JPS638314A - Drug for external use - Google Patents

Abstract

PURPOSE:A drug for external use, containing arbutin as an active ingredient and useful as cosmetics having improved whitening effect and quasi-drugs for external use having excellent preventing effect on liver-spot, ephelis, etc. CONSTITUTION:A drug for external use containing arbutin expressed by the formula in an amount of 0.1-1.0% for cosmetics and 0.5-2.0% for quasi-drugs. The arbutin has remarkable inhibitory action on melanization and improved preventing effect on liver-spot, ephelis, etc., and is used as an active ingredient in drugs for external use, e.g. cosmetics such as lotion, pack, milky lotion, cream, etc., or quasi-drug such as ointment, lotion, liniment, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an external preparation containing arbutin as an active ingredient.

As used herein, the term "external preparation" is used to include not only cosmetics but also quasi-drugs used for external use (ointments, lotions, liniments, emulsions, etc.). therefore,
More specifically, the present invention relates to cosmetics and stains containing arbutin as an active ingredient and having an excellent skin-whitening effect;
The present invention relates to a quasi-drug for external use that is highly effective in preventing freckles and the like.

[Prior art and problems to be solved by the invention] Arbutin used as an active ingredient of the external preparation of the present invention is a compound represented by the formula: and its molecular weight is 272.2.
It is 5. Arbutin is soluble and easily soluble in water. Traditionally, arbutin has not been used as a medicinal ingredient.

[Means for Solving the Problems] However, the present inventor has discovered that arbutin has a surprisingly remarkable melanin production inhibiting effect and is excellent in whitening the skin and preventing spots and freckles, and has developed the present invention. was completed.

[Effects and Examples] As mentioned above, the arbutin of the present invention exhibits a remarkable melanin production inhibiting effect, but the mechanism of action responsible for this has not yet been fully elucidated.

Culturing the melanin production suppressing effect of arbutin of the present invention 13
The study was conducted using 16 mouse melanoma cells. 136.1251111 g of arbutin was heated and dissolved in 10 ml of water to obtain a 50 mM solution. Furthermore, this solution was diluted 10 times to obtain a 5+nM solution. Add these solutions to 10 ml of Eagle's MEM medium containing 1,096 ml of 0 to 0
．． 05ml was added. Addition concentration of arbutin to 0.01
．． When the melanin production inhibitory effect was investigated at 0.05.0, 1.0.3 and 05mM, 001-0.5+
Suppression of melanin production was observed at a concentration of nM.

The external preparation of the present invention can be used in the form of general cosmetics such as lotions, bags, milky lotions, and creams, as well as in the form of externally applied quasi-drugs such as softeners, lotions, liniments, and emulsions. used.

The external preparation of the present invention contains arbutin as an active ingredient at 0.00% in the case of cosmetics. O1-3,0%, preferably 0,1-10
%, in the case of quasi-drugs, 0.01 to 3.0%, preferably 0.5 to 2.0%.

Next, the present invention will be explained in more detail using examples and adhesive examples, but the present invention is not limited to these.

Example 1 0-Sion 1 Polyoxyethylene hardened Himanura (60E, O,)
1.0g 2 Flavoring
Trace amount 3 ethanol lo
, 0g4 Paraoxybenteroic acid ester O, 1g5
Dipotassium glycyrrhizinate 0.1g6 Sorbitol solution (70%) 3.0g 7 Concentrated glycerin 3.0g8 Arbutin 0.3g9 Purified water
A total amount of 100 g of the components 1 to 9 was uniformly stirred and dissolved to prepare 100 g of lotion.

Example 2 Bag 1 Polyvinyl alcohol 12.0g2 Titanium oxide 4.0g3 Propylene glycol 2.0g4 Polyethylene glycol 1500 2.0g5 Ethanol
to, og6 arbutin
0.5g7 Purified water Total amount 100g Stir and mix 1 to 7 evenly and puncture 100
J was prepared.

Example 3 Emulsion 1 Polyoxyethylene sorbitan monostearate (20 fE, O,) 1.0
g2 Polyoxyethylene sorbitol tetraoleate (60E, O,) 0.5 g
3 Lipophilic glyceryl monostearate 1.0g 4 Stearic acid 0.5g5 Behenyl alcohol 0.5g6 Avocadoura 4.0g7 Glyceryl trioctanoate 40'8 Natural vitamin E
O,02g9 Roseoxybenzoic acid ester
0.2g10 xanthan gum 0.
14 gll 1.3-butylene glycol
5.0g12 ethanol
2.0g13 Arbutin 0.
5g14 fragrance trace amount 1
5 Purified water total amount 100g1-9
10.11 and 15 were dissolved by heating (Liquid B). Solution B was added to AM, stirred to emulsify, and cooled (solution C).

Add 12 to 14 to liquid C, stir and mix, cool and make an emulsion.
One batch of 100 g was produced.

Example 4 Cream 1 Polyoxyethylene sorbitan monostearate (20E, 0.) 1.0 g
2 Polyoxyethylene sorbitol tetraoleate (80E, O,) 1.5g3
Lipophilic glyceryl monostearate 1.5g 4 White beeswax 2.0g5 Paraffin 2.0g6 Stearic acid 3.0g7 Behenyl alcohol 3.0g8 Liquid paraffin
5.0g9 Almondura 1
2.0g10 natural vitamin E O
,02gll Methylpolysiloxane 0
．． 1g12 paraoxybenzoic acid ester 0.2
g13 1.3-butylene glycol 5.0
g14 ethanol 2.0g
15 Arbutin t, ogI
6 Fragrance trace amount 17
Dissolve the entire amount of purified water by heating ions 1 to 12 (solution A), and separately add 13 and 17.
H dissolved (Bd). Solution B was added to solution A, stirred to emulsify, and cooled (solution C). 14 to 16 were added to Solution C, stirred and mixed, and cooled to prepare 100 g of cream.

Example 5 Ointment 1 Polyoxyethylene sorbitan monostearate (20E, O,) 1.0 g
2 Polyoxyethylene sorbitol tetraoleate (40E, O,) 1.5g
3 Self-emulsifying glyceryl monostearate 1.5g 4 White beeswax 2.0g5 Paraffin 3.0d6 Stearic acid 3.0g7 Behenyl alcohol 3.0g8 Liquid paraffin
5.0g9 Glyceryl trioctanoate
20.0g10 Paraoxybenzoic acid ester 0
．． 2g11 Glycerin 5.0
g12 Sodium hydroxide 0.02
g13 Ethanol 2.0g
14 Arbutin 1.0g1
5 Purified water total amount 100g1-1
0 was dissolved by heating (solution A), and separately, 11.12 and 15 were dissolved by heating (B?&). Solution B was added to solution A, stirred to emulsify, and cooled (solution C).

13 and 14 were added to Solution C, stirred and mixed, and cooled to prepare 100 g of ointment.

Example 6 0-silica agent 1 Polyoxyethylene hardened castor ura (60E, O,)
1.0g 2 ethanol ts, og3
Paraoxybenzoic acid ester O,1sr4 Citric acid 0.1g5 Sodium citrate 03g61.3-Butylene glycol 4,0g7 Arbutin
0.5g8 Purified water Total amount 100g Stir and dissolve 1 to 8 uniformly to make lotion 10
0g was prepared.

Example 7 Liniment agent 1 Tragacanth 5.0g2 Glycerin IO,0g3 Ethanol 1O10□4 Arbutin
0.3g5 Purified water
A total of 100 g of liniment agents 1 to 5 were uniformly stirred and mixed to prepare 100 g of liniment agent.

Example 8 Emulsion 1 Polyoxyethylene sorbitan monostearate (201E, O,) 1.0
g2 Tetra, polyoxyethylene sorbitol oleate (40 [E, O,) 0, 5
g3 Lipophilic glyceryl monostearate 1.0g 4 Stearic acid 0.5g5 Behenyl alcohol 0.5g6 Liquid paraffin 4.0g7 Glyceryl trioctanoate 4.0g8 Cetyl octoate
2,0g9 Paraoxybenzoic acid ester 0,2g10 Carboxyvinyl polymer
0.05 gll 1.3-butylene glycol
5,0g12 Sodium hydroxide
0.025g13 ethanol
2.0g [4 Arbutin 0
．． 8g15 Purified water Total amount 100
Dissolve g1-9 by heating (A solution), and separately 10-1
2 and 15 were dissolved by heating (solution B). Solution B was added to solution A, stirred to emulsify, and cooled (solution C).

13 and 14 were added to Solution C, stirred and mixed, and cooled to prepare 100 g of emulsion.

Example 9 For each of the cosmetics obtained in Examples 1 to 4, 60 randomly selected men and women (20 men, 40 women, age 20
Participants (approximately uniformly distributed between the ages of 50 to 50) used the product for 3 months and completed a questionnaire regarding safety and efficacy. The results are shown in Table 1.

[Left below: Example 10 For each of the external quasi-drugs obtained in Examples 5 to 8, 50 randomly selected men and women (20 men, 30 women, aged between 20 and 50 years old) were tested. (extracted almost uniformly) were used for 3 months, and a questionnaire regarding safety and efficacy was conducted.The results are shown in Table 2.

[From the results in Tables 1 and 2 below, the external preparation of the present invention hardly causes skin irritation or skin rash, and can be used safely. It can be seen that the effect is also excellent.

Reference Example A patch test of arbutin of the present invention was conducted on 50 healthy adults (20 men, 30 women) aged 20 to 59 under the following conditions.

Test drug.

Arbutin 2% aqueous solution control (physiological saline) Application time: 48 hours Application site: Inner upper arm skin Patch: Patch test bandage (manufactured by Taisho Pharmaceutical Co., Ltd.) As a result of the evaluation 48 hours after application, arbutin was As with the control, none showed a positive reaction.

[Effects of the Invention] The external preparation of the present invention can be safely used without causing skin irritation or skin rash, and has excellent effects of whitening the skin and preventing spots and freckles.

Claims (1)

[Claims] 1. An external preparation containing arbutin as an active ingredient.