JPS61271215A - Dermal external drug - Google Patents

Abstract

PURPOSE:A dermal external drug, containing methylhydroquinone and capable of exhibiting more remarkably improved skin beautifying and whitening effect than hydroquinone. CONSTITUTION:A dermal external drug containing methylhydroquinone expressed by the formula. The compound expressed by the formula is a compound obtained by substituting one of the hydrogen atoms in the parent nucleus of the hydroquinone by methyl group, but exhibits more remarkably improved beautifying and whitening effect than the hydroquinone. The amount of the compound expressed by the formula to be incorporated is preferably 0.1-5wt%. An oil, humectant agent, surfactant, etc, may be optionally incorporated in addition to the essential component expressed by the formula. The addition of an ultraviolet light absorber or well-known beautifying and whitening agent is further effective for preventing and treating liver spot, ephelis, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a skin preparation for external use that has significantly improved skin whitening effects.

[Conventional technology] Although there are some points that are unclear about the mechanism by which skin spots occur, in general, melanin pigments are formed due to hormonal abnormalities or stimulation of ultraviolet rays from sunlight, and this is caused by the formation of melanin within the skin. It is thought that it is abnormally deposited. Treatments for such bruises include the administration of large amounts of substances that suppress melanin production, such as large doses of vitamin C, injections of glutathione, or the use of ointments, creams, and lotions containing L-ascorbic acid, cysteine, etc. Methods such as making it into a form and applying it locally are used. Additionally, hydroquinone preparations are used as pharmaceuticals in Europe and America.

[Problems to be Solved by the Invention] Thiol compounds such as L-ascorbic acids, glutathione, and cysteine have an extremely slow onset of their effects, and therefore do not have sufficient whitening effects. On the other hand, although the effects of hydroquinone have been recognized to some extent, they are not necessarily satisfactory.

Means for Solving Problem E] In view of the above circumstances, the present inventors have conducted extensive research and found that methylhydroquinone is a compound in which one of the hydrogen atoms in the mother nucleus of hydroquinone is replaced with a methyl group. The present invention was completed after recognizing that it exhibits a remarkable skin whitening effect compared to hydroquinone.

That is, the present invention is an external skin preparation characterized by containing methylhydroquinone.

The skin external preparation of the present invention can exhibit a remarkable whitening effect compared to existing skin external preparations containing hydroquinone or the like.

Hereinafter, the configuration of the present invention will be explained in detail.

The compound used in the present invention is methylhydroquinone represented by the formula (1), and this compound is contained in the extract of Ichiyakusou (Staghorn grass), which is a plant of the Sectaceae family. It is also generally commercially available as a reagent. Although a whitening effect can be expected from the extract of Ichiyakuso, it is preferable to use methylhydroquinone alone. In addition, the blending amount is 0.01 to 10 in the total amount of the skin external preparation.
% by weight, preferably 0.1-5% by weight. 0.05
If it is less than 101% by weight, the whitening effect will be poor. Even if it is blended in excess of this amount, no increase in effectiveness can be expected.

0 The external skin preparation of the Japanese invention can be in the form of cream, milky lotion, lotion 1, bag, jelly, soap, ointment, etc. In addition to the above-mentioned essential ingredients, the skin external preparation of the present invention contains:
Add oil, moisturizer, surfactant, pigment, fragrance, as needed.
Water, alcohol, thickeners, preservatives, antioxidants, chelating agents, skin nutrients, hair nutrients, enzymes, etc. are blended.

In addition, for the prevention and treatment of spots, freckles, etc., it is even more effective to add an ultraviolet absorber or a known whitening agent. Typical examples of ultraviolet absorbers include N, a benzoic acid-based ultraviolet absorber;

N-dimethyl PABA amyl ester, N,N-dimethyl PABA octyl ester, salicylic acid type UV absorber, homomenthyl salicylate, cinnamic acid type UV absorber, isopropyl-p-methoxycinnamate, octyl methoxycinnamate, 2- Ethoxyethyl-p-cinnamate, as a benzophenone ultraviolet absorber, 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxybenzophenone-5-
Sulfonates, other ultraviolet absorbers include urocanic acid, 2-(2°-hydroxy-5'-methyl-phenyl)benzotriazole, 4-methoxy-4°-t-
Examples include butyl-dibenzoylmethane. or,
Examples of known skin whitening agents include L-ascorbic acid, L-
Ascorbic acid monostearate, L-ascorbic acid monopalmitate, L-ascorbic acid monooleate,
L-alcorbic acid monophosphate, L-ascorbic acid 2-sulfuric acid, L-ascorbic acid dipalmitate, L-ascorbic acid dioleate, human placenta extract, animal placenta extract, cysteine, glutathione, hydroquinone, kojic acid, etc. It will be done.

The amount of ultraviolet absorber and known whitening agent is 0.
．． Approximately 0.05 to 10% by weight is appropriate.

[Effects of the Invention] Next, in order to clarify the whitening effect of methylhydroquinone used in the present invention, a practical use test was conducted on a neutral cream containing methylhydroquinone.

(Test method) Subject 3 with post-inflammatory hyperpigmentation and melasma on the face
0 people served as a panel - 10 of them received the neutral cream of Example 2, the other 10 received the formulation from Example 2 (comparative example) described later, and the remaining 1
Subject 0 used the product of Example 2 in which methylhydroquinone was replaced with hydroquinone once a day for 8 weeks on the face, and the lightening effect was visually judged after 8 weeks of use.

As is clear from the above results, it is clear that the neutral cream containing 2% by weight of methylhydroquinone exhibits a remarkable improvement effect compared to the comparative example and the neutral cream containing 2% by weight of hydroquinone.

[Example] Next, the present invention will be explained in detail with reference to Examples. The present invention is not limited thereby. The blending amount is in weight%.

Example 1 Vanishing cream Stearic acid 5.0 Stearyl alcohol 4.0 Stearic acid butyl alcohol ester 8.0 Glycerin monostearate 2°O methylhydroquinone 1.0 Propylene glycol 10.0 Caustic potash 0.2 Preservative/antioxidant Agent Appropriate amount fragrance
Appropriate amount of ion exchange water
Residue (manufacturing method) Add propylene glycol and caustic potash to ion-exchanged water, dissolve, heat, and keep at 70°C (water phase). Mix other ingredients, heat and melt and keep at 70°C (oil phase). Gradually add the oil phase to the water phase, and after all addition is complete, maintain the temperature for a while to allow the reaction to occur. Then, emulsify the mixture uniformly using a homomixer, and cool to 30°C while stirring well.

Example 2 Neutral Cream Stearyl Alcohol 7.0 Stearic Acid 2.0 Hydrogenated Lanolin
2.0 squalane
5.02-Octyldodecyl alcohol
6.0 Polyoxyethylene (25 moles) Cetyl alcohol ether 3.0 Glycerin monostearate 2.0 Methylhydroquinone 2.0 Propylene glycol
5.0 fragrance
Appropriate amount of preservatives/antioxidants Appropriate amount of ion-exchanged water Remainder (manufacturing method) Add propylene glycol to ion-exchanged water and heat.
Keep at 0°C (aqueous phase). Mix other ingredients and heat and melt 7.
Keep at 0°C (oil phase). The oil phase is pre-emulsified by adding the oil phase to the water phase, uniformly emulsified using a homomixer, and then cooled to 30°C while stirring well.

Example 3 Cold cream solid paraffin 5・O wax 10.0 Vaseline
15.0 Liquid paraffin
41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) Sorbitan monolaurate 2.0 Soap powder
0.1 Methylhydroquinone 0.01 Borax
0.2 ion exchange water
Residual fragrance: Appropriate amount Preservative/Antioxidant: Appropriate amount (manufacturing method) Add soap powder and borax to ion-exchanged water, heat and dissolve.
Keep at °C (aqueous phase). Mix the other ingredients and heat and melt for 70 minutes.
Keep at °C (oil phase). The oil phase is gradually added to the water phase while stirring to carry out the reaction. After the reaction is completed, the mixture is uniformly emulsified using a homomixer, and after emulsification, the mixture is cooled to 30°C while stirring well.

Example 4 Emulsion Stearic acid 2.5 Cetyl alcohol 2.0 Vaseline
5.0 liquid paraffin
10.0 Polyoxyethylene (10 mol) Monooleic acid ester 2.0 Polyethylene glycol 1500 3.0 Triethanolamine 1.0 Methylhydroquinone 1.0 Ion exchange water
residual fragrance
Appropriate amount Preservative/Antioxidant Appropriate amount (manufacturing method) Add polyethylene glycol 1500 and triethanolamine to ion-exchanged water, dissolve by heating, and keep at 70°C (water phase). Mix other ingredients, heat and melt and keep at 70°C (oil phase). The oil phase is pre-emulsified by adding the oil phase to the water phase, and the mixture is uniformly emulsified using a homomixer. After emulsification, the mixture is cooled to 30°C while stirring well.

Example 5 Lotion (alcohol phase) 95% ethyl alcohol 25.0 Polyoxyethylene (25 mol) Hardened castor oil ether 2.0 Antioxidant/preservative Appropriate amount fragrance
Adequate amount of methylhydroquinone
3.0 (aqueous phase) Glycerin 5.0 Sodium hexametaphosphate Appropriate amount UV absorber
Appropriate amount of ion exchange water
Residue (manufacturing method) Solubilize after adjusting the aqueous phase and alcohol phase.

Example 6 Jelly 95%! Chirufur:z-ru 10.0 Dipropylene glycol 15.0 Methylhydroquinone 10.0 Polyoxyethylene (15 mol) Oleyl alcohol ether 2.0 Carboxy vinyl polymer (Product name: Carboball 941) 1.0 Caustic soda 0.15L -Arginine 0.1 UV absorber
Appropriate amount of fragrance
Appropriate amount of preservatives.

Ion-exchanged water Residual (manufacturing method) Uniformly dissolve Carboball 941 in ion-exchanged water, and then dissolve dipropylene glycol, polyoxyethylene (15 mol), oleyl alcohol ether, and other components in 95% ethanol, and add to the aqueous phase. Added. Then, it is neutralized and thickened with caustic soda and L-arginine.

Example 7 Beer-off type pack (alcohol phase) 95%! 10.0 Polyoxyethylene (15 mol) Oleyl alcohol ether 2.0 Olive oil 2.0 Methylhydroquinone 0.5 Preservative
Appropriate amount of fragrance
Appropriate amount (aqueous phase) Polyvinyl alcohol 12.0 Glycerin 3.0 Polyethylene glycol 1500 1.0 Ion exchange water
Residue (Method M) Prepare the aqueous phase at 80°C and cool to 50°C. The alcohol phase excluding olive oil and pre-cofermented Q10 is adjusted at room temperature and added to the aqueous phase, then olive oil in which coenzyme Q1o has been dissolved is added, mixed uniformly, and allowed to cool.

Example 8 Ointment Vaseline 40.0 Stearyl alcohol 15.0 Wood wax
15. .

POE (10), t rate 0.25 Glyceryl monostearate 0.25 Methylhydroquinone 6.0 Sorbitol
5.0 Propylene glycol
S, O ion-exchanged water Residual patent applicant Shiseido Co., Ltd. (Volunteer to write procedural amendments) February 1, 1986? (''

Claims (1)

[Claims] A skin external preparation characterized by containing methylhydroquinone.