Minoxidil-containing compositions

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition containing minoxidil as an active component and designated for increase of hair growth. The composition comprises also dibutylhydroxytoluene and butylhydroxyanisole taken in the amount 0.005-0.5 mass part per one part of minoxidil in the concentration of minoxidil from 3% to 6% and at pH value 5.5-7.0 or 5.7-6.3 (variants), and to a method for prevention of staining the minoxidil-containing composition. Compositions prevent staining minoxidil as time passes and provide uniform dissolving and stability of active component.

EFFECT: improved and valuable properties of composition.

5 cl, 2 tbl, 11 ex

 

The technical FIELD TO WHICH the INVENTION RELATES.

The present invention relates to compositions containing Minoxidil, which is protected from staining over time.

Background of invention

Minoxidil is a component that is assumed to be an external agent, hair growth due to its inherent effect of increasing hair growth.

However, Minoxidil when storing it in the form of a solution has the disadvantage as the tendency to staining over time, and therefore there is a potential risk of reduction in value caused by this effect.

The problems solved by the present invention

The aim of the present invention is to prevent dyeing compositions containing Minoxidil.

Description of the invention

Normally, in order to introduce a component which tend to appear in the liquid, it is possible to improve protivoukachiwauschee properties of the drug by the introduction of such antioxidant, as dibutylaminoethanol. However, the authors of the present invention found that in the case of a liquid product containing Minoxidil, the combination with such antioxidant, as dibutylaminoethanol, practically does not prevent staining or even enhances it.

As a result of extensive investigations directed the military to solve this problem, found that when the pH of the liquid compositions containing Minoxidil, is brought to a value of from 5.5 to 7.0, the above disadvantage can be overcome and significantly enhance the protective effect regarding coloring liquid drug, which led to the creation of the present invention.

That is, the present invention relates to compositions containing Minoxidil, which includes one or two compounds selected from the group including dibutylaminoethanol and butylhydroxyanisole, and has a pH from 5.5 to 7.0.

In addition, the present invention relates to a method of preventing coloring compositions containing Minoxidil, which includes the introduction in the composition one or more compounds selected from the group comprising dibutylaminoethanol and butylhydroxyanisole, and bringing the pH of the composition to a value of from 5.5 to 7.0.

The method of implementation of the present invention

Antioxidant, intended for use in the present invention preferably is one or two compounds selected from the group including dibutylaminoethanol, butylhydroxyanisole, editorview acid, EDTA-2Na, isopropylacetate, propylgallate, guaiac acid, α-diglycerin, potassium dichloroisocyanurate, 2,6-di-t-butyl-4-METHYLPHENOL, soy lecithin, thioglycolate sodium, sodium salt diablock the th acid, palmitate ascorbic acid, 2-mercaptobenzimidazole and sulfate oksihinolina. In addition, as an antioxidant can also be used plant extracts and preferably one or two of the extract is selected from the group comprising extracts of clove, geranium leaves, rhubarb, bark Phellodendron, peony root, moutan bark, coptis rhizome, unshiu peel of a lemon, hops ordinary, root Scutellaria, brown tree bark, stem, root platycodon, ginger, safflower and root of Angelica Japanese. The mentioned plant extracts can be obtained using water, alcohol, containing from 2 to 4 carbon atoms (for example, ethanol, propylene glycol, 1,3-butyleneglycol or glycerol) or mixtures thereof as the extracting solvent.

The number of one or two compounds selected from the group comprising dibutylaminoethanol and butylhydroxyanisole, in the composition of the present invention is in the range of preferably 0.005 to 0.5 wt. parts per mass. part of Minoxidil and particularly preferably from 0.01 to 0.5 mass. parts. Adding to the lack of antioxidant can sometimes speed up the painting, even if the pH is in the range from 5.5 to 7.0.

In the composition of the present invention prevents staining effect becomes the becomes lower with decreasing pH, so the pH is preferably adjusted to a value of 5.5 or higher and particularly preferably up to 5.7 or higher.

From the viewpoint of solubility of Minoxidil pH is preferably adjusted to 7.0 or lower and particularly preferably up to 6.3 or below.

Regulation of the pH of the composition of the present invention can be carried out with the use of such traditional pH regulator, such as an organic acid (e.g. citric acid, malic acid and lactic acid) or inorganic acid (e.g. phosphoric acid, hydrochloric acid and sulfuric acid).

In the composition of the present invention, the concentration of Minoxidil is in the range preferably from 1 to 10% of the mass. and particularly preferably from 3 to 6% of the mass. based on the weight of the entire composition.

The composition of the present invention may preferably contain as solvent polyhydric alcohol.

Of the polyhydric alcohols are preferred such as propylene glycol, dipropyleneglycol, 1,3-butyleneglycol, glycerin, hexyleneglycol and polyethylene glycol, and more preferable is 1,3-butyleneglycol. From glycols are preferred Macrogol 200 and Macrogol 400. The number of input polyhydric alcohol is preferably in the range from 1 to 50 mass. parts per mass. frequent is of Minoxidil.

Preparative forms of the compositions of the present invention, but not limited by them, can be any lotions, aerosols and gels, and obtaining them can be carried out in accordance with the General methods of obtaining medicinal or cosmetic products.

Compositions of the present invention, if necessary, may contain soljubilizatory (for example, esters of fatty acids, esters of fatty acid and polyhydric alcohol, glycerides of fatty acids with medium chain length, vegetable oil or simple alkalemia esters of glycerol), surfactants (for example, nonionic surfactants, derivatives of lecithin or polymeric emulsifiers), mulgirigala stabilizers, promoters adsorption, etc.

The advantages of the present invention

The present invention allows to obtain compositions containing Minoxidil, staining which over time can be prevented.

Embodiments of the present invention

In more detail, the present invention will be illustrated using the following examples and experiments.

pH determines to 5 ml using a pH meter with a glass electrode (manufactured by DKK-Toa Corp.) within 5 minutes.

Example 1

Phosphoric acid (0.5 ml) are added to Minoxidil (5 g), 1,3-butyleneglycol the Yu (30 g), ethanol (50 g) and dibutylaminoethanol (0.5 g), and total volume of the mixture is brought to 100 ml of purified water and dissolved under stirring, resulting in a gain composition type of lotion, the pH of which is 6.0.

Example 2

Phosphoric acid (0.9 ml) is added to Minoxidil (5 g), 1,3-butyleneglycol (30 g), ethanol (50 g) and dibutylaminoethanol (0.1 g) and total volume of the mixture is brought to 100 ml of purified water and dissolved under stirring, resulting in a gain composition type of lotion with a pH of 5.5.

Example 3

Citric acid (0.55 g) are added to Minoxidil (5 g), 1,3-butyleneglycol (30 g), ethanol (50 g) and dibutylaminoethanol (0.5 g) and total volume of the mixture is brought to 100 ml of purified water and dissolved under stirring, resulting in a gain composition type of lotion, the pH of which is 6.4.

Example 4

Phosphoric acid (0,02 ml) are added to Minoxidil (3 g), 1, 3-butyleneglycol (30 g), ethanol (50 g) and butylhydroxyanisole (0.5 g) and total volume of the mixture is brought to 100 ml of purified water and dissolved under stirring, resulting in a gain composition type of lotion, the pH of which is 7.0.

Example 5

Phosphoric acid (0.3 ml) are added to Minoxidil (5 g), propylene glycol (52 g), ethanol (25 g) and dibutylaminoethanol (0.5 g) and total volume of the mixture is brought to 100 ml of purified water and dissolved when displacement is Ivanyi, in the result, get the composition type of lotion, the pH of which is 6.0.

Comparative example 1

Purified water is added to Minoxidil (3 g), 1,3-butyleneglycol (30 g), ethanol (50 g) and dibutylaminoethanol (0.5 g) and total volume of the mixture was adjusted to 100 ml, the mixture was dissolved under stirring, resulting in a gain composition type of lotion, the pH of which is 8.8.

Comparative example 2

Minoxidil (5 g), propylene glycol (52 g) and ethanol (25 g) are mixed and the total volume of the mixture is brought to 100 ml with purified water, and dissolved with stirring, resulting in a gain composition type of lotion, the pH of which is 8.7.

Comparative example 3

Minoxidil (5 g), propylene glycol (52 g), ethanol (25 g) and phosphoric acid (0.3 ml) are mixed, the total volume of the mixture is brought to 100 ml of purified water and dissolved under stirring, resulting in a gain composition type of lotion, the pH of which is 6.0.

Comparative example 4

Minoxidil (5 g), propylene glycol (52 g), ethanol (25 g) and dibutylaminoethanol (0.5 g) are mixed, the total volume of the mixture is brought to 100 ml of purified water and dissolved under stirring, resulting in receiving the composition, the pH of which is 8.7.

Experiment 1

Each of the compositions of examples 1-4 and comparative example 1 are placed in a flask of PET and stored at 50°for one is months, observing the appearance (color tone). Appearance is assessed according to the following standards.

0: Staining is not installed, no trademark issues.

1: Installed slight staining, no trademark issues.

2: Set the colouring, the emergence of commodity problems.

The results obtained are presented in table 1.

Table 1
DrugsExample 1Example 2Example 3Example 4Comparative example 1
pH65,56,478,8
Score01012

Staining installed in comparative example 1 and, judging by this, there is a problem with the commercial implementation. In the compositions according to examples 1-4 was not found or no detected light staining and judging by this, no commodity is not a problem.

Experiment 2

Each of the compositions of example 5 and comparative examples 2-4 are placed in a flask of PET and after storage at 50°within one month, measure the absorbance (420 nm)using absorbtiometry (production Beckroan Co.).

The results of t is established with representation in table 2.

Table 2
DrugsExample 5Comparative example 2Comparative example 3Comparative example 4
PH68,768,7
EIT0.5 g0 g0 g0.5 g
The absorbance (420 nm)0,0130,0210,0580,039

The results for comparative examples 2 and 3 show that the dyeing compositions containing Minoxidil increases with decreasing pH. In addition, the results of comparative example 4 show that the staining increases with the addition of BHT, not to mention the fact that it can be avoided.

In contrast, a significant positive effect on the prevention of staining in example 5 in comparison with all the comparative examples.

1. Composition containing Minoxidil and designed to increase hair growth, which includes one or two compounds selected from the group including dibutylaminoethanol and butylhydroxyanisole in the amount of 0.005 to 0.5 wt. hours per 1 wt. PM mi is oxidise, has a concentration of Minoxidil from 3 to 6 wt.% and pH from 5.5 to 7.0.

2. Composition containing Minoxidil and designed to increase hair growth, which includes one or two compounds selected from the group including dibutylaminoethanol and butylhydroxyanisole in the amount of 0.005 to 0.5 wt. hours per 1 wt. hours of Minoxidil has a concentration of Minoxidil from 3 to 6 wt.% and pH from 5.7 to 6.3.

3. A composition comprising Minoxidil, according to claim 1 or 2, which further includes a polyhydric alcohol.

4. A composition comprising Minoxidil, according to claim 1 or 2, which further includes a glycol.

5. The way to prevent staining compositions containing Minoxidil, which includes the introduction into the composition of one or two compounds selected from the group comprising dibutylaminoethanol and butylhydroxyanisole, and bringing the pH of the composition to a value of from 5.5 to 7.0.



 

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