JPH09175950A - Composition containing carpronium chloride - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for hair, comprising carpronium chloride, pantothenyl ethyl ether and a water-soluble chitin derivative, reduced in stickiness after use and capable of raising the stability of carpronium chloride to water. SOLUTION: This composition coptaining carpronium chloride comprises the carpronium chloride having local vasodilator actions and pantothenyl ethyl ether and a water-soluble chitin derivative having stabilizing actions on the carpronium chloride and hair root activating actions (e.g. hydroxypropyl chitosan). Furthermore, one more crude drugs having hair growth, trichogenous or hair tonic effects (e.g. Polygoni multiflori Radix or Panacis japonici Rhizoma) are contained therein. The carpronium chloride is used in an amount of 0.1-10wt.% and other ingredients are blended in the following amounts based on 1 pt.wt. carpronium chloride: (1/20) to 20 pts.wt. pantothenyl ethyl ether, (1/100) to (1/5) pt.wt. water-soluble chitin derivative and (1/5) to 20 pts.wt. crude drugs. The composition is the one for hair growth, trichogenous and hair tonic use and effective against alopecia, dandruff, pruritus, hair production insufficiency, baldness, etc.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a composition containing carpronium chloride.

[0002]

2. Description of the Related Art Carpronium chloride is a compound having a local vasodilatory action and is known as an active ingredient of a hair growth stimulant (see Japanese Patent Publication No. 42-5680).

At present, when carpronium chloride is used as a hair growth stimulant, it is used as a liquid preparation for external use, and an aqueous alcohol solution is used as a solvent for the liquid preparation. Ethanol is often used as the alcohol for such liquid preparations. This is because ethanol has (1) Volatility, so it takes away the heat of evaporation and gives the skin a refreshing feeling.
This is due to the effects of (2) dissolving the components to be blended well, and (3) promoting the drying of wet hair.

However, due to the effect of the aqueous alcohol solution, the liquid may cause a decrease in water content of the scalp, which may cause abnormalities in the scalp. In order to improve these, a moisturizing agent (also referred to as a wetting agent) such as a polyhydric alcohol such as glycerin or a natural moisturizing component such as sodium pyrrolidonecarboxylate is added. However, when the humidity is high, such as in summer, the inclusion of these moisturizers absorbs moisture in the atmosphere and causes stickiness.

Therefore, if the amount of the moisturizing agent is reduced to eliminate stickiness, moisture in the skin may be released in the case of low humidity such as in winter, which causes the skin to dry.

Further, carpronium chloride is easily hydrolyzed and is unstable to water. Although pharmaceutical products need to guarantee quality for a long period of time, it is very difficult to maintain the content rate of carpronium chloride in products for products that have passed a long time since they were manufactured due to the instability of carpronium chloride. Have difficulty.

Therefore, the pH is adjusted in order to suppress the hydrolysis of the compound, but it is often insufficient for long-term storage. In order to solve this problem, it has been proposed to add pantotenyl ethyl ether to an aqueous solution of carpronium chloride (see JP-A-51-143616), but this is not always satisfactory.

[0008]

DISCLOSURE OF INVENTION Problems to be Solved by the Invention The present inventors have conducted extensive studies to solve the above-mentioned problems of stickiness after use and unstable properties of carpronium chloride in water.

[0009]

As a result, the above problems can be solved by further adding a water-soluble chitin derivative to an aqueous solution of carpronium chloride and pantotenyl ethyl ether, and further stabilization of pantotenyl ethyl ether can be achieved. The present invention has been completed by discovering that the above can be achieved.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION The present invention includes the following inventions (A) to
(P). (A) a composition containing carpronium chloride, pantotenyl ethyl ether and a water-soluble chitin derivative,

(B) A composition containing one or more herbal medicines, carpronium chloride, pantotenyl ethyl ether and a water-soluble chitin derivative,

(C) Assemblies, cashews, ginseng carrots, salamanders, ginseng, ginger, sardines, sardines,
Cloves, Kaiso, Ivy, Manner wax,
A composition containing one or more crude drugs selected from the group consisting of burdock and Dutch pepper, carpronium chloride, pantotenyl ethyl ether and a water-soluble chitin derivative,

(D) The composition according to the above (B) or (C), wherein the crude drugs are cashews and ginseng ginseng.

(E) The composition according to any one of (A) to (D) above, wherein the water-soluble chitin derivative is polyoxyalkylene chitosan.

(F) The composition according to any one of (A) to (E) above, wherein the water-soluble chitin derivative is hydroxypropyl chitosan.

(G) A composition containing cashew, ginseng ginseng, carpronium chloride, pantotenyl ethyl ether and hydroxypropyl chitosan,

(H) A composition containing a tincture of cashew, a tincture of ginseng, carpronium chloride, pantotenyl ethyl ether and hydroxypropyl chitosan,

(I) Carpronium chloride is 0.1 to 1
The composition according to any one of (A) to (H) above, which has a concentration of 0% by weight.

(J) Carpronium chloride is 0.5 to 5
The composition according to any one of (A) to (H) above, which is a concentration of wt%,

(K) Cashew 1/5 to 20 parts by weight,
Chixetun ginseng 1/5 to 20 parts by weight, carpronium chloride 1 part by weight, pantotenyl ethyl ether 1
/ 20 to 20 parts by weight and hydroxypropyl chitosan 1/100 to 1/5 parts by weight,

(L) 1-10 parts by weight of cashew, 1-10 parts by weight of ginseng carrot, carpronium chloride
1 part by weight, pantotenyl ethyl ether 1/5 to 5
Parts by weight and hydroxypropyl chitosan 1/50 ~
A composition containing 1/10 parts by weight,

(M) A composition containing 1 part by weight of cashew, 1 part by weight of ginseng carrot, 1 part by weight of carpronium chloride, 1 part by weight of pantotenyl ethyl ether and 1/25 part by weight of hydroxypropyl chitosan,

(N) A lotion containing 1% by weight of cashew, 1% by weight of ginseng carrot, 1% by weight of carpronium chloride, 1% by weight of pantotenyl ethyl ether and 0.04% by weight of hydroxypropyl chitosan,

(O) The composition according to any one of (A) to (M) above for hair, or (N) above.
Lotion described in, and

(P) The composition according to any one of (A) to (M) or the lotion according to (N), which is used for hair growth, promotion of hair growth or hair growth.

The following are the components of the composition of the present invention: carpronium chloride, pantotenyl ethyl ether,
The water-soluble chitin derivative and crude drugs will be described.

Carpronium chloride used in the present invention is a compound having a local vasodilatory action and represented by the following structural formula.

[0028]

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The pantotenyl ethyl ether used in the present invention is a compound having not only the stabilizing action of carpronium chloride but also the activating action of hair roots and represented by the following structural formula.

[0030]

[Chemical Formula 2] HOCH ₂ C (CH ₃ ) ₂ CHOHCONHCH ₂ CH ₂ CH ₂ OC ₂ H ₅

The water-soluble chitin derivative used in the present invention is a water-soluble derivative obtained by chemically modifying poorly water-soluble chitin or chitosan. More specifically, a hydrophilic group is introduced into chitin or chitosan. It is a water-soluble derivative. Specific examples of this include the following.

(1) Polyoxyalkylene chitin or polyoxyalkylene chitosan

[0033]

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[In the formula, a represents a number exceeding ^1, and R ¹ and R ² are the same or different and each is a hydrogen atom, -C
OCH ₃ or _{- (EO) p1 - (PO} ) q1 - (B
O) _r1- H, R ³ is a hydrogen atom _or- (EO) <sub>p2
- (PO) q2 - (BO</sub> ) to r2 -H, ^{R 4} is a hydrogen atom or a _{- (EO) p3 - (PO} ) q3 - (BO) r3 -
Indicates H (where p1, q1, r1, p2, q2, r
2, p3, q3 and r3 are the same or different and each represents a number of 0-5. However, p1 + q1 + r1 ≠
0, p2 + q2 + r2 ≠ 0, p3 + q3 + r3 ≠ 0. Further, EO means an oxyethylene chain, PO means an oxypropylene chain, and BO means an oxybutylene chain).
However, EO and P in R ¹ , R ² , R ³ and R ⁴
The order of bonding O and BO does not matter. ]

(2) Carboxymethyl chitin or carboxymethyl chitosan

[0036]

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[In the formula, b represents a number exceeding 1, R ⁵ represents a hydrogen atom or -COCH ₃ , and R ⁶ and R ⁷ are the same or different, and each represents a hydrogen atom, -CH ₂ COOH,
Shows a -CH ₂ COONH ₄ ⁺ or _-CH 2 COOM (M denotes an alkali metal). However, R ⁶ and R ⁷ are not hydrogen atoms at the same time. ]

(3) Phosphorylated chitin or phosphorylated chitosan

[0039]

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[0040]

[Chemical 6]

(4) Sulfated chitin or sulfated chitosan

[0042]

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[0043]

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(5) Dihydroxypropyl chitin or dihydroxypropyl chitosan

[0045]

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[Wherein f represents a number exceeding 1 and R ¹⁶
Is a hydrogen atom, -COCH ₃ or _-CH 2 CH (OH)
CH ₂ OH, R ¹⁷ and R ¹⁸ are the same or different and each is a hydrogen atom or —CH ₂ CH (OH) CH ₂
Indicates OH. However, R ¹⁷ and R ¹⁸ are not hydrogen atoms at the same time. ]

(6) Chitosan N-2-hydroxypropyl sulfonate

[0048]

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[0049]

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In the present invention, of these water-soluble chitin derivatives, polyoxyalkylene chitosan is preferable, and hydroxypropyl chitosan is particularly preferable. The structure of hydroxypropyl chitosan is shown below.

[0051]

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[Wherein R is a hydrogen atom or a group

[0053]

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(In the formula, m means an integer of 1 or more)
And n represents an integer of 1 or more. ]

The herbal medicines in the present invention are herbal medicines such as animals and plants themselves, parts of animals and plants, or secreted products thereof.
It means an extract of the crude drug and a mixture of the crude drug and the extract of the crude drug. The crude drug extract as used herein refers to a liquid obtained by adding an appropriate leaching agent such as water or ethanol to a crude drug or a liquid obtained by concentrating the leachate, and specific examples thereof include extracts and tinctures.

The herbal medicines used in the present invention are not particularly limited, but herbal medicines having a hair-growth, hair growth-promoting or hair-growth effect are preferable. Specific examples thereof include herbal medicines such as senburi, cashew, ginseng, salamander, ginseng, ginger, ginger, dio, clove, kaiso, ivy, mannenrow, burdock and Dutch pepper. One kind or two or more kinds can be appropriately selected from the group consisting of crude drugs. The one or more kinds of herbal medicines refers to, for example, assemblage, assemblage and cashew, assemblage and cashew extract, and assemblage, cashew and cashew extract.

In one or more kinds of herbal medicines used in the present invention, a combination of Kashi and Chixetuni ginseng is preferable. Particularly preferred is the combination of an extract of Kashi and an extract of Ginseng. Among them, the combination of Kinkou tincture and Tixetin ginseng tincture is particularly preferable.

The dosage form which the composition of the present invention can take is not particularly limited as long as it is various commonly used dosage forms, but an external preparation is preferred. Specific examples thereof include creams, mousses, suspensions, emulsions, liniments, lotions and aerosols. Lotions and aerosols are particularly preferable. The composition of the present invention may be formulated by a generally known production method.

The composition of the present invention may contain humectants such as glycerin, sorbitol, propylene glycol, sodium lactate, sodium pyrrolidonecarboxylate and hyaluronic acid. In addition, surfactants, emulsifiers, thickeners, preservatives, pH adjusters, colorants, flavoring agents, bactericides,
It may further contain a cooling stimulant, an antipruritic agent, an antidandruff agent, and the like.

When the composition of the present invention is used as an external preparation, the concentration of carpronium chloride is usually preferably 0.1 to 10% by weight, particularly preferably 0.5 to 5% by weight (see Japanese Patent Publication No. 42-5680). ).

The composition ratio of the composition of the present invention is 1 part by weight of carpronium chloride.

Pantotenyl ethyl ether is 1/2
0 to 20 parts by weight is preferable, and 1/5 to 5 parts by weight is particularly preferable (see JP-A-51-143616).

The water-soluble chitin derivative is 1/100 to 1 /
5 parts by weight is preferable, and 1/50 to 1/10 parts by weight is particularly preferable.

[0064] The amount of crude drug (crude drug extract is converted to crude drug) is preferably 1/5 to 20 parts by weight.
Particularly preferred is 10 to 10 parts by weight.

The composition of the present invention is preferably used for hair, and more specifically for hair growth, hair growth promotion or hair nourishment.

In particular, the composition of the present invention has the following effects and effects: hair growth, thinning hair, promotion of hair growth, promotion of hair growth, hair loss (hair loss).
Prevention, post-disease / postpartum hair loss, dandruff, itching, hair growth, alopecia areata, hair loss, pilocytic alopecia, seborrheic alopecia, diffuse alopecia, juvenile baldness (hair loss) The elderly bald can be mentioned.

The composition of the present invention may be used by applying or spraying an appropriate amount on the site where hair grows or the site where hair grows, depending on the purpose of treatment or prevention.

Hereinafter, the present invention will be described in more detail with reference to Examples and Test Examples, but the present invention is not limited to these.

[0069]

【Example】

 1. Example 1 Lotion Agent A lotion agent having the following formulation was prepared.

Prescription Raw material name Carpronium chloride 1 g 1-menthol 0.3 g Kashi tincture 3 ml (corresponding to 1 g as cucumber) Chixetuni ginseng tincture 3 ml (corresponding to 1 g as thixetunidin) Pantothenyyl ether 1 g Concentrated glycerin 1 g Pyrrolidone carvone Sodium acid salt 1g 4% Hydroxypropyl chitosan solution 1g 95 (v / v)% ethanol 49ml Hydrochloric acid Appropriate amount Purified water Total amount 100ml

Manufacturing method Carpronium chloride, 1-menthol, tincture of tincture, tincture of ginseng, pantothenyl ethyl ether, concentrated glycerin, sodium pyrrolidonecarboxylate and 4% hydroxypropyl chitosan solution are dissolved in 95% ethanol, and then dissolved. After adding an appropriate amount of purified water and adjusting the pH to around 5 with hydrochloric acid, the total amount was 100 ml with purified water to obtain a lotion.

2. Example 2 Aerosol agent The lotion agent of Example 1 was used as a stock solution to fill 19 parts into a pressure resistant container, and then 1 part of LPG as a propellant was filled to produce an aerosol agent.

3. Comparative Example A lotion having the following formulation was prepared.

Prescription Raw material name Carpronium chloride 1 g 1-menthol 0.3 g Kashi tincture 3 ml (corresponding to 1 g as cucumber) Chixetuni ginseng tincture 3 ml (corresponding to 1 g as thixetunidin) Pantothenyyl ether 1 g Concentrated glycerin 3 g Pyrrolidone carvone Sodium acid salt 5g 95 (v / v)% ethanol 49ml Hydrochloric acid Appropriate amount Purified water Total amount 100ml

Manufacturing method Carpronium chloride, 1-menthol, tincture of tincture, tincture of ginseng tincture, pantothenyl ethyl ether, concentrated glycerin and sodium pyrrolidonecarboxylate are dissolved in 95% ethanol, and then purified water is added in an appropriate amount. After adjusting the pH to around 5 with hydrochloric acid, the total amount was 100 ml with purified water to obtain a lotion.

[0076]

[Test example]

1. Sensory Evaluation Regarding Stickiness In order to confirm the sensory evaluation regarding the stickiness of the composition of the present invention, a sensory evaluation was conducted on 20 male and female subjects by the paired comparison method. The results are shown in Table 1. Further, when this result was tested by t-test, the lotion agent of Example 1 (hereinafter sometimes abbreviated as Example L) at a 10% risk rate was a lotion agent of Comparative Example (hereinafter abbreviated as Comparative Example L). However, the lotion agent of Example 1 was less sticky.

[0077]

[Table 1]

2. Measurement of physical properties regarding stickiness Viscosity of the lotion agent of Example 1 and the lotion agent of Comparative Example (measurement method: 25 ± 1 ° C., B-type viscometer, BL adaptor, measured at 30 rpm), loss on drying (measurement method) : 105 ° C, after 3 hours, weighed to calculate volatilization rate and residual rate) and residual rate at constant temperature and constant humidity (measurement method: 30
℃, 32% RH (relative humidity) or 30 ℃, 75% RH
After being left for 1 day, the weight is weighed and calculated by the following formula. The residual rate = 100−volatilization rate) was tested. as a result,
As shown in Table 2, the lotion of Example 1 had substantially the same viscosity and residual rate as the lotion of Comparative Example, but the residual rate of loss on drying was small.

It is considered that even if the amount of the moisturizer is reduced, the moisturizing property is maintained to some extent in both low humidity (winter time) and high humidity (summer time) conditions.

[0080]

[Table 2]

3. Stability Test of Carpronium Chloride and Pantotenyl Ethyl Ether A lot amount of the lotion agent of Example 1 and a lotion agent of Comparative Example were taken, and left in a constant temperature bath at 50 ° C., 60 ° C. and 70 ° C. for a certain period of time, and then subjected to liquid chromatography. The starting% of carpronium chloride and pantotenyl ethyl ether were calculated and calculated. Table 3 shows the results.

Table 4 shows the results of stability prediction (% at the start) after 3 years at 25 ° C. using the Arrhenius equation. As is clear from Table 4, the lotion agent of Example 1 was more stable than both the lotion agents of Comparative Examples and both carpronium chloride and pantotenyl ethyl ether.

[0083]

[Table 3]

[0084]

[Table 4]

[0085]

The composition of the present invention containing a water-soluble chitin derivative eliminates stickiness as apparent from sensory evaluation and physical property measurement. In addition, not only carpronium chloride but also pantotenyl ethyl ether showed excellent stability effects, so that quality can be guaranteed for a long period of time. Furthermore, carpronium chloride and pantotenyl ethyl ether have local vasodilatory action and hair roots. It became possible to sustain the activation action for a long period of time. Further, when the composition of the present invention is shipped as a product such as a hair restorer, the amount of carpronium chloride and pantotenyl ethyl ether added to the composition can be significantly reduced, which is economically excellent.

Claims (16)

[Claims] 1. A composition containing carpronium chloride, pantotenyl ethyl ether and a water-soluble chitin derivative. 2. A composition containing one or more crude drugs, carpronium chloride, pantotenyl ethyl ether and a water-soluble chitin derivative. 3. One or more species selected from the group consisting of Assemblies, cashews, ginseng, salamander, danshen, ginger, ginger, dio, clove, kaiso, ivy, mannenrow, burdock and Dutch pepper. Containing the above herbal medicines, carpronium chloride, pantotenyl ethyl ether and water-soluble chitin derivative 4. The composition according to claim 2 or 3, wherein the herbal medicines are cashews and ginseng ginseng. 5. The composition according to claim 1, wherein the water-soluble chitin derivative is polyoxyalkylene chitosan. 6. The composition according to claim 1, wherein the water-soluble chitin derivative is hydroxypropyl chitosan. 7. A composition containing cashews, ginseng ginseng, carpronium chloride, pantotenyl ethyl ether and hydroxypropyl chitosan. 8. A composition containing an oyster tincture, a ginseng tincture, a carpronium chloride, pantotenyl ethyl ether and hydroxypropyl chitosan. 9. The composition according to claim 1, wherein the carpronium chloride is in a concentration of 0.1 to 10% by weight. 10. A composition according to claim 1, wherein the carpronium chloride is in a concentration of 0.5 to 5% by weight. 11. Cass 1/5 to 20 parts by weight, Chixetuni ginseng 1/5 to 20 parts by weight, carpronium chloride 1 part by weight, pantotenyl ethyl ether 1/20
~ 20 parts by weight and hydroxypropyl chitosan 1 /
Composition containing 100 to 1/5 parts by weight 12. 1 to 10 parts by weight of cashew, 1 to 10 parts by weight of ginseng carrot, 1 part by weight of carpronium chloride, 1/5 to 5 parts by weight of pantotenyl ethyl ether and 1/50 to 1/50 of hydroxypropyl chitosan.
Composition containing 10 parts by weight 13. A composition containing 1 part by weight of cashew, 1 part by weight of ginseng ginseng, 1 part by weight of carpronium chloride, 1 part by weight of pantotenyl ethyl ether and 1/25 part by weight of hydroxypropyl chitosan. 14. A lotion containing 1% by weight of cashew, 1% by weight of ginseng carrot, 1% by weight of carpronium chloride, 1% by weight of pantotenyl ethyl ether and 0.04% by weight of hydroxypropyl chitosan. 15. The composition according to claim 1, which is for hair, or the lotion according to claim 14. 16. The composition according to any one of claims 1 to 13 for hair growth, promotion of hair growth or hair nourishment or the lotion according to claim 14.