to Examples 4 to 6 and Comparative Examples 1 to 3, a predetermined amount (0.2 g) of each sample was patched on the back of a healthy adult male and female for 24 hours. It was. The pin chamber was then removed and after 4 hours the skin condition change was read. The criteria for evaluation are as follows.

-: No erythema or unusual phenomenon

+-: Slightly reddish

+: Significantly redder than the surroundings

++: Severe reddening and swelling around

In addition, the degree of stimulation was determined according to Equation 1 below.

[Equation 1]

Stimulus degree = [(±) number * 1 + (+) number * 2 + (++) number * 3] / (±) number * 1 + (+) number * 2 + (++) number * 3 + ( -)Number]

The results are shown in Table 4.

TABLE 4

As can be seen from the results of Table 4, Examples 4 to 6, which promote percutaneous absorption, showed stable irritation with no significant difference compared to Comparative Examples 1 to 3.

Experimental Example 3 Moisture Retention Capacity Test

In order to determine the water retention capacity of the samples prepared according to Examples 4 to 6 and Comparative Examples 1 to 3, the following test was performed twice a day for three months on 24 men and women with dry hands on the back. Was performed.

First, the skin moisture content measuring device (skin sulfis hygrometer) is used to measure the moisture content of the skin before using the samples according to Examples 4 to 6 and Comparative Examples 1 to 3 in the area of 4 cm × 4 cm of the subject's hand and the like. (Skin Surface Hygrometer), model name: SKICON-200, manufactured by IBS of Japan). The skin moisture content was then measured after 3 months of use of the samples in the same manner. The results are shown in Table 5 (unit of numerical values used here is ㎲).

TABLE 5

As can be seen from the results of Table 5, in Examples 4 to 6 containing nicotinamide-containing ceramide liquid crystals, the effect of retaining water was superior to Comparative Examples 1 to 3 in which nicotinamide was simply blended. Water retention capacity also increased significantly in proportion to nicotine content.

Experimental Example 4 Test for Measuring Dry Skin Improvement Effect

In order to examine the dry skin improvement effects of the samples prepared according to Examples 4 to 6 and Comparative Examples 1 to 3, the males and females of the dry hand region were subjected to twice a day for three months. The test was performed.

First, the scale generated on the skin before using the samples according to Examples 4 to 6 and Comparative Examples 1 to 3 in the area of the 4 cm × 4 cm area of the subject's hand, etc., was selected as a dry evaluation parameter. After measuring the scale of the hand, the scale area was measured by image analysis. Then, after using the samples for 3 months in the same manner, the scale area generated on the skin was measured. The results are shown in Table 6 and the figures used are% of scale area.

TABLE 6

As can be seen from the results of Table 6, Examples 4 to 6 containing nicotinamide-containing ceramide liquid crystals significantly reduced the scale area compared to Comparative Examples 1 to 3 in which nicotinamide was simply blended. From this it can be seen that the nicotine-containing ceramide liquid crystal according to the present invention is excellent in the improvement effect of dry skin.

As described above, the cosmetic composition containing the nicotinamide-containing ceramide liquid crystal according to the present invention has remarkably promoted transdermal absorption, excellent moisture retention ability, excellent dry skin improvement effect and excellent stability.

Claims (2)

One or more ceramides selected from cerebroside, ceramide I, ceramide II, ceramide III, ceramide IV, ceramide V and ceramide VI derivatives; Fiji-15 Olate, Fiji-15 Stearate, Cetearece-15, Cateares-16, Cateares-17, Cateares-18, Cateares-20, Cateares-22, Cateares-23, Cete At least one nonionic surfactant selected from the group consisting of Ares-24 and Ceteares-25; Cetostearyl alcohol; cholesterol; And At least one oil selected from the group consisting of octyldodecanol, squalane, octyldodecyl myristate, octyl palmitate and capric capric triglyceride; Each of these Nicotinamide-containing ceramides comprising 0.1 to 10% by weight of nicotinamide in a non-aqueous solvent-based ceramide liquid crystal formulated at a weight ratio of 2.0 to 6.0: 1.0 to 20: 1.0 to 2.0: 2.0 to 4.0: 1.0 to 2.0. LCD Cosmetic composition comprising 0.1 to 20% by weight of the nicotinamide-containing ceramide liquid crystal according to claim 1 per total weight of the cosmetic composition.