JP2001097848A - Preparation composition for external use - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation composition which is used for external use, has excellent adhesivity to diseased skin parts and excellent coverability, whose coating films covering the diseased parts can rapidly be washed out, can prevent the suppuration of the diseased parts due to the infection of bacteria, and can further promote the hemostasis and dryness of the diseased parts to lead to the early restoration and recovery of the wounds. SOLUTION: This preparation composition for external use contains a hydrophilic colloidal water-soluble polymer such as Arabian gum or alginic acid and a liquid hydrocarbon compound such as propane, pentane or caster oil.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation composition used for affected skin. More specifically, it is an external preparation that can quickly form a film by spraying on the affected area of the skin and dry protect the affected area infiltrated with sweat, blood or body fluid, and that the film can be easily washed off with water. And an external preparation composition.

[0002]

2. Description of the Related Art Conventionally, local astringents such as zinc oxide have been used for the purpose of absorbing exudates (blood and lymph) from the wound surface and ulcer surface of the skin, forming a film on the affected part and protecting it from drying. Such astringents are useful drug components in that they provide early repair of trauma lesions by covering and protecting the infiltrated lesions to promote drying and preventing suppuration due to bacterial infection.

[0003] However, it has been pointed out that zinc oxide adhering to the skin cannot be easily removed simply by washing it away with running water or the like. In addition, zinc oxide has a problem that hands and the like become dirty when used.

[0004]

DISCLOSURE OF THE INVENTION The present invention has been made to solve the above-mentioned problems, and an object of the present invention is to provide an astringent action and an affected area protective action which can be used in a sanitary manner without soiling hands and clothing during use. And an external preparation composition having an effect of healing the affected area, and a skin external preparation comprising the composition. Furthermore, an object of the present invention is an external preparation composition which forms a film on an affected area by spraying on the affected area, thereby promoting hemostasis and drying of the affected area, thereby promptly repairing a wound. It is an object of the present invention to provide a composition for external use in which the formed film can be easily washed away with water or warm water, and a skin external preparation comprising the composition.

[0005]

SUMMARY OF THE INVENTION The present inventors have developed a water-soluble polymer, particularly a hydrophilic colloid, when developing an external preparation for skin which is effective for wounds, abrasions, etc., which are accompanied by blood flow or exudation of body fluids and skin diseases. It has been found that the above problem can be solved by using a composition containing a water-soluble polymer having a liquid state and a liquid hydrocarbon compound as an external preparation composition.
The present invention is based on this finding.

That is, the present invention is an external aerosol preparation comprising any one of the following embodiments. (1) An external preparation composition comprising a hydrophilic colloidal water-soluble polymer and a liquid hydrocarbon compound. (2) The hydrophilic colloid-like water-soluble polymer is at least one selected from the group consisting of gum arabic, alginic acid, guar gum, gelatin, tara gum, starch, tragacanth, phasellane, pectin and salts thereof (1 The external preparation composition according to (1). (3) The liquid hydrocarbon compound is propane, pentane, hexane, butane, castor oil, triglyceride, lanolin,
Squalane, squalene, dimethyl ether, glycerin, sunflower oil, eucalyptus oil, turpentine oil, cocoa oil,
The external preparation composition according to (1) or (2), which is at least one selected from the group consisting of rose oil and isopropyl myristate.

(4) Further, as components which can be expected to have medicinal effects, acrinol, isopropanol, benzalkonium chloride, benzethonium chloride, dilute tincture, chlorhexidine gluconate, ethanol, povidone iodine, mercurochrome, isopropylmethylphenol, ethyl aminobenzoate, glycyrrhetinic acid , Indomethacin,
Prednisolone valerate acetate, ketoprofen, bufexamac, hydrocortisone, thymol, piroxicam,
Felbinac, nonanilic acid vanillylamide, glycol salicylate, salicylic acid, allantoin, dipotassium glycyrrhizinate, tocopherol acetate, lidocaine, sulfur, cetylpyridinium chloride, chlorpheniramine maleate, dibucaine hydrochloride, naphazoline hydrochloride, iodine,
Diphenhydramine, diphenhydramine hydrochloride, alum, L-menthol, DL-menthol, DL-camphor, pyridoxine hydrochloride, urea, vitamin A oil, benzyl nicotinate, crotamiton, capsicum tincture, peppermint oil, undecylenic acid, zinc undecylenate, exalamide, black Trimazole, miconazole nitrate, econazole nitrate, thioconazole, zinc diethyldithiocarbamate, thiantol, tolcyclate, tolnaphthalate, haloprosin, berberine benzoate, hinokitiol, chlorhexidine hydrochloride, diphenylimidazole,
D-camphor, diethyl phthalate, chlorohydroxyaluminum, chitosan, turpentine, ascorbic acid,
The external preparation according to any one of (1) to (3), comprising at least one selected from the group consisting of olive oil and epsilon-aminocaproic acid in a proportion of 0.01 to 50% by weight. Composition.

(5) Further, mannitol,
Glucose, chitin, anhydrous silicon, hydrated silicon, fructose, lactose, sucrose, sucrose, sodium stearate, aspartame, sorbitol, xylitol, stevioside,
Shellac, titanium oxide, sodium chloride, talc, macrogol, tannic acid, sodium copper chlorophyllin,
(1) to (4), wherein at least one selected from the group consisting of potassium iodide, methylsiloxane, and isopropyl alcohol is contained at a ratio of 0.01 to 50% by weight; External preparation composition.

[0009]

BEST MODE FOR CARRYING OUT THE INVENTION The external preparation composition of the present invention comprises a drug composition having excellent adhesion and covering properties to the skin and formed on the affected area of the skin based on the components contained therein and the composition thereof. The coating has the characteristic that it can be quickly washed away with water.

As a composition exhibiting the above-mentioned properties, there can be mentioned a composition containing a water-soluble polymer and a liquid hydrocarbon compound.

The water-soluble polymer is not particularly limited as long as it is a water-soluble polymer compound which can be applied to the skin or mucous membranes. Preferably, the water-soluble polymer absorbs water relatively easily. A hydrophilic colloid-like water-soluble polymer having a property of swelling to form a hydrogel can be used. According to such a water-soluble polymer, it absorbs bodily fluids such as sweat and blood and lymph leached at wounds and the like, and swells thereby, and distributes and adheres the drug composition on the skin or mucous membrane, At the same time, the release rate of the medicinal component contained in the drug composition can be controlled.

Suitable hydrophilic colloidal water-soluble polymers include untreated starches such as corn starch and potato starch, carboxylated starches such as trapa starch, carboxymethyl starch and corn swollen starch, and sodium starch glycolate. Various starches including starch derivatives; seaweed polysaccharides such as carrageenan; seed polysaccharides such as guar gum, carob bean gum, tara gum and tamarind seed gum; resin polysaccharides such as arabic gum, tragacanth gum and karaya gum; pericarp polysaccharides such as pectin; xanthan gum; Fermented polysaccharides such as gellan gum, curdlan and pullulan; mannans such as galactomannan and glucomannan; and various thickening polysaccharides (swellable polysaccharides) such as phasellan and derivatives thereof Proteinaceous gelling agent such as gelatin and glue, cellulose and carboxymethyl cellulose sodium, methyl cellulose, ethyl cellulose,
Cellulose derivatives such as hydroxyethylcellulose, hydroxyethylmethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose; alginic acid, salts of alginic acid such as sodium alginate and calcium alginate, and alginic acid derivatives such as propylene glycol alginate; alginic acid derivatives such as propylene glycol alginate; polyvinyl Examples include synthetic swellable polymers such as alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, polyacrylic acid, polymethacrylate, and hydroxyethyl methacrylate, and derivatives thereof.

Among them, polysaccharides such as gum arabic, guar gum, cod gum, tragacanth, facellulan and pectin and salts thereof, proteinaceous gelling agents such as gelatin, alginic acid, sodium alginate,
Examples thereof include propylene glycol alginate, starch and derivatives thereof.

These hydrophilic colloidal water-soluble polymers can be used alone or in any combination of two or more. The mode of combination is not particularly limited, but preferably, gum arabic, guar gum, cod gum, tragacanth, facellulan, pectin, gelatin, alginic acid or salts thereof (sodium alginate, propylene glycol alginate) and water-soluble polysaccharides of starch are each optional. For example, the two types of combinations include all 36 combinations of the above components.

The mixing ratio of these water-soluble polymers is not particularly limited and can be appropriately selected and used. Preferably, the mixing ratio is 0.0% per 100% by weight of the external preparation composition (total amount).
The ratio can be 1 to 90% by weight, more preferably 5 to 60% by weight.

In the present invention, as the liquid hydrocarbon compound, conventionally known liquid compounds used in the field can be widely mentioned. Specifically, olive oil, jojoba oil, castor oil, camellia oil, evening primrose oil, sunflower oil, safflower oil, peanut oil, squalane, guinea pig oil, avocado oil, sunflower oil, eucalyptus oil, turpentine oil, cacao oil,
Vegetable oils such as rose oil, corn oil, rapeseed oil, cottonseed oil, coconut oil and poppy oil; animal oils such as tallow, lard, wool oil, lanolin; minerals such as petrolatum, paraffin, silicone oil, squalane, squalene Oils; fatty acid esters such as glycerin and triglyceride, isopropyl myristate, seil isooctanoate, n-butyl myristate, isopropyl linoleate, propyl ricinolate, isopropyl ricinolate, isobutyl linoleate, heptyl ricinolate, diethyl sebacate, Diisopropyl adipate, cetyl alcohol, stearyl alcohol, behenyl alcohol, batyl alcohol, kimyl alcohol, salami beeswax, whale wax,
Higher fatty acid esters such as water wax, higher fatty alcohols and waxes; higher fatty acids such as stearic acid, oleic acid and palmitic acid; mono-, di-, and triglyceride mixtures of saturated or unsaturated fatty acids having 12 to 18 carbon atoms; dimethyl ether And propane, pentane, hexane, and butane.

Preferably, it is a component having high biocompatibility, which is highly safe for living bodies, especially skin, and specifically, castor oil, triglyceride, lanolin, squalane, squalene, dimethyl ether, glycerin, sunflower oil, eucalyptus oil. , Turpentine, cocoa oil, rose oil, isopropyl myristate, propane, pentane,
Hexane and butane can be mentioned.

In the present invention, these liquid hydrocarbon compounds may be used alone or in any combination of two or more. The mode of combination is not particularly limited, but preferably oily components 1 or 2 such as castor oil, triglyceride, lanolin, squalane, squalene, dimethyl ether, glycerin, sunflower oil, eucalyptus oil, turpentine oil, cocoa oil, rose oil and isopropyl myristate. And above, propane,
Combinations with one or more of pentane, hexane and butane can be mentioned. For example, as the combination of the two types, 52, such as the former oil component and the latter propane, is used.
All possible combinations can be mentioned.

The mixing ratio of these liquid hydrocarbon compounds is not particularly limited and may be appropriately selected and used, but is preferably 1 to 80% by weight, more preferably 1 to 80% by weight, per 100% by weight of the external preparation composition (total amount). May have a ratio of 2 to 50% by weight.

The external preparation composition of the present invention further comprises, in addition to the above-mentioned components, saccharides such as mannitol, glucose, fructose, lactose, sucrose, sucrose, aspartame, sorbitol, xylitol, stevioside, sodium stearate, shellac, chitin, Anhydrous silicon, hydrated silicon, titanium oxide, sodium chloride, talc, macrogol, tannic acid, copper copper chlorophyllin, potassium iodide, methyl siloxane, isopropyl alcohol, and the like can be added. These may be used alone or in any combination of two or more.

The mixing ratio of these components is not particularly limited and can be appropriately selected and used, but is preferably 0.01 to 50% by weight, more preferably 1 to 50% by weight, per 100% by weight of the external preparation composition (total amount). To 30% by weight.

The external preparation composition of the present invention is not particularly limited as long as it contains the above-mentioned components as components, and may be appropriately selected according to the intended use and the indication disease. Can be used for selection.

For example, the active ingredients generally formulated as an external preparation for the treatment of skin wounds include well-known external pharmaceutical ingredients such as disinfectants / disinfectants, local anesthetics, anti-inflammatory agents, corticosteroids, and antibiotics. And an auxiliary component such as an absorption enhancer or a healing enhancer.

[0024] For example, the ingredients to be blended with the expectation of medicinal effect include acrinol, isopropanol, benzalkonium chloride, benzethonium chloride, dilute tincture, chlorhexidine gluconate, ethanol, povidone iodine, mercurochrome, isopropylmethylphenol, ethyl aminobenzoate, Glycyrrhetinic acid, indomethacin, prednisolone acetate valerate, ketoprofen, bufexamac, hydrocortisone, thymol, piroxicam, felbinac, vanillyl amide nonanoate,
Glycol salicylate, salicylic acid, allantoin, dipotassium glycyrrhizinate, tocopherol acetate, lidocaine, sulfur, cetylpyridinium chloride, chlorpheniramine maleate, dibucaine hydrochloride, naphazoline hydrochloride, iodine, diphenhydramine, diphenhydramine hydrochloride, alum, L-menthol, DL- Menthol, DL-camphor, pyridoxine hydrochloride, urea, vitamin A oil, benzyl nicotinate, crotamiton, peppermint tincture, peppermint oil, undecylenic acid, zinc undecylenate, exalamide, clotrimazole, miconazole nitrate, econazole nitrate, thioconazole, diethyldithiocarbamine Zinc acid, thiantol, tolcyclate, tolnaftate, haloprosin, berberine benzoate, hinokitiol, Chlorhexidine, diphenyl imidazole, D- camphor, diethyl phthalate, aluminum chlorohydrate, chitosan, turpentine,
Ascorbic acid, olive oil, epsilon-aminocaproic acid and the like can be exemplified. These may be used singly or in any combination of two or more depending on the purpose.

The compounding ratio of these medicinal components is not particularly limited and can be appropriately selected and used, but preferably 0.01 to 5 per 100% by weight of the external preparation composition (total amount).
0% by weight, more preferably 0.05 to 10% by weight.

Further, the external preparation composition of the present invention may contain optional components in addition to the above components as long as the effects of the present invention are not impaired. Examples of the optional component include a carrier, a base, a solvent, and various additives used for a pharmaceutical preparation for external use, and specific examples thereof include a lubricant such as magnesium stearate and ethanol, isopropyl alcohol and the like. Solvents such as alcohols and isopropyl myristate, and other additives such as adhesion improvers, stabilizers, preservatives, dissolution aids, emulsifiers, suspending agents, and pH adjusters are exemplified.

The external preparation composition of the present invention is further filled into a sprayer or a spray container together with a propellant, if necessary.
It can be prepared as an aerosol or spray.

The propellant is not particularly limited as long as it does not affect the base component and the medicinal component used in the present invention and is pharmaceutically acceptable. Any of those usually used in the art can be used. Can also be used.

Specifically, fluorinated hydrocarbons and fluorocarbons;
Liquefied gas such as liquefied petroleum gas, pentane gas, dimethyl ether or the like containing at least one of propane, normal butane and isobutane; carbon dioxide; nitrogen gas. A liquefied petroleum gas containing at least one of propane, normal butane and isobutane, and a liquefied gas such as dimethyl ether, more preferably a liquefied petroleum gas. The liquefied petroleum gas usually contains propane, normal butane or isobutane alone or in combination of two or more, and contains 90% by weight or more, preferably 95% or more, and contains pentane gas and the like as other components. Is also good.

In the composition for external use of the present invention, the mixing ratio (weight ratio) of the drug component and the propellant is not particularly limited, but is usually 1: 1 to 50, preferably 1: 1 to 1: 1.
0, more preferably 1: 4 to 9.

The external preparation composition of the present invention has a hygroscopic action and an astringent action based on each component contained in the composition and its composition, and adheres to an affected part infiltrated by blood and lymph effusion. By quickly forming a film, the affected part is dried and protected, and in addition to the action of the medicinal component incorporated therein, early healing of the affected part wound and various diseases can be promoted. In addition, the composition for external use of the present invention is characterized in that a film formed by applying (discharging and spraying) the agent to the affected area of the skin can be easily washed off with water or hot water based on its components and its composition. .

The external preparation composition of the present invention is prepared in any dosage form generally used for external preparations without any particular limitation on the dosage form. Specific examples of the dosage form include solutions, suspensions, emulsions, lotions, ointments, creams, sprays, aerosols, foams, patches, plasters, and the like. Above all, according to a dosage form such as a spray, an aerosol, and a foam, there is no risk of soiling the hands at the time of application of the medicine, and since the application does not involve other tools, it can be used hygienically until the end.

The amount of the composition for external use of the present invention to be used varies depending on the kind of the disease, the degree of the symptom, and the size of the affected part, and cannot be specified unconditionally, but is usually used in the range of about 0.01 to 10 g per day. It can be applied to the affected area once a day or at appropriate times.

[0034]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to Examples and Experimental Examples, but the present invention is not limited to the Examples and the like. In addition,% described below means% by weight unless otherwise specified. Example 1 Starch 40% Castor oil 10% Sucrose 48% Acrinol 2% Total 100% A composition comprising the above formulation was mixed and prepared to prepare an external preparation composition of the present invention.

Example 2 Gelatin 10% Tara gum 5% Squalane 20% Isopropyl methyl phenol 4% Chitin 1% Fructose 20% Liquefied butane gas 40% Total 100% Of the above formulation, components other than liquefied butane gas are mixed and prepared. The obtained composition was charged into a nebulizer together with liquefied butane gas to prepare an external preparation composition of the present invention in the form of an aerosol.

Example 3 Benzethonium chloride 1% Diphenhydramine hydrochloride 1% Triglyceride 15% Starch 15% Xylitol 20% Liquefied propane gas 48% Total 100% Of the above formulation, components other than liquefied propane gas were mixed and prepared. The obtained composition was charged into a sprayer together with liquefied propane gas to prepare an external preparation composition of the present invention in the form of an aerosol.

Comparative Example 1 Benzethonium chloride 1% Diphenhydramine hydrochloride 1% Starch 20% Xylitol 30% Liquefied propane gas 48% Total 100% Of the above formulation, components other than liquefied propane gas were mixed and prepared. The product was charged into a sprayer together with liquefied propane gas to prepare an external preparation composition of Comparative Example in the form of an aerosol.

EXPERIMENTAL EXAMPLE 1 As a test agent, the external preparation composition of the present invention prepared in Examples 1 to 4 was used by 60 volunteers to give a feeling of use (stickiness and stiffness) and a coating property (adhesion) on the skin. Properties, film strength), detergency of the film, and irritation to the skin (biocompatibility) were evaluated on a five-point scale of "good, moderately good, ordinary, slightly poor, bad". Table 1 shows the results.
In the table, ○, Δ, and × are based on the following criteria, respectively.

：: Both “bad” and “slightly bad” are 0%.

Δ: “bad” is 40% or less, or “slightly bad” is 40% or less ×: “bad” is 40% or more or “slightly bad” is 40
%that's all

[0041]

[Table 1]

From these results, it was found that the external preparation composition of the present invention was excellent in film-forming property and adhesiveness, was excellent in washing and removing properties, was less irritating to the skin, and was excellent in usability.

[0043]

The external preparation composition of the present invention, which contains a hydrophilic colloid-like water-soluble polymer and a liquid hydrocarbon compound, has excellent adhesiveness and coatability of the drug composition to the skin, and This has the effect that the coating formed of the drug composition formed on the affected area of the skin can be quickly washed away with water.

 ──────────────────────────────────────────────────続 き Continuing on the front page (72) Inventor Yuji Tsuji 3-13-35, Mitsujinaminami, Yodogawa-ku, Osaka, Osaka Prefecture (72) Inventor Hideki Shirogane 3-13 Mitsuyaminami, Yodogawa-ku, Osaka, Osaka −35 F-term in Kobayashi Pharmaceutical Co., Ltd.

Claims (5)

[Claims] An external preparation composition comprising a hydrophilic colloidal water-soluble polymer and a liquid hydrocarbon compound. 2. The hydrophilic colloidal water-soluble polymer is at least one selected from the group consisting of gum arabic, alginic acid, guar gum, gelatin, tara gum, starch, tragacanth gum, phasellan, pectin, and salts thereof. The external preparation composition according to claim 1. 3. A liquid hydrocarbon compound comprising propane, pentane, hexane, butane, castor oil, triglyceride, lanolin, squalane, squalene, dimethyl ether,
The external preparation composition according to claim 1 or 2, wherein the composition is at least one selected from the group consisting of glycerin, sunflower oil, eucalyptus oil, turpentine oil, cocoa oil, rose oil, and isopropyl myristate. 4. A component which can be expected to have a medicinal effect, such as acrinol, isopropanol, benzalkonium chloride,
Benzethonium chloride, dilute tincture of tin iodine, chlorhexidine gluconate, ethanol, povidone iodine, mercurochrome, isopropylmethylphenol, ethyl aminobenzoate, glycyrrhetinic acid, indomethacin, prednisolone valerate acetate, ketoprofen, bufexamac, hydrocortisone, thymol, piroxicam, felbinac, nonanoic amide , Glycol salicylate, salicylic acid, allantoin, dipotassium glycyrrhizinate, tocopherol acetate, lidocaine, sulfur,
Cetylpyridinium chloride, chlorpheniramine maleate, dibucaine hydrochloride, naphazoline hydrochloride, iodine, diphenhydramine, diphenhydramine hydrochloride, alum, L-menthol, DL-menthol, DL-camphor, pyridoxine hydrochloride, urea, vitamin A oil, benzyl nicotinate, Crotamiton, Pepper tincture, peppermint oil, undecylenic acid, zinc undecylenate, exalamide, clotrimazole, miconazole nitrate, econazole nitrate, thioconazole, zinc diethyldithiocarbamate, thianthol, tolcyclate, tolnaftate, haloprosin, berberine benzoate, hinokitiol hydrochloride Chlorhexidine, diphenylimidazole,
D-camphor, diethyl phthalate, chlorohydroxyaluminum, chitosan, turpentine, ascorbic acid,
The olive oil and at least one selected from the group consisting of epsilon-aminocaproic acid are contained at a ratio of 0.01 to 50% by weight.
An external preparation composition according to any one of the above. 5. The composition further comprises mannitol, glucose, chitin, anhydrous silicon, hydrated silicon, fructose, lactose, sucrose, sucrose, sodium stearate, aspartame,
At least one selected from the group consisting of sorbitol, xylitol, stevioside, shellac, titanium oxide, sodium chloride, talc, macrogol, tannic acid, copper chlorophyllin sodium, potassium iodide, methylsiloxane, and isopropyl alcohol;
The external preparation composition according to any one of claims 1 to 4, wherein the composition is contained at a ratio of 1 to 50% by weight.