JP2001187741A - Skin care medicinal composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a medicinal composition for external use for skin that can efficiently exclude sebaceous matters in the hair follicles and has excellent high therapeutic effect without conspicuous whiteness at the applied parts, particularly is useful for treatment of acne. SOLUTION: This skin care medicinal preparation characteristically comprises (A) at least one selected from sodium chloride, magnesium chloride, magnesium sulfate, calcium chloride, potassium chloride, sodium hydrogen carbonate and sodium carbonate and (B) at least one selected from polyhydric alcohols.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a pharmaceutical composition for external use on the skin, and more particularly, to a pharmaceutical composition for external use on the skin where the applied portion is white and inconspicuous.

[0002]

2. Description of the Related Art Acne vulgaris (acne) is a very common skin disease, and usually occurs most often from before puberty to after puberty, that is, from about 13 to 23 years old. Many factors are involved in the development of acne vulgaris, and the background or facilitating factors of the development are endocrine changes during puberty, genetic factors, external stimuli, nervous stress,
Skin impureness, external temperature, etc. are mentioned, and the direct causes of the onset are 1) sebaceous follicles, 2) increased sebum secretion,
3) Presence of bacteria in hair follicle, 4) Keratinization of hair follicle funnel (Nishijima Atsuko, Pharmaceutical Journal, Vol. 22, No. 6, p. 1148, 19)
1986).

[0003] Among these factors, in particular, keratinization of the hair follicle funnel prevents the increased discharge of sebum outside the hair follicle and promotes the growth of anaerobic bacteria in the hair follicle. It is a major factor in making acne vulgaris worse. Further, the keratinization of the follicle funnel also suppresses penetration of various drugs such as antibiotics, bactericides, and anti-inflammatory agents applied externally to the treatment site, and the therapeutic effect of these external preparations is reduced.

As a means for solving the above problem, it is known to use a drug having an action of exfoliating the keratinized stratum corneum, for example, a keratolytic agent such as salicylic acid. However, since these agents have an irritating effect on the skin, the amount used in the composition is limited, and a sufficient effect cannot be obtained.

On the other hand, in order to promote the discharge of sebum in the hair follicle, an external preparation containing an inorganic powder such as bentonite as a sebum adsorbent, or a specific salt mixture such as sodium or magnesium chloride or carbonate is used. It is also known that the compounded external preparation is effective for healing dermatosis (Japanese Patent Application Laid-Open No. 7-26786).
9, JP-A-7-267870, US Pat. No. 4,943,432
etc). However, these external preparations do not have a sufficient effect of discharging sebum from the hair follicles, and further, there is a problem in that when the external preparation is applied to the skin, the application part is conspicuously white.

[0006]

SUMMARY OF THE INVENTION The present invention has been made in view of the above-mentioned problems, and has an object to efficiently remove sebum in hair follicles and have a high therapeutic effect on the skin with a white and inconspicuous applied portion. An object of the present invention is to provide a pharmaceutical composition, particularly a pharmaceutical composition for treating acne.

[0007]

Means for Solving the Problems The present inventors have made intensive studies to achieve the above object, and as a result, have found that the above object can be solved by blending a specific inorganic salt and a polyol at a specific ratio. The present invention has been completed.

That is, the present invention relates to (A) sodium chloride,
Provided is a pharmaceutical composition for external use, characterized by containing at least one selected from magnesium chloride, magnesium sulfate, calcium chloride, potassium chloride, sodium hydrogen carbonate, and sodium carbonate, and (B) polyhydric alcohols.

[0009]

DETAILED DESCRIPTION OF THE INVENTION The component (A) of the present invention is an inorganic salt selected from sodium chloride, magnesium chloride, magnesium sulfate, calcium chloride, potassium chloride, sodium hydrogen carbonate and sodium carbonate. These inorganic salts are
One type or a mixture of two or more types may be used, but two or more types are preferable, and at least sodium chloride is contained from the viewpoint of skin permeability and stability of the preparation. Is preferred. That is, a preferred inorganic salt mixture is a mixture of sodium chloride and an inorganic salt selected from magnesium chloride, magnesium sulfate, calcium chloride, potassium chloride, sodium hydrogen carbonate, and sodium carbonate.

In the present invention, the amount of the inorganic salt of the component (A) is in the range of 1 to 16% by weight, preferably 1 to 14% by weight, more preferably 1 to 12% by weight in the composition. In this range, the stability of the composition and the skin treatment effect are particularly good.

The polyhydric alcohol which is the component (B) of the present invention includes glycerin; polyglycerin such as diglycerin and triglycerin; 1,3-butylene glycol;
Glycols such as propylene glycol and ethylene glycol; and sugar alcohols such as sorbitol and mannitol. Preferred are glycerin, 1,3-butylene glycol and propylene glycol, and particularly preferred is glycerin.

The content of the component (B) in the composition is not particularly limited, but is 0.01 to 50% by mass, particularly 0.2 to 50% by mass.
When the content is 30% by mass, the stiffness of the skin due to the inorganic salt is suppressed, and a composition having an excellent feeling upon use can be obtained.

The pharmaceutical composition for external use on the skin of the present invention contains 10 to 10 carbon atoms in order to promote the penetration of the active ingredient into the skin.
It preferably contains a nonionic surfactant having 22, preferably 12 to 18 hydrocarbon groups. Specifically, polyoxyethylene (EO2 to 50) alkyl ether, polyoxyethylene (EO3 to 30) (poly) oxypropylene (PO1 to 3) alkyl ether, glycerin fatty acid ester, polyoxyethylene (EO5 to EO5)
15) Glycerin fatty acid ester, sorbitan fatty acid ester, polyoxyethylene (EO6-20) sorbitan fatty acid ester, polyoxyethylene sorbit (E
O6-60) fatty acid ester, polyoxyethylene (E
O2-50) fatty acid ester, polyoxyethylene (E
O3-60) Castor oil, polyoxyethylene (EO5-
100) Hardened castor oil, lecithin derivatives, glycerin fatty acid esters, polyoxyethylene (EO5 to 15) fatty acid esters, polyoxyethylene (EO5 to 30) sterols, and the like.

Of these, polyoxyethylene (EO)
2-50) alkyl ether, polyoxyethylene (E
O5-100) hydrogenated castor oil, polyoxyethylene (E
O6-20) Sorbitan fatty acid esters are preferably used.

The content of the nonionic surfactant in the composition is preferably 0.001 to 20% by mass, particularly preferably 0.01 to 10% by mass, and more preferably 0.1 to 3% by mass. Within this range, the effect of promoting sebum excretion from hair follicles is remarkably obtained.

Furthermore, the pharmaceutical composition for external use on the skin of the present invention preferably contains a keratolytic agent. Examples of the keratolytic agent include sulfur, resorcin, salicylic acid, glycolic acid, urea, vitamin A acid, thioxolone, dibenzothiophene, benzoyl peroxide, papain and the like. These are preferably added in the composition in an amount of 0.01 to 5% by mass. In this range, a composition having a good keratolytic effect and no irritation to the skin can be obtained.

Further, the pharmaceutical composition of the present invention preferably contains a bactericide in order to improve the effect of treating acne. Examples of the disinfectant include benzalkonium chloride, benzethonium chloride, decalinium chloride, chlorhexidine hydrochloride, isopropylmethylphenol, hinokitiol, triclosan, trichlorocarbanilide, berberine, thymol, and photosensitive element 201. Among these, cationic disinfectants such as benzalkonium chloride, benzethonium chloride, decalinium chloride, and chlorhexidine hydrochloride can be preferably used. These are contained in the composition preferably in an amount of 0.001 to 5% by mass, particularly preferably 0.01 to 2% by mass.

The pharmaceutical composition for external use on the skin of the present invention can contain various active pharmaceutical ingredients. Specifically, anti-inflammatory agents such as dipotassium glycyrrhizinate, glycyrrhizic acid, glycyrrhetinic acid, ibuprofen piconol, indomethacin, mefenamic acid, allantoin, zinc oxide, epsilon aminocaproic acid, tranexamic acid, guaiazulene, bufexamac, prednisolone, hydrocortisone, Antibiotics such as tetracycline, erythromycin, gentamicin sulfate, diphenhydramine or its hydrochloride, antihistamines such as chlorpheniramine, chlorpheniramine maleate, isopendyl hydrochloride, local anesthetics such as dibucaine, lidocaine, takeine, ethyl paraaminobenzoate, crotamiton Steroids such as antipruritics such as hydrocortisone acetate and dexamethasone acetate fluorosinolone acetonide It is.

The amount in these compositions can be appropriately compounded in an appropriate amount according to each drug component. For example, the anti-inflammatory agent is usually 0.01 to 10% by mass, the antibiotic is usually 0.1 to 5% by mass, and the antihistamine is 0.1 to 2% by mass.
% By mass, 0.1 to 2% by mass of a local anesthetic, and 0.1% of an antipruritic.
It is blended in the range of 1 to 10% by mass.

In the pharmaceutical composition for external use on the skin of the present invention, in addition to the above essential components, various components usually contained in external preparations such as a humectant, a thickener, a stabilizer, a pH adjuster, a fragrance and the like are contained. It can be blended within a range that does not impair the effects of the present invention. As humectants, hyaluronic acid, pyrrolidone carboxylic acid,
Trimethylglycine, collagen, urea, etc., thickeners such as hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, water-soluble polymers such as carboxyvinyl polymer, etc., stabilizers such as sodium edetate, and pH adjusters such as water Sodium oxide, citric acid and the like can be preferably used. Further, as the flavor, rose oil, lavender oil, sage oil, eucalyptus oil, peppermint oil, rosemary oil, vegetable essential oils such as chamomile oil, limonene, linalool, farnesol, citral, menthol, γ-undecalactone, eugenol, Geraniol, citronellol, orlanchiol and the like.

The pharmaceutical composition for external use on the skin of the present invention may be in the form of a uniform aqueous solution or an aqueous gel, an emulsion or the like, which can be produced by a usual method for producing an external preparation.

In the case of an emulsion, W / O, O / W, W / O
/ W, any type of emulsion may be used, but preferably the oil phase component / water phase component is 40/60 to 5 /
95, preferably 20/80 to 5/95. This range gives a composition with a refreshing feel.

[0023]

The present invention will be described in more detail with reference to the following Examples and Comparative Examples. For the acne treatment formulations described in Tables 1 to 3, after heating, polyhydric alcohols, nonionic surfactant and purified water were mixed well and made uniform, then the active ingredient was stirred and dissolved and dispersed, and inorganic salts were added. Each sample was further stirred and mixed to prepare each sample, and the following evaluation was performed.

The sediment- discharging palmitic acid was dissolved in chloroform (concentration: 50% by mass), and the unglazed plate was immersed in this solution to impregnate the porous of the unglazed plate with palmitic acid under vacuum. After immersing the unglazed plate in each solution, it was observed using a microscope whether or not palmitic acid was eluted from the porosity of the unglazed plate. In this test, since the porous diameter of the unglazed plate is similar to that of the hair follicle, impregnating it with palmitic acid, a sebum component, creates a model in which sebum is accumulated in the hair follicle. This test can evaluate sebum excretion from hair follicles. ○ Sebum discharge was observed △ Sebum discharge was somewhat stopped × Sebum discharge was hardly observed.

Judgment of whitening after application Each composition was applied to the skin of the face under a constant temperature and humidity condition of room temperature of 20 ° C. and a humidity of 40% RH, and was visually evaluated 30 minutes later. ◎ No whitening ○ Almost no whitening △ Some whitening × Some whitening

[0026]

[Table 1]

[0027]

[Table 2]

[0028]

[Table 3]

(Example 16) Emulsion type preparation A cream having the following composition was prepared. This cream had no whitening after application, had no stickiness, had a refreshing feel, and had a good feeling in use. Oil phase: sorbitan monostearate 3.0 polyoxyethylene (20) sorbitan monostearate 4.0 octyldodecanol 1.0 diisopropyl adipate 1.0 soybean lecithin 0.5 aqueous phase: sodium chloride 5.0 Magnesium chloride 2.0 Magnesium sulfate 1.0 Calcium chloride 0.5 Potassium chloride 0.5 Sodium bicarbonate 0.1 Sodium carbonate 0.05 Benzethonium chloride 10.0 Carboxyvinyl polymer 0.2 Potassium hydroxide (pH) Appropriate amount purification Water

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 31/045 A61K 31/045 33/06 33/06 33/10 33/10 A61P 17/00 A61P 17 / 00 17/10 17/10 F term (reference) 4C083 AA122 AB112 AB311 AB312 AB331 AB332 AB341 AB342 AB361 AB362 AC121 AC122 AC182 AC312 AC372 AC432 AC442 AC472 AC692 AD092 AD532 CC02 DD27 DD32 DD33 DD34 DD41 EE06 EE14 4C086 AA01 HAA16 HA17 MA02 MA04 MA08 MA17 MA63 NA05 NA14 ZA89 ZA91 4C206 AA01 AA02 CA05 MA02 MA04 MA05 MA30 MA83 ZA89 ZA91

Claims (4)

[Claims] (1) at least one selected from the group consisting of (A) sodium chloride, magnesium chloride, magnesium sulfate, calcium chloride, potassium chloride, sodium hydrogen carbonate, and sodium carbonate; and (B) at least one selected from polyhydric alcohols. A pharmaceutical composition for external use on the skin, comprising: 2. A pharmaceutical composition for external use on the skin, further comprising a nonionic surfactant. 3. A pharmaceutical composition for external use on the skin, further comprising a keratolytic agent. 4. The pharmaceutical composition for external use on the skin according to claim 1, which is a therapeutic agent for acne.