JP2002003358A - Skin care preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin care preparation capable of preventing flabby skin, deletion of gloss, or the like, besides prevention of chapped skin and improvement in chapped skin and having a high effect on prevention of aging. SOLUTION: This skin care preparation is obtained by formulating one or more kinds of extracted solutions of plants selected from Sophora angustifolia, Acacia catechu, Eugenia aromatica, Saxifraga stolonifera, hop, rosemary, lithospermum root, Hypericum erectum Thunb, Hypericium perforatium L. and tea with tranexamic acid as active ingredients.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin,
More specifically, the present invention relates to a skin external preparation having a high effect of preventing skin aging, preventing sagging of skin, loss of gloss, and the like, in addition to prevention of skin roughness and improvement of skin roughness.

[0002]

2. Description of the Related Art Conventionally, tranexamic acid has been used in pharmaceuticals as an anti-inflammatory agent, and it has recently been found that tranexamic acid has an effect of improving rough skin, but the effect of preventing aging is still insufficient. Did not meet the expectations. In addition, there has been a demand for a further improvement in rough skin.

[0003]

Means for Solving the Problems The inventors of the present invention have conducted intensive studies to find a method for preventing skin aging and improving skin roughness, and for improving the effect of preventing aging by preventing sagging of the skin and loss of gloss. It has been found that this object can be achieved by blending a specific plant extract with tranexamic acid, and the present invention has been completed.

[0004]

That is, the present invention relates to a plant extract selected from the group consisting of Clara, Acacia, Clove, Saxifraga, Hop, Rosemary, Sikon, Hypericum, St. John's wort and tea. Tranexamic acid and tranexamic acid as active ingredients. A skin external preparation for improving skin roughness and a skin external preparation for preventing aging.

[0005] All of the plant extracts used in the present invention are known to have an elastase inhibitory action (JP-A-10-17460, JP-A-10-17460).
JP-A-182414, JP-A-11-246337, JP-A-11-246338, JP-A-11-246
246385, JP-A-11-2466386, JP-A-11-246387, JP-A-11-2
46388, JP-A-11-315008). The amount of these plant extracts is 0.00001 to 0.1% by weight, preferably 0.00.0% by weight, based on the total amount of the external preparation for skin.
001 to 0.1% by weight. If the amount is less than 0.00001% by weight, the effect is not exhibited. If the amount exceeds 0.1% by weight, precipitation occurs over time, which is not preferable in terms of stability.

[0006] The amount of tranexamic acid in the present invention is not particularly limited, but is preferably in the total amount of the external preparation for skin.
0.01 to 10.0% by weight, more preferably 0.1%
~ 5.0% by weight.

[0007] In addition to the above-mentioned essential components, the skin external preparation of the present invention also contains other components usually used in skin external preparations such as cosmetics and pharmaceuticals, such as avocado oil, palm oil, peanut oil, rice bran oil, jojoba oil. , Carnauba wax, lanolin,
Oils such as liquid paraffin, oxystearic acid, isostearyl palmitate, isostearyl alcohol; humectants such as glycerin, sorbitol, polyethylene glycol, pyrrolidone carboxylic acid and its salts, collagen, hyaluronic acid and its salts, chondroitin sulfate and its salts Ultraviolet absorbers such as amyl paradimethylaminobenzoate, urocanic acid and ethyl diisopropylcinnamate; antioxidants such as sodium erythorbate, sage extract and parahydroxyanisole; sodium stearyl sulfate, diethanolamine cetyl sulfate, cetyltrimethylammonium saccharin, Surfactants such as polyethylene glycol isostearate and glyceryl arachiate; preservatives such as ethylparaben and butylparaben;
Extracts such as oak, spinach, loquat, peonies, assemblage, birch, carrot, aloe, mallow, iris, grape, yokuinin, loofah, lily, saffron, senkyu, ginger, ononis, garlic, etc .; glycyrrhizic acid derivatives, glycyrrhetinic acid derivatives , Salicylic acid derivatives, hinokitiol, zinc oxide, allantoin and other anti-inflammatory agents; placental extracts, glutathione, ascorbic acid derivatives and other whitening agents; royal jelly, photosensitizers, cholesterol derivatives, activators such as various amino acids, etc .; Blood circulation promoters such as sodium sulfate; antiseborrheic agents such as sulfur and thiantole; fragrance; water; alcohol; thickeners such as carboxyvinyl polymer; coloring agents such as titanium yellow, carsamine, and safflower red, if necessary. Mix appropriately Door can be.

[0008] The dosage form of the external preparation for skin of the present invention is arbitrary,
Any dosage form, such as a solution system, a solubilizing system, an emulsifying system, a powder dispersing system, a water-oil two-layer system, a water-oil-powder three-layer system, may be used.

The use of the external preparation for skin of the present invention is also optional. Facial cosmetics such as lotions, emulsions, creams, packs and the like, makeup cosmetics such as foundations, lipsticks, eye shadows, etc., body cosmetics and detergents , Ointments and the like.

[0010]

EXAMPLES Next, the present invention will be specifically described with reference to Examples and Comparative Examples. The present invention is not limited by this. The compounding amount is% by weight.

Examples 1 to 10 and Comparative Examples 1 to 12 Creams having the following formulations were prepared by the method described below. A. Cetanol 0.5% by weight Vaseline 2.0 Squalane 7.0 Self-emulsifying glyceryl monostearate 2.5 Polyoxyethylene sorbitan monostearate (20EO) 1.5 Pantothenyl ethyl ether 0.5 Jojoba oil 5.0 B. Dipropylene glycol 5.0 1,3-butylene glycol 5.0 Vegum (montmorillonite) 5.0 Plant extract (as dry solids) Transcriptic acid described in Tables 1 to 3 Potassium hydroxide described in Tables 1 to 3 3 water residue

(Preparation method) A (oil phase) and B (aqueous phase) are each heated to 70 ° C. and completely dissolved. Add A to B and emulsify with an emulsifier. The emulsion was cooled using a heat exchanger to obtain a cream.

[0013]

[Table 1] {Example 1 2 3 4 5 6 7 8} ──────────────────────────────── Clara extract 0.001 − − − − − − − − Acacia extract − 0.001 − − − − − − Clove extract − − 0.001 − − − − − Saxifraga extract − − − 0.001 − − − − Hop extract − − − − 0.001 − − − Rosemary extract − − − − − 0.001 − − Sicon Extract − − − − − − − 0.001 − Hypericum extract − − − − − − − − 0.001 Tranexamic acid 2.0 2.0 2.0 2.0 2.0 2.0 2.0 2.0 ─────────────────── ───────────────

[0014]

[Table 2] Example 9 10 Comparative Example 1 2 3 4 5 6 ────────────────────────────────── Hypericum perforatum extract 0.001 − − − − − − − − tea extract − 0.001 − − − − − − − Clara extract − − − 0.001 − − − − Acacia extract − − − − 0.001 − − − Clove extract − − − − − 0.001 − − Saxifraga extract − − − − − − 0.001 − Hop extract − − − − − − − −0.001 Tranexamic acid 2.0 2.0 2.0 − − − − − ──────────────────────────── ──────

[0015]

[Table 3] Comparative Example 7 8 9 10 11 12 ────────────────────────────── Rosemary extract 0.001 − − − − − Sicon extract − 0.001 − − − − Hypericum Extract − − 0.001 − − − Hypericum perforatum extract − − − 0.001 − − tea extract − − − − 0.001 − tranexamic acid − − − − − − ─────────────── ───────────────────

The creams obtained in Examples 1 to 10 and Comparative Examples 1 to 12 were used to evaluate the effect of preventing and improving the roughness of the skin on the human body panel, and to evaluate the sagging and gloss of the skin.

That is, with respect to the effect of preventing skin roughness and improving skin roughness, the skin surface morphology of a healthy woman (face) is replicated using a replica method with silicone resin and observed with a microscope (17 ×). Using 110 persons (rough skin panels) determined to have skin roughness evaluations 1 and 2 based on the criteria shown in Table 4 based on the criteria shown in Table 4 based on the state of the skin pattern and the peeling state of the stratum corneum, Examples 1 to 10 and Comparative Example 1 Example 1
Twenty-two creams obtained in １２12 were allocated so that each of them was applied to ten persons and applied twice a day. Two weeks later, replicas on the left and right sides of the face were taken again, the condition of the skin was observed, and evaluated according to the criteria shown in Table 4. Tables 5 and 6 show the results.

For the sagging and gloss of the skin, the skin condition before and after using the above-mentioned panel was visually evaluated. The results are shown in Tables 5 and 6.

(Evaluation of visual observation) A: The skin is very sticky and there is no sagging. ：: There is still skin and no sagging. Δ: The skin does not have much swelling and feels sagging. ×: The skin has no sagging and is sagging.

[0020]

[Table 4] ──────────────────────────── Evaluation score ──────────────── ──────────── 1 Skin sulcus and skin hills disappear. Extensive stratum corneum turning. 2 Skin sulcus and skin hills are unclear. Turn of the stratum corneum. 3 Skin sulcus and skin ridge are observed but flat. 4 Skin sulcus and skin hills are clear. 5 Skin sulcus and skin ridges are clear and well-organized. ────────────────────────────

[0021]

[Table 5] {Example 1 2 3 4 5 6 7 8 9 10}レ プ リ カ Replica evaluation 1 0 0 0 0 0 0 0 0 0 0 0 2 0 1 1 1 0 0 1 0 0 10 32 10 32 33 21 22 22 42 22 33 21 35 22 15 15 6 6 7 6 5 6 6 6 7}観 Visual evaluation Before use ◎ 0 1 1 1 0 1 0 1 0 0 0 2 2 3 2 1 4 2 3 3 2 △ 5 4 5 6 4 4 3 5 4 3 × 3 3 1 2 1 5 1 4 2 3 5 After use ◎ 4 4 3 5 4 3 5 4 4 5 3 ○ 6 5 6 3 3 5 5 4 4 4 5 △ 0 1 1 2 3 2 0 2 1 2 × 0 0 0 0 0 0 0 0 0 0 0 ─────────── ───────────────────

[0022]

[Table 6] Comparative Example 1 2 3 4 5 6 7 8 9 10 11 12 レ プ リ カ Replica evaluation 1 1 3 2 4 2 1 3 4 3 3 4 4 6 2 3 5 5 4 6 5 4 5 5 4 3 4 3 3 3 1 1 1 1 ... ... ... ... ... ... ... 2 1 1 1 2 1 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 評 価 Visual evaluation Before use ◎ 0 0 0 0 0 0 0 0 0 0 0 0 0 2 3 10 2 1 2 2 0 1 1 3 0 3 4 5 6 2 5 4 7 7 5 4 6 × 5 3 4 4 4 6 4 4 1 3 4 3 4 After use ◎ 1 0 1 0 1 10 0 0 1 0 0 0 5 2 2 1 2 3 2 1 1 2 2 1 △ 3 4 5 6 4 3 4 5 4 5 6 x 13 3 4 13 5 5 5 3 4 2 4} ──────

From the results shown in Tables 5 and 6, the facial part using a cosmetic composition containing a specific plant extract and tranexamic acid was significantly more effective in preventing rough skin than the facial part using other cosmetics. It can be seen that the effect of improving skin roughness is recognized, and that the sagging and gloss of the skin are also significantly improved.

Example 11 Cream A. Stearic acid 10.0% by weight Stearyl alcohol 4.0 Butyl stearate 8.0 Monoglycerin stearate 2.0 Vitamin E acetate 0.5 Vitamin A palmitate 0.1 Macadamia nut oil 1 0.0 Perfume 0.4 Preservatives Appropriate amount B. Glycerin 4.0 1,2 Pentanediol 3.0 Ichiyakuso extract 1.0 Potassium hydroxide 0.4 Clara extract (as dry solids) 0.01 Tranexamic acid 0.1 Magnesium phosphate ascorbate 0.1 L-arginine hydrochloride 0.01 Erythritol 1.0 Trisodium edetate 0.05 Purified water residue (Preparation method) The oil phase of A and the aqueous phase of B are heated to 70C, respectively. Dissolve completely. Add phase A to phase B and emulsify with an emulsifier. The emulsion was cooled using a heat exchanger to obtain a cream.

Example 12 Cream A. Cetanol 4.0 wt% Vaseline 7.0 Isopropyl myristate 8.0 Squalane 15.0 Monoglycerin stearate 2.2 POE (20) Sorbitan monostearate 2.8 Vitamin E Nicotinate 2.0 Fragrance 0.3 Antioxidant qs Preservative qs B. glycerin 10.0 Zhuyaku extract 0.01 Dipropylene glycol 4.0 Hypericum extract (as dry solids) 0.1 Tranexamic acid 5.0 Pyrrolidone carboxy Sodium acid 1.0 Lysine 3.0 Disodium edetate 0.01 Purified water residue (Preparation method) A cream was obtained according to Example 11.

Example 13 Emulsion A. Squalane 5.0% by weight Oleyl oleate 3.0 Vaseline 2.0 Sorbitan sesquioleate 0.8 Polyoxyethylene oleyl ether (20EO) 1.2 Evening primrose oil 0.5 Fragrance 0 0.3 Preservatives Appropriate amount B.1,3-butylene glycol 4.5 Melissa extract 1.5 Ethanol 3.0 Carboxyvinyl polymer 0.2 Potassium hydroxide 0.1 L-Arginine L-aspartate 0.01 Chouzi Extract (as dry solids) 0.0001 Tranexamic acid 0.5 Erythritol 0.5 Sodium hexametaphosphate 0.05 Purified water Residue (Production method) An emulsion was obtained according to Example 11.

Example 14 Foundation A. Cetanol 3.5% by weight Deodorized lanolin 4.0 Jojoba oil 5.0 Vaseline 2.0 Squalane 6.0 Stearic acid monoglycerin ester 2.5 POE (60) hydrogenated castor oil 1. 5 POE (20) cetyl ether 1.0 pyridoxine tripalmitate 0.1 preservative appropriate amount perfume 0.3 B. propylene glycol 10.0 blended powder 12.0 L-arginine 5.0 asenyaku extract (as dry solids) ) 0.05 Tranexamic acid 0.05 Trisodium edetate 0.2 Purified water residue (Preparation method) A foundation was obtained according to Example 11.

Example 15 Lotion A. Ethanol 5.0% by weight POE oleyl alcohol ether 2.0 2-Ethylhexyl-P-dimethylaminobenzoate 0.18 Fragrance 0.05 B.1,3-butylene glycol 9.5 Sodium pyrrolidone carboxylate 0.5 Sodium hyaluronate 0.01 Sicone extract (as dry solids) 0.00001 Tranexamic acid 10.0 Nicotinamide 0.3 Glycerin 5.0 Hydroxypropyl β-cyclodextrin 1.0 Purified water Residue ( Production method) The alcohol phase of A was added to the aqueous phase of B and solubilized to obtain a lotion.

Example 16 Pack (1) Polyvinyl alcohol 10.0% by weight (2) Polyethylene glycol (molecular weight 400) 0.4 (3) Glycerin 3.0 (4) Ethanol (95%) 8.0 (5) Saxifraga extract (as dry solids) 0.1 (6) Tranexamic acid 1.0 (7) Preservative 0.1 (8) Perfume 0.1 (9) Purified water residue (Production method) (4), ( 7) and (8) are mixed and dissolved, and (1), (2) and (3)
And (5), (6), and (9) were mixed and dissolved at 80C, and the mixture was stirred and then allowed to cool to room temperature to obtain a pack.

[0030]

As described above, the external preparation for skin of the present invention, by combining a plant extract having an elastase inhibitory effect with tranexamic acid, prevents skin roughening and prevents sagging of the skin and loss of gloss. This has the advantage that the effect of preventing aging can be significantly increased.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (reference) A61K 7/00 A61K 7/00 U 7/021 7/021 31/222 31/222 35/78 35/78 J CD QA61P 17/00 A61P 17/00 43/00 111 43/00 111 F-term (reference) 4C083 AA111 AA112 AA122 AB032 AB282 AC012 AC022 AC072 AC102 AC112 AC122 AC132 AC182 AC242 AC352 AC402 AC422 AC432 AC442 AC532 AC552 AC582 AC642 AC852 AD042 AD092 AD112 AD252 AD352 AD412 AD512 AD622 AD632 AD642 AD662 CC04 CC05 CC07 CC12 DD23 DD27 DD31 4C088 AB12 AB38 AB45 AB57 AB59 AB66 BA08 MA63 NA05 ZA89 ZC20 ZC75 4C206 AA01 AA02 FA44 MA02 MA04 MA83 NA05 ZA89 ZC20 ZC75

Claims (3)

[Claims] 1. Clara, Asenyaku, Clove, Saxifraga, Hop, Rosemary, Sicon, Hypericum,
A skin external preparation for improving skin roughness, comprising one or more plant extracts selected from St. John's wort and tea as active ingredients, and tranexamic acid. 2. Clara, Asenyaku, Clove, Saxifraga, Hop, Rosemary, Sikon, Hypericum,
An external preparation for preventing aging, which comprises as an active ingredient one or more extracts of plant selected from St. John's wort and tea, and tranexamic acid as active ingredients. 3. The composition according to claim 1, wherein the amount of the plant extract is 0.00001 to 0.1% by weight as dry solids, and the amount of the tranexamic acid is 0.01 to 10.0% by weight. The topical skin preparation according to the above.