JPH0262818A - Hair-tonic composition - Google Patents

Abstract

PURPOSE:To obtain a practical hair-tonic composition having improved transcutaneous absorptivity and free from defects such as skin irritation by using minoxidil in combination with glycerol dicapric acid ester, glycerol dicaprylic acid ester, etc. CONSTITUTION:The objective composition contains minoxidil and one or more compounds selected from glycerol dicapric acid ester, glycerol dicaprylic acid ester, glycerol monoisostearic acid ester, propylene glycol monoisostearic acid ester, etc. The amount of minoxidil is 0.05-5.0wt.%, preferably 0.2-2.0wt.% based on the whole composition. The composition may be compounded usually with an additive for hair-tonic (e.g., propylene glycol, glycerol, preservative, oil and disinfectant).

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an excellent hair nourishing composition that enhances transdermal absorption of minoxidil.

[Prior art] Ever since it was discovered that minoxidil has a hair-growth effect (
Although hair growth agents using minoxidil have been developed (US Pat. No. 4,139,619), the hair growth effect was not sufficient due to the low transdermal absorption rate of minoxidil.

Therefore, hair tonics containing various substances that promote the transdermal absorption of minoxidil are being considered.

[Problems to be Solved by the Invention] Some of these drugs have a relatively high transdermal absorption rate of minoxidil, but because the compound used as a minoxidil transdermal absorption promoting agent is solid at room temperature, It has disadvantages in that it makes the hair stiff when applied, and it irritates the skin, causing damage to the skin.

Having such defects means that it cannot be used as a hair nourishing agent and is not practical.

[Means for Solving the Problem] As a result of intensive research to solve the problem, the present inventors found that if minoxidil is applied to the hair in the presence of a specific ester, the above-mentioned drawbacks will not occur. They also found that the percutaneous absorption of minoxidil was significantly improved, and completed the present invention.

That is, the present invention is characterized by containing one or more esters selected from glycerin dicapric acid ester, glycerin dicaprylic acid ester, gutsselin monoisostearate, and propylene glycol monoisostearate and minoxidil. It is a hair nourishing composition.

In the present invention, the blending amount of minoxidil is 0.05 to 5.0% by weight of the total amount of the preparation, and 0.2 to 2.0% by weight.
is preferred.

The amount of these esters may be sufficient as long as it promotes transdermal absorption of minoxidil, and is 05 to 30% by weight, preferably 1 to 20% by weight, based on the total amount of the composition.

In the composition of the present invention, other substances commonly used in hair nourishing agents can be blended.

For example, moisturizing agents such as propylene glycol, glycerin, and diglycerin, solvents such as ethyl alcohol, isopropyl alcohol, and purified water, preservatives (parabens, etc.), and oils (vitamin A, vitamin B1, vitamin C1, vitamin D, and vitamin E1). Rough-in, cetyl alcohol,
squalane, onobe oil, etc.), bactericidal agents (sulfur, chlorhexidine gluconate, isopropylmethylphenol, quaternary ammonium salts, hinokitiol, etc.), surfactants (polyoxyethylene fatty acid ester, sorbitan fatty acid ester, glycerin monofatty acid ester) , polyoxyethylene hydrogenated castor oil derivatives, etc.), gelling agents (methylcellulose, hydroxypropylcellulose, carboxyvinyl polymer, etc.), pH adjusters (diisopropanolamine, etc.), antioxidants (dibutylhydroxytoluene, etc.), cooling agents agents (J2-menthol, etc.), anti-inflammatory agents (glycyrrhetinic acid, guaiazulene, etc.), peripheral vasodilators (tocopherol acetate, benzyl nicotinate, carrot extract, Jasmine japonica extract, capsicum extract, etc.), adrenocortical hormones (hydrocoach acetate, etc.) antihistamines (diphenhydramine hydrochloride, isothipendyl hydrochloride, etc.), local anesthetics (dibucaine hydrochloride, nodocaine hydrochloride, etc.), keratolytic agents (urea, salicylic acid, etc.)
, follicular hormones (17β-estradiol, estrone, etc.), progesterone (progesterone, 17α-hydroxyprogesterone acetate, etc.), anti-androgens (cibrothyrone acetate, 4-androstene-3, etc.)
-one-17β-carboxylic acid, etc.), fragrances, sequestering agents, ultraviolet absorbers, pigments, etc., may be incorporated within the range that does not impair the effects of the present invention.

The hair nourishing composition of the present invention is prepared into various types of hair nourishing agents such as lotions, milky lotions, creams, gels, aerosols, etc. according to commonly used methods (for example, methods specified in the 11th edition of the Japanese Pharmacopoeia).

[Effects of the Invention] According to the present invention, the hair growth effect of minoxidil is extremely high,
Moreover, it has become possible to provide a practical hair tonic that does not have drawbacks such as skin irritation.

Further, according to the present invention, the amount of minoxidil added can be reduced compared to the conventional amount without reducing the hair-nourishing effect of minoxidil.

[Example] Hereinafter, the present invention will be specifically explained with reference to Examples and Test Examples.

(Example 1) Ethyl alcohol 80g Propylene glycol 5g Minoxidil,
0.5 g Glycerin dicaprylic acid ester 10 g The above composition was stirred and dissolved to prepare a lotion type hair nourishing agent.

(Example 2) Minoxidil 1g Glycerin Monoisostearate Propylene Glycol Ethyl Alcohol g 0g 0g Polyoxyethylene (20) Polyoxypropylene <6) Decyl Tetradecyl Ether Hinokitiol Glycyrrhetinic Acetate Tocopherol Assembly Extract Carrot Extract! - Menthol acetate hydrocortiscine hydrochloride diphenhydramine 17β-estradiol g 0.2g 0.2g 0.2g 3.6g g 0.3g 0.0016g 0.1g O,0008g The above composition was treated in the same manner as in Example 1. A lotion-type hair nourishing agent was prepared.

(Example 3) Minoxidil 0.5g Glycerin dicapric acid ester 5g Propylene glycol 10g Ethyl alcohol
40g Polyoxyethylene (60) Hydrogenated castor oil derivative 2g Carboxyvinyl polymer diisopropanolamine 0.7g The above composition was stirred and mixed to prepare a gel type hair growth agent.

(Example A) 4g stearyl alcohol 1 vitamin E acetate 0.
2g, hinokitiol 0.1g, glycyrrhetinic acid 0.2g, glycerin monostearate 1g,
Propylene glycol monoisostearonate 5
g1 5 g of squalane, 13 g of ffl movable paraffin, 4 g of polyoxyethylene (20) sorbitan monostearate were dissolved by stirring while heating.

Minoxidil 0.5g, propylene glycol 7g, ethyl roseoxybenzoate 0.1g 1 purified water 5
9. 9 g was stirred and dissolved while heating.
The mixture was added to the solution and emulsified using a homomixer to prepare a cream-type hair tonic.

(Example 5) 2 g of polyoxyethylene sorbitan monooleate and 5 g of propylene glycol monoisostearate were mixed and dissolved.

In advance, add 10 g of propylene glycol, 10 g of ethyl alcohol, 68.5 g of purified water, and 0 minoxidil.
A solution obtained by stirring and dissolving 5 g of the above solution was added to the above solution, and the mixture was stirred and emulsified.

This was placed in an aerosol can, and 4 g of liquefied petroleum gas was charged under pressure to prepare an aerosol type hair growth agent.

(Test Example 1) Hair growth effect test of minoxidil-containing composition (1) Preparation of test sample: According to the preparation method of Example 1 above, sample 1 was prepared with the following formulation.
-9, comparative samples 1-12 and control samples 1-2 were prepared.

Minoxidyl ester Propylene Glyfur Ethyl Alcohol 0.5g (See Table 1) 5.0g (See Table 1) Table 1 *4 In the table, GDCIO means glycerin dicaprylate, GDC8 means glycerin dicaprylate, GMIS indicates glycerin monoisostearate, PGMIS indicates propylene glycol monoisostearate, MI indicates isopropyl myristate, ward indicates glycerin monolaurate, ■ indicates propylene glycol monolaurate, and LA indicates lauryl alcohol.

(2) Test animals: C3) A group of 10 strain 1 mice (male, 7 weeks old),
For each group of animals, hair was removed from a 2 cm x 3 cm area on the back using clippers and used for the test.

(3) Hair growth test: ■Test samples 1-9, comparative samples 1-12, and control samples 1-
Separate groups of test animals were assigned to each of 2, and 2 mg of the drug was applied once a day to the depilated area.

The hair color of the test animal is black, and the skin color at the hair removal area is gray, and the tone changes from gray to black as the hair grows, so the degree of blackness of the hair color is determined as follows: The degree of hair growth was evaluated by measuring as follows.

In other words, a spectrophotometer (high-speed spectrocolorimeter 0MS-120
0 type, manufactured by Murakami Color Research Institute Co., Ltd.), using LM
Test area elongation value immediately after hair removal based on a″4b14 color system,
The aM value, b8 value, and the L0 value, a0 value, and b' value of the test area 10 days and 20 days after application of the sample were measured, and the respective differences ΔL0, Δa0, and Δb0 were calculated, and DE'ab=
((ΔL')”+(ΔaM)!+(ΔbM) 1
) The color difference DE'ab value was determined from the formula 1/t, and the blackness of the hair color was expressed as the average value of the − group.

In addition, the degree of hair growth in the test area 10 and 20 days after application of the sample was visually evaluated on the following 6 scales.

Judgment criteria for visual evaluation: O: No hair growth is observed 1: Hair is growing 2: Terminal hair is fully grown 3: Terminal hair is growing at about 50% of the normal level 4: Terminal hair is normal Approximately 75% growth 5: Terminal hair is approximately 100% of normal growth 2 This result is
Shown in the table.

20 days after application of the sample, the hair in a 2 cm x 3 cm area of the test area was clipped with clippers, and its weight was measured to determine the amount of hair growth due to the sample.

The relationship between the amount of hair growth (mg) and the color difference DE'ab value obtained in the previous section (2) is shown in FIG.

From this figure, it can be seen that the two are clearly in a proportional relationship.

(Test Example 2) Skin irritation evaluation test for minoxidil-containing preparations In the hair growth test of Test Example 1, after applying the test sample, C3)1
The condition of the skin at the area where the test sample was applied in the mice was visually observed, and the skin irritation of the test sample was evaluated on the following 6 scales.

; No skin irritation±; Slight erythema +; Erythema observed; Erythema and edema observed; Erythema, edema, and small lining observed; Dog sagging observed This result is the second Shown in the table.

* - in the DE'ab value means that measurement is not possible because the skin has erythema.

[Brief explanation of the drawing]

FIG. 1 is a graph showing the relationship between the amount of hair growth and the color difference DE'ab. Figure 1 Growth amount (mg)

Claims (1)

[Claims] (1) It is characterized by containing one or more esters selected from the group consisting of glycerin dicapric acid ester, glycerin dicaprylic acid ester, glycerin monoisostearate, and propylene glycol monoisostearate and minoxidil. Hair nourishing composition.