JP2610310B2 - External preparation - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention prevents the various phenomena of the skin due to the production of melanin such as spots and freckles, and has an excellent fairness effect, using rotrelin, a component of Kamala, as an active ingredient. It relates to an external preparation.

[Conventional technology]

Conventionally, kojic acid and kojic acid derivatives are known as substances that suppress melanin production. In addition, fair-skin cosmetics containing these substances as active ingredients are also disclosed in, for example, JP-B-56-18-18.
No. 569, JP-A-56-7710, JP-A-56-7776, and JP-A-56-779616.
Various publications. Also, flavonol compounds are known. For example, cosmetics and skin coatings containing quercetin as an active ingredient are disclosed in JP-A-55-9230.
Nos. 5 and 145-1517, which contain quercetin fatty acid ester as an active ingredient.
Japanese Patent Application Laid-Open Nos. Sho 55-111411 and 57-35506 disclose the active ingredients containing myricetin, fisetin, gutiscetin, and ramnetin as active ingredients. Further, as a compound containing a 3-hydroxychromone compound as an active ingredient, JP-A-55-111410,
No. 55-143908.

[Problems to be solved by the invention]

An object of the present invention is to provide a new external preparation having a safe and effective melanin production inhibitory effect.

[Means for Solving the Problems] The present inventors have conducted extensive searches and studies on new melanin production inhibiting substances, and found that the present inventors have found that Kamala tincture previously found as a melanin production inhibiting substance (Japanese Patent Application Laid-Open No. 2913
The present invention was completed by finding out that rottlerin, which is a component of the invention, has an excellent melanin production inhibitory action.

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

Rotrelin 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 glandular hair and bristles generated on the epidermis of the fruit of Kusunohagashiwa.

It is known that Kamala, a raw material, exerts an anthelmintic effect by paralyzing the motor nerves and muscles of the insect body and has a purgative effect.

The external preparation of the present invention is used to include quasi-drugs used externally, such as emulsions, lotions, and liniments, in addition to cosmetics such as creams, lotions, and packs.

The external preparation of the present invention comprises the active ingredient lotrelin,
5 to 0.001% (weight) for cosmetics, preferably 1 to
0.01% (weight), 10% to 0.001% for quasi-drugs
(Weight), preferably 1 to 0.01% (weight).

When formulated into an external preparation, in a cream or ointment, a hydrophilic component, for example, a humectant such as glycerin or sorbite is added to purified water to form an aqueous phase, and the oil phase is beeswax, paraffin, microcrystalline wax, or the like. Ceresin, higher fatty acids, solid oils such as hydrogenated oil, vaseline,
It is prepared by adding oil components such as preservatives and surfactants to semi-solid oils such as lanolin and glyceride, and liquid oils such as kuqualane, liquid paraffin and various ester oils. Warm the aqueous phase thus obtained, gradually add the oil phase heated to the same temperature while gently stirring and emulsify to give a cream or ointment of a general cream or ointment. In the production, a lotterin, which is an active ingredient, is added to the oil phase to prepare a cream or ointment.

In emulsions, humectants such as glycerin in purified water,
Add an acid or alkali pH adjuster, mix by heating, add ethanol to make the aqueous phase, solid oil such as beeswax and paraffin, semi-solid oil such as petrolatum and lanolin, squalane, liquid paraffin, various ester oils, etc. Oil components such as preservatives and surfactants are added to the liquid oil component, mixed and heated to form an oil phase, and the oil phase is added to the aqueous phase to perform pre-emulsification, and then carboxyvinyl polymer and carboxymethyl cellulose are added. In the production of a general emulsion in which a protective colloid agent such as the above is added, and the emulsion is uniformly emulsified with a homomixer to obtain an emulsion, an active ingredient rotrelin is added to the oil phase to form an emulsion.

In the case of a pack, a humectant such as glycerin and a film agent such as polyvinyl alcohol and veegum are added to purified water to swell, and if necessary, a powder such as kaolin, talc, zinc oxide or the like is added, and a fragrance, preservative, etc. In the production of a general pack preparation which is prepared by adding ethanol in which a preparation and the like are dissolved and kneading until a paste is formed, lotrelin as an active ingredient is added to make a pack preparation.

 Next, examples of the present invention will be described.

〔Example〕

 Example 1 Cream Rotrelin 0.1% Polyoxyethylene stearyl ether 2.0% Polyoxyethylene cetyl ether 2.0% Beeswax 6.0% Cetanol 6.0% Isopropyl palmitate 10.0% Liquid paraffin 30.0% Polyethylene glycol monostearate 1.0% Methyl paraoxybenzoate 0.2% Purified water To make the total amount 100.

Example 2 Emulsion Lotrelin 0.01% Self-emulsifying geriserol monostearate 0.5% Polyoxyethylene cetyl ether 2.0% MC stearic acid 2.0% Cetanol 1.5% Isopropyl myristate 10.0% Methyl parahydroxybenzoate 0.2% Fragrance Trace amount Purified water 100% And

Example 3 Packing agent Lotrelin 1.0% Methyl parahydroxybenzoate 0.08% Carboxyvinyl polymer 1.0% Calcium carbonate 0.6% Titanium dioxide 0.02% Fragrance Trace amount Make the total amount 100 with purified water.

 Incidentally,% in this example is% by weight.

The melanin production inhibitory effect of rotrelin, an active ingredient of the present invention, will be clarified by the following test.

Test Example Melanin production test of B16 cells 4 × 10 ⁴ B16 cells derived from mouse melanoma were suspended in Eagle's MEM medium containing 10 ml of 10% fetal bovine serum, and the suspension was placed in a 25 cm ² culture flask in the presence of 5% CO ₂ 37 Incubate at ° C. On day 0 and day 3, lotrelin was added at 0.25 μM / 1,0.50 μm, respectively.
Replace with a medium containing M / 1, 1.0 μM / 1 and culture for 5 days.
The cells were washed with a phosphate buffer (pH 7.2) containing 0.8 W / V saline, then detached using a solution containing trypsin and EDTA, and the cells were collected by filtration. The reflected light intensity (blackness) at 500 nm of the cells collected on the filter paper was determined by a densitometer.

For comparison, a test using Kamala tincture disclosed as a prior art in the specification of the present application was also performed.

As a test sample, 100 ml of Kamala tincture (extracted with 10% ethanol) was concentrated under reduced pressure by an evaporator to obtain 2.51 g of a dried product, and the dried product was prepared as a sample in the same manner as Rottlerin and subjected to the same test.

 The test results were as shown in Table 1 below.

-: No change +: Slightly thin ++: Clearly thin ++
+: Very thin As a result, whitening of cells was observed depending on the concentration of lotrelin.

〔The invention's effect〕

The external preparation of the present invention is an extremely useful invention which can be used safely without causing skin roughness, skin irritation and the like, and has an effect of preventing skin whitening, spots, freckles and the like.

Claims (1)

(57) [Claims] An external preparation comprising rotrelin as an active ingredient.