JPH11263727A - Minoxidil formulated liquid preparation composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a liquid preparation composition prevented in coloring with time by including minoxidil and an amino acid. SOLUTION: This liquid preparation composition is obtained by including minoxidil and an amino acid, preferably in an amount of 0.01-20 pts.wt. based on 1 pt.wt. minoxidil. The amino acid includes preferably a sulfur-containing amino acid (e.g. taurine, cysteine, cystine or methionine). The solvent for liquid preparation is preferably a mixed solution of 10-50 V/V% water with 1-6C alcohols (preferably ethanol, propylene glycol or 1, 3-butylene glycol. Minoxidil is preferably formulated in an amount of 0.1-5 wt.% based on total preparation. When the liquid preparation is diluted to 20 times with purified water, pH of the diluted solution is preferably 4-9. Container for storing the composition is preferably made of a material such as PET, glass, polyethylene or polypropylene. The liquid preparation can be formulated with a solution auxiliary, a thickener, a absorbefacient, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a minoxidil-containing liquid composition which prevents coloring over time.

[0002]

2. Description of the Related Art Minoxidil is a component which is expected as an externally used hair restorer due to its hair restorer effect.

[0003] However, when minoxidil is stored in a solution state, it has a drawback that it is liable to be colored over time, which sometimes leads to a decrease in commercial value. Although the coloring mechanism of the minoxidil-containing liquid preparation has an unknown point, it is presumed that light is involved. Therefore, it is necessary to use a light-shielded container in order to commercialize the minoxidil-containing liquid product, but such a container is inconvenient because the remaining amount of the contents is not clear.

[0004] In general, in order to incorporate a component which is easily colored into a liquid, the composition is improved by adding an antioxidant, an anti-chelating agent and the like. However, there is no sufficient effect on the prevention of coloring of the minoxidil-containing liquid over time. Was.

On the other hand, it is also conceivable that the product is colored from the beginning so that the product is not noticeable even when colored. However, since the hair restorer is used after being applied to the scalp, it is not preferable to color the hair from the beginning since it stains clothes and bedding.

[0006]

SUMMARY OF THE INVENTION An object of the present invention is to prevent coloring of a liquid formulation containing minoxidil.

[0007]

Means for Solving the Problems The present inventors have conducted various studies to solve the above-mentioned problems. As a result, when amino acids, particularly taurine, are added to a liquid containing minoxidil, surprisingly, the coloring of the liquid can be prevented. It has been found that the present invention has been completed and the present invention has been completed.

That is, the present invention is a liquid composition comprising minoxidil and an amino acid.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, any amino acid can be used as long as it can be blended with a hair restorer, including salts.

In the present invention, among the amino acids, sulfur-containing amino acids (taurine, cysteine, cystine, methionine, homocysteine, etc.) are preferred from the viewpoint of the coloring prevention effect, and among them, taurine is particularly preferred.

In the liquid composition of the present invention, the concentration of minoxidil is preferably 0.1 to 5% by weight of the liquid preparation. If the amount is less than 0.1% by weight, the efficacy of minoxidil as a hair restorer will be weak, and if it exceeds 5% by weight, formulation design will be difficult.

In the present invention, the higher the amount of the amino acid, the better the effect of preventing the coloring of the liquid preparation can be expected.
20 parts by weight are preferred.

In the liquid composition of the present invention, the solvent of the liquid is preferably a water-containing organic solvent. This is because amino acids do not dissolve when only an organic solvent is used, and minoxidil does not dissolve when only water is used. The water content at this time is 10 to 50 V / V%
Is preferred. Here, the organic solvent to be used must be a solvent which is uniformly mixed with water and which does not adversely affect the skin even when used as an external preparation for skin. From that point,
As the organic solvent, alcohols having 1 to 6 carbon atoms (ethanol, propanol, isopropanol, ethylene glycol, propylene glycol, 1,3-butylene glycol, glycerin and the like) are preferable, and among them, ethanol, propylene glycol and 1,3- One or more selected from the group consisting of butylene glycol is particularly preferred.

In the present invention, from the viewpoint of preventing coloration, those having a pH of 4 to 9 when the solution is diluted 20 times with purified water are preferred.

According to the present invention, the storage container for the minoxidil-containing liquid composition can be selected as long as it can be used for general liquid preparations. However, materials such as PET, glass, polyethylene, and polypropylene are particularly preferable. preferable.

The liquid preparation of the present invention can be prepared by a general method for preparing a liquid preparation, but it is preferable to mix an amino acid previously dissolved in water with an organic solvent when compounding an amino acid. This is because it takes time to dissolve the amino acid in the water-containing organic solvent later from the viewpoint of the dissolution rate of the amino acid.

According to the present invention, although the coloring prevention effect of the preparation by the amino acid was recognized, it is also expected that the pharmacological action (anti-inflammatory action, skin irritation reducing action, antipruritic action, etc.) of the amino acid is exhibited. it can.

The liquid preparation of the present invention may contain components generally used in external preparations (dissolution aids, thickeners, absorption promoters, pH adjusters, etc.).

[0019]

According to the present invention, it is possible to prevent coloring of a liquid formulation containing minoxidil.

[0020]

The present invention will be described in more detail with reference to the following Examples and Test Examples.

Example 1 1 g of minoxidil, 0.04 g of taurine, 10 g of propylene glycol, 60 g of ethanol and a total amount of 100 ml
Of purified water was stirred and dissolved to obtain a liquid composition.

Comparative Example 1 A comparative liquid preparation was obtained in the same manner as in Example 1 except that taurine was omitted.

Test Example 1 Each of three liquid preparations of Example 1 and Comparative Example 1 was filled in a transparent glass bottle, and irradiated with light of 3000 Lux at room temperature for 34 days. The results of measuring the absorbance at a wavelength of 420 nm at the start of the test and after the test are shown in Table 1.

[0024]

[Table 1]

Example 2 1 g of minoxidil, 0.1 g of taurine, 10 g of propylene glycol, 60 g of ethanol and purified water made up to 100 ml with purified water were stirred and dissolved to obtain a liquid preparation.

Test Example 2 The liquid composition of Example 2 and the comparative liquid of Comparative Example 1 were
Each was placed in a colorless glass bottle and left at room temperature for 6 months at a window illuminated by room light. After 30 days and 6 months, the color was judged visually by three measurers who did not know the contents of the solution. In addition, at the start of the test and after 6 months, 42
The absorbance at 0 nm was measured.

The results are shown in Table 2.

[0028]

[Table 2]

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ Identification code FI // A61K 7/06 A61K 7/06

Claims (10)

[Claims] 1. A liquid composition comprising minoxidil and an amino acid. 2. The liquid composition according to claim 1, wherein the amino acid is a sulfur-containing amino acid. 3. The liquid composition according to claim 1, wherein the amino acid is taurine. 4. The liquid composition according to claim 1, wherein the amount of the amino acid is 0.01 to 20 parts by weight per 1 part by weight of minoxidil. 5. The liquid composition according to claim 1, wherein the solvent of the liquid is a mixture of water and an alcohol having 1 to 6 carbon atoms. 6. The liquid composition according to claim 5, wherein the content of water in a mixture of water and an alcohol having 1 to 6 carbon atoms is 10 to 50 V / V%. 7. The liquid composition according to claim 5, wherein the alcohol having 1 to 6 carbon atoms is one or more selected from the group consisting of ethanol, propylene glycol and 1,3-butylene glycol. 8. The compounding amount of minoxidil is 0.1% of the whole preparation.
The liquid composition according to any one of claims 1 to 7, wherein the content is from 5 to 5% by weight. 9. An anti-coloring agent for a minoxidil-containing solution containing an amino acid as an active ingredient. 10. A method for preventing coloring of a minoxidil-containing liquid preparation, which comprises mixing an amino acid.