JPH0242009A - External preparation - Google Patents

Abstract

PURPOSE:To obtain an external preparation preventing stain, freckle, etc., exhibiting excellent fair-complexioned effects comprising rottlerin, a component of kamala of gland seta and bundle fiber, occurring in epidermis of fruit of Mallotus philoppinwnaia Muller Argoviensis as an active ingredient. CONSTITUTION:A cosmetic such as cream, toilet lotion or pack and a quasi-drug such as emulsion, lotion or liniment containing 1-0.01wt.% rottlerin shown by the formula obtained by extraction and purification from kamala. Cream, ointment, milky lotion, etc., are prepared by adding rottlerin to an oil phase part and blending the oil phase part with a water phase part. The external preparation is safely usable without causing disorder such as rash of skin.

Description

[Detailed Description of the Invention] [Field of Industrial Application] The present invention uses rottlerin, a component of Kamala, as an active ingredient to prevent various skin phenomena caused by melanin production such as spots and freckles, and has an excellent skin whitening effect. This topic relates to external preparations.

[Conventional technology]

Conventionally, kojic acid and kojic acid derivatives are known as substances that suppress melanin production. Furthermore, skin fairing cosmetics containing these substances as active ingredients were also produced, for example, in
No. 8569, JP-A-56-7710, JP-A No. 56-77
Various disclosures are made in No. 76, No. 56-79616, and the like. Flavonol compounds are also known. For example, cosmetics and skin liniments containing quercetin as an active ingredient include JP-A-55-92305 and JP-A-57-14.
As disclosed in Japanese Patent Publication No. 517 and containing quercetin fatty acid ester as an active ingredient, Japanese Patent Publication No. 58-3447
7, which contains myricetin, fisetin, gutiscetin, rhamnetin, etc. as active ingredients, include JP-A-55-111411 and JP-A-57-35506.
It is disclosed in the publication No. In addition, as an active ingredient of 3-hydroxychromone compound, there is
-111410 and No. 55-143908, respectively.

[Problem to be solved by the invention]

The object of the present invention is to provide a new external preparation that has a safe and effective melanin production inhibiting effect.

[Means to solve the problem]

The present inventor conducted a wide search for new melanin production inhibitors,
After repeated research, the present inventor discovered Kamala tincture (Japanese Patent Application Laid-Open No. 63-291
The present invention was completed based on the discovery that rottlerin, a component of the product (see Publication No. 3), has an excellent melanin production inhibiting effect.

The present invention is an external preparation containing rottlerin as an active ingredient.

Rottlerin of the present invention is a compound having the following structural formula.

This compound is a known substance extracted and purified from Kamala, which is the glandular hairs and bundles of hairs produced on the epidermis of the camphor tree fruit.

Kamala, the raw material, is known to have an anthelmintic effect by paralyzing the motor nerves and muscles of the insect body, and also to have a cathartic effect.

The external preparations of the present invention include cosmetics such as creams, lotions, and packs, as well as quasi-drugs used for external use such as emulsions, lotions, and liniments.

The external preparation of the present invention contains rottlerin as an active ingredient, in the case of cosmetics, 5 to 0.001% (by weight), preferably 1% (by weight).
~0.01% (weight), 10-0 for quasi-drugs
．． 001% (by weight), preferably 1-0.01% (by weight)
)contains.

When formulating into external preparations, creams or ointments, hydrophilic ingredients such as humectants such as glycerin and sorbitol are added to purified water to form the aqueous phase, and the oil phase consists of beeswax, paraffin, microcrystalline wax, etc. Oil components such as preservatives and surfactants are added to solid oils such as ceresin, higher fatty acids, and hydrogenated oils, semi-solid oils such as vaseline, lanolin, and glycerides, and liquid oils such as cuqualane, liquid paraffin, and various ester oils. Prepare.

A general cream or ointment is prepared by heating the aqueous phase obtained in this way and gradually adding the oil phase heated to the same temperature while stirring gently to emulsify it. During production, the active ingredient rottlerin is added to the oil phase to form a cream or ointment.

In the case of emulsions, humectants such as glycerin, acidic or alkaline pH adjusters, etc. are added to purified water, heated and mixed, ethanol is added to form the aqueous phase, and solid oils such as beeswax and paraffin, semi-containing substances such as vaseline and lanolin are added. Oily components such as preservatives and surfactants are added to liquid oils such as solid oils, squalane, liquid paraffin, and various ester oils, mixed and heated to form an oil phase, and the oil phase is added to the aqueous phase to form a reserve. In the production of general emulsions, in which emulsification is performed, a protective colloid such as carboxyvinyl polymer or carboxymethyl cellulose is added to the emulsion, and the emulsion is homogeneously emulsified using a homomixer, rottlerin, an active ingredient, is added to the oil phase. Make it into an emulsion.

For puncture agents, moisturizers such as glycerin, film agents such as polyvinyl alcohol, and vegum are added to purified water to swell it, and if necessary, powders such as kaolin, talc, and zinc oxide are added to add fragrance and preservatives. In the production of general packs, which involve adding ethanol in which ingredients have been dissolved and kneading the mixture until it becomes a paste, rottlerin, an active ingredient, is added to form a pack.

Next, examples of the present invention will be described.

〔Example〕

Example 1 Cream loftrelin 0.1% polyoxyethylene stearyl ether 2.0% polyoxyethylene cetyl ether 2.0% beeswax 6.0% cetanol 6.0% isoprobyl palmitate) 10.0% liquid paraffin 30
．． 0% polyethylene glycol monostearate 1.0
% Methyl roseoxybenzoate 0.2% Make the total volume to 100 with purified water.

Example 2 Emulsion Rottlerin 0.01% Self-emulsifying glycerol monostearate 0.5% Polyoxyethylene cedyl ether 2.0% MC stearic acid 2.0% Cetanol
1.5% isopropyl myristate)
10.0% Methyl roseoxybenzoate 0.
2% fragrance Make the total volume to 100% with a small amount of purified water.

Example 3 Backing agent Rottlerin 1.0% Methyl paraoxybenzoate 0.08% Carboxyvinyl polymer 1.0% Calcium carbonate 0
．． 6% titanium dioxide 0.02% fragrance A small amount of purified water makes the total amount 10%
(Let it be l.

Note that % in this example is % by weight.

The melanin production inhibiting effect of losotorelin, the active ingredient of the present invention, will be clarified by the following test.

Test Example Melanin production test of Bi6 cells 4 x 10' mouse melanoma-derived B16 cells were
Suspended in Eagle Mε;4 medium containing 10 ml of % tallow serum and cultured at 37°C in the presence of 5% CO2 in a 25 cm” culture bottle. !J/ 1 jI!, 0.50 μ
M/1β, 1.0 μ: Replace with medium containing A/1β and culture for 5 days. Cells were washed with phosphate buffer (pH 7.2) containing 0.8 W/V saline, then trypsinized and BD
Cells were harvested by detachment using a TA-containing solution and filtration. The reflected light intensity (blackness) at 500 nm of the cells collected on the filter paper was determined using a densitometer.

The test results were as shown in Table 1 below.

Table 1: No change +: Slightly thin ++: Clearly thin +10: Very thin As a result, whitening of cells was observed depending on the concentration of rottlerin added.

〔Effect of the invention〕

The topical preparation of the present invention can be safely used without causing any problems such as rough skin or skin rash, and has a whitening effect on the skin, preventing spots and
This is an extremely useful invention that has the effect of preventing freckles and the like.

Claims (1)

[Claims] 1. An external preparation characterized by containing rottlerin as an active ingredient.