JP7570469B2 - External Composition - Google Patents

Description

The present invention relates to a topical composition that contains chiro-inositol and water and can suppress the formation of precipitates after drying.

Inositol (1,2,3,4,5,6-cyclohexanehexaol) has a structure in which one hydrogen atom on each carbon atom of cyclohexane is replaced by a hydroxyl group, and is a compound known as a vitamin-like substance. Inositol has nine stereoisomers due to the combination of the stereochemical configuration of the hydroxyl groups, of which myo-inositol (cis-1,2,3,5-trans-4,6-cyclohexanehexaol) is widely used as an active ingredient or additive in pharmaceuticals (including quasi-drugs) (see Non-Patent Documents 1-3).

On the other hand, among the stereoisomers of inositol, chiro-inositol (cis-1,2,4-trans-3,5,6-cyclohexanehexaol) has been found in recent years to have an excellent hair growth effect, and it has been reported that it can be used in topical compositions such as hair growth agents (see Patent Document 1). However, the formulation technology for topical compositions containing chiro-inositol has not been fully investigated.

Quasi-drug Raw Materials Standards 2006 Integrated Edition, Yakuji Nipposha, p. 318 Pharmaceutical Additives Standards 2003, Yakuji Nipposha, pp. 101-102 Pharmaceutical Additives Encyclopedia 2000, Yakuji Nipposha, p. 26

Patent No. 6244065

As a result of various investigations into topical compositions containing chiro-inositol in order to improve their effectiveness, usability, convenience, etc., it was found that topical compositions containing chiro-inositol and water have the problem that when applied to body parts such as hair or skin and then dried, chiro-inositol forms a precipitate on the surface of the body part. If chiro-inositol forms a precipitate on the surface of the body part, not only will the desired effects of chiro-inositol not be fully exerted, but the usability will also be impaired.

The object of the present invention is to provide a formulation technology that can suppress the formation of precipitates after drying in a topical composition containing chiro-inositol and water.

The inventors conducted extensive research to solve the above problems and discovered that by incorporating a sugar alcohol into a topical composition containing chiro-inositol and water, the formation of precipitates on the surface of body parts such as hair and skin can be suppressed even when the composition is applied to body parts such as hair and skin and then dried. The present invention was completed through further research based on this finding.

That is, the present invention provides the following aspects.
Item 1. A composition for external use comprising chiro-inositol, a sugar alcohol, and water.
Item 2. The composition for external use according to Item 1, wherein the sugar alcohol is xylitol.
Item 3. The composition for external use according to Item 1 or 2, containing 0.001 to 20% by weight of the chiro-inositol.
Item 4. The composition for external use according to any one of Items 1 to 3, containing the sugar alcohol in an amount of 0.001 to 20% by weight.
Item 5. The composition for external use according to any one of Items 1 to 4, which is a composition for external use for hair or scalp.
Item 6. A method for suppressing the formation of precipitates after drying of a topical composition containing chiro-inositol and water, comprising:
The topical composition is formulated with a sugar alcohol together with chiro-inositol and water.
A method for inhibiting the formation of precipitates after drying of the topical composition.

According to the present invention, even if an external composition containing chiro-inositol and water is applied to body parts such as hair and skin, the formation of chiro-inositol precipitates on the body parts after drying can be suppressed, so that the desired effects of chiro-inositol (e.g., hair growth effect) can be effectively achieved without impairing the feeling of use.

The topical composition of the present invention is characterized by containing chiro-inositol, a sugar alcohol, and water. The topical composition of the present invention will be described in detail below.

[Chiro-inositol]
Chiro-inositol is a known ingredient that is known to have hair growth effects and the like.

The chiro-inositol used in the present invention may be in the D-, L-, or DL-form, but is preferably in the D-form.

The chiro-inositol used in the present invention may be extracted from natural sources such as buckwheat, beans, and citrus fruits, produced and extracted from legumes and the like by fermentation, or chemically synthesized.

The content of chiro-inositol in the topical composition of the present invention may be appropriately set depending on the formulation form and use of the topical composition, but may be, for example, 0.001 to 20% by weight, preferably 0.01 to 10% by weight, more preferably 0.1 to 10% by weight, even more preferably 1 to 5% by weight, and particularly preferably 1 to 2% by weight.

[Sugar alcohol]
In the topical composition of the present invention, the sugar alcohol plays a role in suppressing the formation of chiro-inositol precipitates in the topical composition after application and drying.

The sugar alcohols used in the present invention are not particularly limited as long as they are pharma- ceutically or cosmetically acceptable, but examples include xylitol, erythritol, lactitol, maltitol, mannitol, sorbitol, etc. These sugar alcohols may be used alone or in combination of two or more.

Among these sugar alcohols, xylitol is preferred from the viewpoint of more effectively suppressing the formation of precipitates after drying.

In the topical composition of the present invention, the ratio of chiro-inositol to sugar alcohol is, for example, 10 to 1000 parts by weight of sugar alcohol per 100 parts by weight of chiro-inositol. From the viewpoint of more effectively suppressing the formation of precipitates after drying, the ratio of sugar alcohol is preferably 50 to 500 parts by weight, more preferably 50 to 200 parts by weight, per 100 parts by weight of chiro-inositol.

The sugar alcohol content in the topical composition of the present invention is, for example, 0.001 to 20% by weight. From the viewpoint of more effectively suppressing the formation of precipitates after drying, the sugar alcohol content in the topical composition of the present invention is preferably 0.01 to 10% by weight, more preferably 0.1 to 9% by weight, and even more preferably 1 to 9% by weight.

[water]
In the topical composition of the present invention, water serves as a base. The content of water in the present invention may be the balance other than chiro-inositol, sugar alcohol, and other components described below, and may be, for example, 1 to 99.98% by weight, preferably 10 to 99% by weight, more preferably 40 to 98% by weight, and even more preferably 40 to 60% by weight.

[Monohydric lower alcohol]
The topical composition of the present invention may contain a monohydric lower alcohol. The type of monohydric lower alcohol used in the present invention is not particularly limited, but examples thereof include monohydric lower alcohols having 2 to 6 carbon atoms, more specifically, ethanol, propanol, butanol, isopropanol, etc. These monohydric lower alcohols may be used alone or in combination of two or more kinds. Among these monohydric lower alcohols, ethanol is preferred.

When the topical composition of the present invention contains a monohydric lower alcohol, its content may be appropriately set depending on the formulation form and use of the topical composition, but may be, for example, 0.1 to 98% by weight, preferably 5 to 50% by weight, and more preferably 30 to 50% by weight.

[Other ingredients]
In addition to the above-mentioned components, the composition for external use of the present invention may contain a physiologically active component, if necessary. Examples of such pharmacological components include hair growth agents other than chiro-inositol, cooling agents, antihistamines, local anesthetics, disinfectants, anti-inflammatory agents, cell activators, skin protective agents, blood circulation promoting components, plant extracts, vitamins, amino acids, mucopolysaccharides, etc.

In addition to the above-mentioned components, the topical composition of the present invention may contain other additives used in topical compositions, if necessary. Examples of such additives include surfactants, polyhydric alcohols, excipients, stabilizers, odorants, dispersants, diluents, emulsifiers, transdermal absorption enhancers, pH adjusters, preservatives, colorants, oils (oils and fats, mineral oils, etc.), moisturizers, thickeners, polymers, film-forming agents, UV absorbers, antioxidants, preservatives, cooling agents, deodorants, pigments, dyes, fragrances, sugars, organic acids, organic amines, etc.

[Dosage form, etc.]
The dosage form of the topical composition of the present invention is not particularly limited, but may be, for example, a liquid or semi-solid form (gel, cream, ointment, paste, etc.), preferably a liquid form.

The topical composition of the present invention can be used as a topical drug (including quasi-drugs), cosmetic product, or other product. In particular, chiro-inositol is known to have an excellent hair growth effect, so the topical composition of the present invention can be suitably used as a topical composition for hair or scalp (topical drug for hair or scalp, and cosmetic product for hair or scalp).

When the topical composition of the present invention is made into a topical medicine (including quasi-drugs), the formulation form is not particularly limited, but examples include gels, creams, lotions, emulsions, liquids, patches, aerosols, liniments, ointments, packs, hair bleach, etc.

When the topical composition of the present invention is made into a cosmetic product, the formulation form is not particularly limited, but examples include hair or scalp cosmetics such as hair growth products, hair tonics, hair sprays, hair mist, hair foams, hair blow dryers, hair liquids, scalp essences, hair dyes, and hair liquids; skin cosmetics such as gels, creams, milky lotions, skin toners, lotions, packs, and ointments; and skin cleansing products such as body shampoos, hair shampoos, and rinses.

2. Precipitation Inhibition Method The precipitation inhibition method of the present invention is a method for inhibiting the formation of precipitates after drying of a topical composition containing chiro-inositol and water, and is characterized by incorporating a sugar alcohol into the topical composition.

In this precipitation inhibition method, the type of sugar alcohol used, the contents of chiro-inositol, sugar alcohol, and water, the types and contents of other ingredients that are blended as necessary, the dosage form of the topical composition, etc. are the same as those in "1. Topical composition" above.

The present invention will be explained in more detail below with reference to examples, but the present invention is not limited to these.

Test Example 1: Test to confirm the presence or absence of precipitates after drying on a petri dish (1)
The topical compositions (liquids) were prepared with the compositions shown in Table 1. 0.1 g of each of the obtained topical compositions was dropped into a petri dish and dried at room temperature for 24 hours. Thereafter, the degree of precipitation was visually confirmed, and the degree of precipitation (white crystals) was evaluated according to the following criteria.
<Criteria for determining the degree of precipitate formation>
◯: No precipitate was observed.
Δ: Formation of a slight amount of precipitate was observed.
×: Formation of precipitates is clearly observed.

The results are shown in Table 1. When chiro-inositol and water were included, the formation of precipitates was observed after drying (Comparative Examples 1 and 2), but when xylitol was further added, the formation of precipitates due to drying was suppressed (Examples 1 to 5).

Test Example 2: Confirmation of the Presence or Absence of Precipitation After Drying on Human Hair External use compositions (liquids) with the compositions shown in Test Table 2 were prepared. 0.8 g of a human hair sample was immersed in 5 g of each of the obtained external use compositions for 3 minutes, then removed and dried at 60° C. for 24 hours. Thereafter, the appearance of the human hair sample was visually observed, and the degree of the formation of precipitates (white crystals) was evaluated according to the same criteria as in Test Example 1.

The results are shown in Table 2. When a topical composition containing chiro-inositol and water was applied to human hair, the formation of precipitates was observed after drying (Comparative Example 1), but the formation of precipitates after drying was suppressed when the topical composition further contained xylitol (Example 1).

Test Example 3: Test to confirm the presence or absence of precipitates after drying on a petri dish (2)
Topical compositions (liquid preparations) having the compositions shown in Table 3 were prepared, and the degree of formation of precipitates (white crystals) after drying of each topical composition was evaluated in the same manner as in Test Example 1 above.

The results are shown in Table 3. These results also confirmed that by adding xylitol to a topical composition containing chiro-inositol and water, the formation of precipitates after drying can be suppressed.

Claims (5)

comprising chiro-inositol, a sugar alcohol, and water;
The composition for external use (excluding self-tanning compositions) wherein the sugar alcohol is at least one selected from the group consisting of erythritol, lactitol, maltitol, mannitol, and sorbitol. The composition for external use according to claim 1 contains 0.001 to 20% by weight of chiro-inositol. The composition for external use according to claim 1 or 2 contains 0.001 to 20% by weight of the sugar alcohol. The composition for external use according to any one of claims 1 to 3, which is a composition for external use for hair or scalp. A method for inhibiting the formation of a precipitate after drying of a topical composition (excluding self-tanning compositions) containing chiro-inositol and water, comprising:
The composition for external use is formulated with chiro-inositol and water, as well as at least one sugar alcohol selected from the group consisting of erythritol, lactitol, maltitol, mannitol, and sorbitol.
A method for inhibiting the formation of precipitates after drying of the topical composition.