JP2020023467A - External preparation, method for improving liquid breaking properties, and agent for improving liquid breaking properties - Google Patents

Abstract

To improve liquid breaking properties of an external composition containing alcohol.SOLUTION: An external preparation has a container in which a member constituting a spout is at least partially composed of an elastomer, and an external composition stored in the container and containing minoxidil and alcohol.SELECTED DRAWING: None

Description

  The present invention relates to an external preparation, a method for improving liquid drainage, and a liquid drainage improving agent.

  Regarding the composition for external use, various studies have been made not only on the components contained therein, but also on the container to be contained from the viewpoint of stability and convenience of use. For example, Patent Literature 1 (JP-A-11-278529), Patent Literature 2 (JP-A-2002-337910), and Patent Literature 3 (JP-A-2006-036317) disclose a medicinal solution such as a medicinal hair restorer. A container that contains a cosmetic liquid or the like and that can discharge a used amount is disclosed.

JP-A-11-278529 JP-A-2002-337910 JP-A-2006-036317

  However, when an external composition containing alcohol is contained in a container provided with a spout made of a member made of plastic or the like, for example, there is a problem that the liquid composition of the external composition has a poor drainage property.

  An object of the present invention is to improve liquid drainage of an external composition containing alcohol.

  [1] An external preparation comprising: a container in which at least a part of a member constituting a spout is made of an elastomer; and an external composition containing minoxidil and alcohol contained in the container.

  [2] The external preparation according to [1], wherein the elastomer is at least one selected from a thermoplastic elastomer and a synthetic rubber.

  [3] The external use according to [2], wherein the thermoplastic elastomer is at least one selected from the group consisting of olefins, styrenes, esters, urethanes, amides, vinyl chlorides, and fluorines. Formulation.

  [4] The external preparation according to [2], wherein the synthetic rubber is a non-diene rubber.

  [5] The external preparation according to any of [1] to [4], wherein the concentration of minoxidil is 1 to 10 w / v%.

  [6] The external preparation according to any one of [1] to [5], wherein the alcohol contains a lower alcohol.

  [7] The external preparation according to any one of [1] to [6], wherein the alcohol contains a polyhydric alcohol.

  [8] The external preparation according to any one of [1] to [7], wherein the external composition further comprises an acid or a salt thereof.

  [9] The external preparation according to any one of [1] to [8], wherein the external composition has a pH of 5 to 8.

  [10] A method for improving the drainage property of the external composition to the elastomer by adding minoxidil to the external composition containing alcohol.

  [11] A liquid drainage improver containing minoxidil, which is added to the external composition to improve the liquid drainage property of the external composition containing alcohol to the elastomer.

  ADVANTAGE OF THE INVENTION According to this invention, the drainage property of the external composition containing alcohol can be improved.

It is a graph showing the increase rate of the contact angle of a composition for external use by addition of minoxidil.

<External preparation>
The external preparation of the present invention includes a container in which at least a part of a member constituting a spout is made of an elastomer, and an external composition containing minoxidil and alcohol contained in the container.

(container)
In the container used for the external preparation of the present embodiment, at least a part of the member constituting the spout is made of an elastomer. Thereby, the liquid drainage property of the composition for external use can be improved. The “spout port” is an opening formed at one end of the container and directly or indirectly communicating with the inside of the container for discharging the external composition inside the container. The “member forming the spout” is composed of at least one member including the periphery of the spout.

  In the member constituting the spout, it is preferable that at least a part of the periphery of the spout is made of an elastomer. In this case, the drainage property of the composition for external use can be more reliably improved. In order to further improve the drainage property, it is more preferable that the entire periphery of the spout is made of an elastomer.

  In addition, if the liquid drainage property of the external use composition is poor, for example, the components contained in the external use composition may be deposited around the spout, so that the external use composition remaining around the spout after use is used. In some cases, it is necessary to wipe off, but in the external preparation of the present embodiment, it is expected that such a problem hardly occurs.

  Further, among the members constituting the spout, when a portion (for example, a tip portion) that comes into contact with the application target of the external composition (for example, skin such as the scalp) is made of an elastomer, the rubber elasticity of the elastomer causes The application target such as the scalp is not damaged and pain is hardly caused, and a moderate stimulation is applied to the application target such as the scalp to obtain a massage effect. As described above, it is possible to provide an external preparation having an excellent feeling upon use.

  Note that the member forming the spout may be formed of a plurality of members. Specifically, for example, the container has a container main body in which an external composition is stored, an intermediate member having a communication hole provided in an opening of the container main body, and an opening ( And a tip member having an opening that indirectly communicates with the inside of the container body via the communication hole of the intermediate member), the member that forms the spout comprises the intermediate member and the tip member. You may. In this case, at least one of the opening of the tip member and the opening on the tip side of the communication hole of the intermediate member corresponds to a spout. Note that the tip member is a member that directly contacts the application target when the external composition is applied (applied), and the intermediate member may be a member that does not directly contact the application target. It is made of an elastomer, and the intermediate member may not be made of the elastomer.

Elastomer is a general term for industrial materials having rubber elasticity.
The elastomer is preferably at least one selected from a thermoplastic elastomer and a synthetic rubber. At least one selected from thermoplastic elastomers and synthetic rubbers can be used alone or in combination of two or more. In addition, for example, two or more kinds of thermoplastic elastomers may be used in combination.

  Thermoplastic elastomers are elastomers that have the property of softening when heated and exhibiting fluidity and returning to a rubbery state when cooled. The thermoplastic elastomer includes, for example, a hard segment corresponding to a crosslinking point of a vulcanized rubber and a soft segment exhibiting rubber elasticity. The thermoplastic elastomer is more preferably at least one selected from the group consisting of olefin-based elastomers, styrene-based elastomers, ester-based elastomers, urethane-based elastomers, amide-based elastomers, vinyl chloride-based elastomers, and fluorine-based elastomers, More preferably, it is at least one selected from the group consisting of olefin-based elastomers, styrene-based elastomers, and ester-based elastomers.

  The olefin-based elastomer is a thermoplastic elastomer (polymer) containing olefin as a constituent component. In the olefin-based elastomer, for example, the hard segment is made of an olefin-based resin (polypropylene or ethylene), and the soft segment is made of an olefin-based rubber (ethylene-propylene rubber or the like). Examples of the olefin-based elastomer include polyethylene; polypropylene; poly-1-butene; homopolymers such as polyisobutylene, propylene-ethylene copolymer; propylene-ethylene-1-butene copolymer; and propylene-1-butene copolymer. Polymer; ethylene-1-butene copolymer; ethylene-1-hexene copolymer; ethylene-1-octene copolymer; ethylene-propylene copolymer; ethylene-propylene-1-butene copolymer; ethylene- Copolymers such as a propylene-non-conjugated diene copolymer; an ethylene-1-butene-non-conjugated diene copolymer; and an ethylene-propylene-1-butene-non-conjugated diene copolymer. Olefin elastomers are excellent in terms of chemical resistance and odor.

  The styrene-based elastomer is a thermoplastic elastomer (polymer) containing styrene as a constituent component. In the styrene-based elastomer, for example, the hard segment is made of polystyrene, and the soft segment is made of a conjugated diene. Examples of the conjugated diene include butadiene, isoprene, chloroprene, and hydrogenated products thereof. Examples of the polystyrene-based elastomer include a styrene-butadiene copolymer, a styrene-ethylene-butadiene-styrene copolymer, a styrene-butadiene-butylene-styrene copolymer, and a styrene-isoprene-styrene copolymer. Styrene-based elastomers are inexpensive and have excellent chemical resistance.

  The ester-based elastomer is a thermoplastic elastomer (polymer) containing an ester as a constituent component. In the ester-based elastomer, for example, the hard segment is made of polyester, and the soft segment is made of polyether or polyester.

  The urethane-based elastomer is a thermoplastic elastomer (polymer) having a urethane structure. In the urethane-based elastomer, for example, the hard segment is made of diisocyanate, and the soft segment is made of polyol. Examples of the polyol include polyester, polyester ether, and polycarbonate.

  The amide-based elastomer is a thermoplastic elastomer (polymer) containing amide as a constituent component. The amide-based elastomer has, for example, a hard segment made of polyamide and a soft segment made of polyether or polyester.

  The vinyl chloride elastomer is a thermoplastic elastomer (polymer) containing vinyl chloride as a component. In the vinyl chloride elastomer, for example, the hard segment is made of polyvinyl chloride, and the soft segment is made of plasticized polyvinyl chloride, acrylonitrile butadiene rubber, and urethane rubber.

  The fluoroelastomer is a thermoplastic elastomer (polymer) containing fluorine as a constituent component. For example, the hard segment is made of a fluororesin and the soft segment is made of a fluororubber.

  Synthetic rubber is a synthetic polymer compound having physical and chemical properties similar to those of natural rubber. The synthetic rubber is preferably a non-diene rubber, and includes ethylene-propylene rubber, ethylene-propylene-diene rubber, butyl rubber, urethane rubber, silicone rubber, fluorine rubber, chlorosulfonated polyethylene, chlorinated polyethylene, acrylic rubber, and polysulfide. It is more preferably at least one selected from the group consisting of rubber and epichlorohydrin rubber, and even more preferably ethylene-propylene rubber or ethylene-propylene-diene rubber.

  Ethylene / propylene rubber is a synthetic rubber containing ethylene and propylene as constituent components.

  Ethylene propylene diene rubber is a synthetic rubber containing ethylene, propylene and diene as constituent components.

  Butyl rubber is a synthetic rubber containing isobutylene and isoprene as constituent components. Urethane rubber is a synthetic rubber having a urethane structure.

Silicone rubber is a synthetic rubber containing silicone as a constituent.
Fluororubber is a synthetic rubber containing fluorine as a constituent.

  Acrylic rubber is a synthetic rubber containing an acrylate or a methacrylate as a component.

  Polysulfide rubber is a synthetic rubber obtained by a condensation reaction of an organic halogen compound and an alkali polysulfide.

  Epichlorohydrin rubber is a synthetic rubber containing epichlorohydrin as a constituent.

  The shape of the container (main body, spout, cap, etc.) is not particularly limited, but can be appropriately selected in the art. The material of the members (main body, cap, inner plug, seal member, etc.) other than the member constituting the spout is also not particularly limited, and the storage stability of the composition for external use, the chemical resistance, strength, and flexibility of the container. It may be appropriately selected in consideration of the properties, weather resistance, and the like. Examples of such a material include polyethylene, polypropylene, polyethylene terephthalate, polystyrene, aluminum, polyvinyl chloride, ABS resin, ethylene-vinyl alcohol resin, acrylonitrile styrene resin, epoxy resin, polyamide imide resin, and glass. A laminate using these resins may be used as the material of the container.

(External composition)
The external composition used for the external preparation of the present embodiment contains minoxidil (including its salt) and alcohol.

  Minoxidil (including its salt) is a known compound, and as a method for obtaining minoxidil, a commercially available product may be used and can be purchased from, for example, Tokyo Chemical Industry Co., Ltd. Examples of the salt of minoxidil include inorganic acid salts such as hydrochloride and sulfate, and organic acid salts such as acetate, citrate, succinate, benzoate and lactate.

  The concentration of minoxidil is preferably 1 w / v% or more and 10 w / v% or less, more preferably 2 w / v% or more and 9 w / v% or less, and more preferably 3 w / v% based on the total amount of the composition for external use. % Or more, more preferably 8 w / v% or less, and most preferably 4 w / v% or more and 7 w / v% or less. Within this range, the effects of minoxidil (such as a hair-growth effect and an effect of improving liquid drainage properties) are easily exhibited, and minoxidil is not easily precipitated.

(solvent)
The composition for external use contains alcohol as a solvent. The alcohol preferably contains a lower alcohol, a polyhydric alcohol, or the like. Ethanol is preferred as the lower alcohol. As the polyhydric alcohol, glycols such as propylene glycol, dipropylene glycol and 1,3-butylene glycol, glycerin, macrogol 300, macrogol 400, macrogol 600 and the like can be used. 1,3-butylene glycol and glycerin are preferred, and propylene glycol and 1,3-butylene glycol are more preferred. Polyhydric alcohols can be used alone or in combination of two or more. The amount of each solvent in the composition for external use is not particularly limited, but the amount of the lower alcohol is preferably 20 to 70 w / v%, more preferably 35 to 60 w / v%, and still more preferably. 40 to 55 w / v%. The blending amount of the polyhydric alcohol is preferably 1 to 30 w / v%, more preferably 5 to 25 w / v%, and still more preferably 8 to 20 w / v%.

  The external composition may further contain water as a solvent. In the final composition, the amount of water is preferably 5 to 40 w / v%, more preferably 10 to 35 w / v%, and still more preferably 15 to 30 w / v%. Within this range, a composition for external use having good solubility of minoxidil and excellent feeling in use can be obtained.

(Fat-soluble antioxidant)
It is preferable that the composition for external use further contains a fat-soluble antioxidant from the viewpoint that the effect of the present invention is more remarkably exhibited. As the fat-soluble antioxidant, for example, dibutylhydroxytoluene and butylhydroxyanisole can be used.

  It is preferable that the composition for external use further contains an acid or a salt thereof from the viewpoint that the effects of the present invention are more remarkably exhibited. Examples of the acid or a salt thereof include lactic acid; sodium lactate; citric acid; sodium citrate; malic acid; sodium malate; succinic acid; sodium succinate; tartaric acid; sodium tartrate; gluconic acid; , Phosphoric acid; hydrochloric acid; and sulfuric acid. These acids may be used as a pH adjuster. Further, an organic base such as triethanolamine; diisopropanolamine; triisopropanolamine; arginine; and an inorganic base such as potassium hydroxide and sodium hydroxide can also be used as the pH adjuster. The above acids can be used alone or in combination of two or more.

  The pH of the composition for external use is preferably 5.0 or more, more preferably 5.5 or more, and even more preferably 6.0 or more, from the viewpoint that the effects of the present invention are more remarkably exhibited. The pH of the composition for external use is preferably 8.0 or less, more preferably 7.5 or less, and even more preferably 7.0 or less. Further, in the above range, minoxidil is easily dissolved, and irritation to the scalp due to high pH can be avoided.

  The composition for external use can further contain a pharmaceutically or physiologically acceptable active ingredient used for a pharmaceutical external preparation, a quasi-drug, cosmetics, and the like. Such active ingredients include pyridoxine hydrochloride, tocopherol acetate, 1-menthol, pantothenyl ethyl ether, panthenol, hinokitiol, diphenhydramine and its salts, or salicylic acid and its salts, glycyrrhizic acid and its salts, assembly extract, Carrot extract and the like. These active ingredients can be used alone or in combination of two or more. Among them, from the viewpoint of feeling of use, it contains at least one selected from pyridoxine hydrochloride, tocopherol acetate, l-menthol, pantothenyl ethyl ether, panthenol, hinokitiol, diphenhydramine and its salts, or salicylic acid and its salts. And more preferably at least one selected from pyridoxine hydrochloride, tocopherol acetate, 1-menthol, and pantothenyl ethyl ether.

  The composition for external use can contain a pharmaceutically or physiologically acceptable additive used for an external preparation for medicine, a quasi-drug, cosmetics and the like. Examples of such additives include antioxidants, surfactants, thickeners, preservatives, stabilizers, stimulants, preservatives, coloring agents, fragrances, and solubilizers. These additives can be used alone or in combination of two or more.

  The form of the composition for external use is not particularly limited, and examples thereof include solutions, suspensions, emulsions, creams, gels, liniments, lotions, aerosols and the like. In addition, an ointment can be used when the water contains enough water to dissolve minoxidil. Among these, liquids, suspensions, emulsions, lotions and aerosols are preferred, and liquids, lotions and aerosols are more preferred. The composition for external use can be produced, for example, by mixing the respective components in accordance with or in accordance with the general rules of the Japanese Pharmacopoeia. Further, the external composition may be a cosmetic composition such as a lotion, a cream, a lotion, an emulsion, a foam, a shampoo, a rinse, a conditioner, a hair tonic, a hair cream, and a hair liquid.

<How to improve drainage>
The present invention also relates to a method for improving the drainage property of an external composition to an elastomer by adding minoxidil to an external composition containing an alcohol. The composition of the composition for external use after the addition of minoxidil is the same as the composition for external use used in the above-mentioned external preparation. The elastomer is the same as the elastomer constituting the container used in the above-mentioned external preparation.

<Liquid drainage improver>
The present invention also relates to a liquid drainage improver containing minoxidil, which is added to an external composition to improve the liquid drainage of an external composition containing an alcohol to an elastomer. The composition of the external composition after the addition of minoxidil is the same as the external composition in the above-mentioned external preparation. The elastomer is the same as the elastomer constituting the container used for the above-mentioned external preparation.

  Hereinafter, the present invention will be described in more detail with reference to Examples, but the present invention is not limited thereto.

  External compositions (sample solutions 1 to 4 and control solutions 1 to 4) having the compositions shown in Table 1 were prepared according to a conventional method. The “appropriate amount” in Table 1 is an amount necessary to adjust the pH of the composition for external use to the value shown in Table 1.

For each of the following materials (Examples and Comparative Examples), the contact angles of the sample liquids 1 to 4 and the control liquids 1 to 4 were measured.
Example 1: Olefinic thermoplastic elastomer (TPO)
Example 2: Styrenic thermoplastic elastomer (TPS)
Comparative Example 1: Polyethylene (PE)
Comparative Example 2: Polypropylene (PP)
Comparative Example 3: Polyethylene terephthalate (PET)
In addition, "Mylastomer (registered trademark) 6030NS (Mitsui Chemicals)" was used as TPO, and "Elastomer AR-S-4925CL (Aron Kasei Co., Ltd.)" was used as TPS.

  The contact angle refers to the angle between the liquid surface and the solid surface at the place where the liquid contacts the solid surface. When the contact angle is large, it indicates that the water repellency is high and the liquid drainage property of the external use composition is good, and when the contact angle is small, it indicates that the liquid is difficult to repel and the liquid drainage property of the external use composition is poor.

  The contact angle was measured according to the following method. On a stage of a contact angle measuring device (manufactured by Kyowa Interface Science Co., Ltd., “Drop Master 500”), a plate having a smooth surface made of each of the materials of Examples 1 and 2 and Comparative Examples 1 to 3 was placed. 0.5 μL of the sample solution or the control solution was dropped on the plate, and after 0.5 seconds, the droplet was photographed with a digital camera from right beside the plate. In addition, the focus of the camera was adjusted to the portion where the droplet is in contact with the surface of the plate and the vertex of the droplet. The photographed image was analyzed using the analysis software “FAMAS” mounted on the contact angle measuring instrument, and the contact angle of the droplet was measured. The measurement was performed five times, and the respective average values were obtained.

Then, based on the following formula, the contact angle increase rate of each of the materials of Examples and Comparative Examples due to the addition of minoxidil was determined.
Contact angle increase rate by addition of minoxidil (%)
= [(Contact angle of sample solution / contact angle of control solution corresponding to sample solution) -1] × 100
The “target liquid corresponding to the sample liquid” is a target liquid having the same number as the sample liquid, and has the same composition as the sample liquid except that it does not contain minoxidil.

  FIG. 1 shows the measurement results of the contact angle increase rate of each sample solution with respect to each of the materials of the example and the comparative example.

  As shown in FIG. 1, the contact angles of the sample solutions 1-1 and 2-4 containing minoxidil and the sample solution 1-2 containing minoxidil and dibutylhydroxytoluene with respect to the elastomers of Examples 1 and 2 were minoxidil. Was higher than the contact angle of the control solution containing no. On the other hand, when the plastics of Comparative Examples 1 to 3 were used, the contact angle of the sample solution 1-1 containing minoxidil was almost the same as that of the control solution (Comparative Examples 1 and 2) or decreased. (Comparative Example 3). The contact angle of the sample solution 1-2 containing minoxidil and dibutylhydroxytoluene was lower than the contact angle of the control solution (Comparative Examples 1, 2, and 3). That is, when minoxidil is added to an external composition containing alcohol, the change in liquid drainage of the composition differs depending on the material. In the case of an elastomer such as an example, the liquid drainage of the external composition is improved. It can be seen that such a plastic cannot improve the drainage property of the composition for external use.

  Next, Table 2 shows the ratio of the contact angle of the sample solution to the material of each example and the comparative example when the contact angle of the sample solution to the material of Comparative Example 1 was 100%.

  As shown in Table 2, when the sample solution 1-1 containing minoxidil and the sample solution 1-2 containing minoxidil and dibutylhydroxytoluene (external composition) were used, the samples of Examples 1 and 2 were used. The contact angle with respect to the elastomer was significantly larger than the contact angles with respect to the plastics of Comparative Examples 1 to 3. That is, when the composition for external use containing alcohol contains minoxidil or minoxidil and dibutylhydroxytoluene, and the member forming the spout (around) contains an elastomer, the liquid drainage property is improved. There is expected.

  The embodiments and examples disclosed this time are to be considered in all respects as illustrative and not restrictive. The scope of the present invention is defined by the terms of the claims, rather than the description above, and is intended to include any modifications within the scope and meaning equivalent to the terms of the claims.

(Formulation example)
Each of the compositions for external use 1 to 48 shown in the following Tables 3 to 8 is filled in a container in which the tip of the member constituting the spout is made of an olefin-based elastomer and the container body is made of polyethylene terephthalate. 1 to 48 were each manufactured. Each of the compositions for external use 1 to 48 was filled in a container in which the tip of the member constituting the spout is made of a styrene-based elastomer and the container body was made of polyethylene terephthalate, to produce formulations 49 to 96, respectively. Each of the compositions for external use 1 to 48 was filled in a container whose tip portion of the spout is made of ethylene propylene diene rubber and whose container body was made of polyethylene terephthalate, to produce formulations 97 to 144, respectively. The unit of each component in Tables 3 to 8 is w / v%.

Claims (12)

  An external preparation comprising: a container in which at least a part of a member constituting a spout is made of an elastomer; and an external composition containing minoxidil and alcohol contained in the container.   The external preparation according to claim 1, wherein the elastomer is at least one selected from a thermoplastic elastomer and a synthetic rubber.   The external preparation according to claim 2, wherein the thermoplastic elastomer is at least one selected from the group consisting of olefins, styrenes, esters, urethanes, amides, vinyl chlorides, and fluorines.   The external preparation according to claim 2, wherein the synthetic rubber is a non-diene rubber.   The topical preparation according to any one of claims 1 to 4, wherein the concentration of minoxidil is 1 to 10 w / v%.   The external preparation according to any one of claims 1 to 5, wherein the alcohol contains a lower alcohol.   The external preparation according to any one of claims 1 to 6, wherein the alcohol contains a polyhydric alcohol.   The external preparation according to any one of claims 1 to 7, wherein the external composition further comprises a fat-soluble antioxidant.   The external preparation according to any one of claims 1 to 8, wherein the external composition further comprises an acid or a salt thereof.   The external preparation according to any one of claims 1 to 9, wherein the external composition has a pH of 5 to 8.   A method for improving the drainage property of an external composition to an elastomer by adding minoxidil to an external composition containing an alcohol.   A liquid releasability improving agent containing minoxidil, which is added to the external composition for improving the liquid releasability of the external composition containing alcohol to the elastomer.