[0001]The present invention is a skin external solid substrate containing a lipid peptide-type compound, preferably a stick Jomotozai excellent in high temperature stability, and containing lipids useful peptide-type compound as a premix material of the skin external solid substrate for It relates to an aqueous composition.
Background technique
[0002]
　Solid composition Aqueous and the high coolness on application to the skin such as obtained, without any stickiness after use compared to solid compositions oily, etc. It is feeling and kidnapping, cosmetics a variety of products on the market to for etc., have been proposed.
　Conventionally as an aqueous solid composition, solid oil-in-water makeup cosmetic containing water and a fatty acid soap and oil and powder (Patent Document 1), alkyl and / or alkenyl oligoglycosides, oily substance, and the nonionic emulsifier stick aqueous cosmetic containing (Patent Document 2) are proposed.
[0003]
　As a kind of the aqueous solid composition include aqueous gel composition. This as an additive to obtain an aqueous gel polymer gelling agent and a low-molecular gelling agents, such as, various compounds have been proposed. For example recent years, biological low molecular gelling agent for lipid peptide-type expansion is expected to high safety medical materials and the like have been proposed.
CITATION
Patent Literature
[0004]
Patent Document 1: JP-A-3-279319 JP
Patent Document 2: JP-T 2002-516818 Patent Publication
Summary of the Invention
Problems that the Invention is to Solve
[0005]
　Aqueous gel obtained using the above lipid peptide-type low molecular gelling agents is relatively rupture strength is low, difficult to certain applications where strength is required, such as the product development to stick the skin external solid substrate such as Met. Further, the solid base material of the external skin, in its usage situation, often including in the midsummer car, but be kept at a high temperature above 50 ° C. is assumed, for example, the aforementioned lipid peptide-type low molecular gelling in the case of aqueous gel obtained by using the agent, not be maintained solid state under these high-temperature environment, it may function and appearance of the product is impaired, ensuring the stability of the substrate with respect to temperature (heat) is important It was a problem.
　The present invention has been made based on the above circumstances, an object to be its resolution, the breaking strength that can be used to stick the base material or the like is high, provides excellent skin external solid substrate thermostability It is to be.
Means for Solving the Problems
[0006]
　The present inventors have formed a hydrogel from result of extensive studies to solve the above problems, a low-molecular lipid peptide or lipid peptide-type compound that consists pharmaceutically usable salts (gelling agent) and water when found that the higher monohydric alcohol gels by appropriate amounts thermal stability skin external solid substrate with dramatically improved, gel particularly suitably used as a stick-shaped base material obtained, the invention was allowed to complete.
[0007]
　Namely, the present invention provides, as a first aspect, a surfactant and water, formula (1) to lipid peptide comprising at least one of a compound or a pharmaceutically usable salt of the formula (3) and type compound, and a monohydric alcohol of at least one saturated or unsaturated carbon atoms 8 to 30, relates to skin external solid substrate.
[Chemical formula 1]

(In the formula, R 1 represents an aliphatic group having a carbon number of 9 to 23, R 2 is a hydrogen atom, or a number of 1 to carbon atoms which may have a branched chain carbon atoms 1 or 2 represents 4 alkyl, R 3 is - (CH 2 ) n represents an -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom 1 or represents a fused heterocyclic ring composed of three 5-membered may have ring or 6-membered ring or 5-membered ring and 6-membered ring.)
[formula 2]

(wherein, R 4 is a carbon number of 9 to 23 represents an aliphatic group, R 5 to R 7 each independently represent hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain carbon atoms 1 or 2, or - (CH 2 ) n represents -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 Yes From then may 5- or 6-membered ring or 5-membered ring and 6-membered ring represents a fused heterocyclic ring composed.)
[Formula 3]

(wherein, R 8 is an aliphatic group having a carbon number of 9 to 23 represents, R 9 to R 12 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain carbon atoms 1 or 2, or - (CH 2 ) n a -X group represents, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or 5-membered nitrogen atom may have 1 to 3 rings or 6-membered ring or 5-membered ring and 6-membered represents a fused heterocyclic ring composed of ring.)
　as a second aspect, 1,2-alkane further comprising a diol or 1,3-alkanediol, to a skin external solid substrate according to the first aspect.
　As a third aspect, further comprising at least one fatty acid, about skin external solid substrate according to the first aspect or the second aspect.
　As a fourth aspect, the different from the 1,2-alkanediol or 1,3-alkanediols, further comprising a polyhydric alcohol of at least one, related to a skin external solid substrate according to the second aspect or third aspect.
　As a fifth aspect, the surfactant is, ethylene glycol alkyl ethers, phospholipids, one or more compounds selected from the group consisting of polyglycerol fatty acid esters and polyoxyethylene polyoxypropylene alkyl ether, a first aspect to about skin external solid substrate according to any one of the fourth aspect.
　A sixth aspect, wherein the fatty acid is stearic acid, about skin external solid substrate according to any one of the third aspect to the fifth aspect.
　As a seventh aspect, the polyhydric alcohol is glycerin, propylene glycol or polyethylene glycol, about a skin external solid substrate according to any one of the fourth aspect to sixth aspect.
　As an eighth aspect, further comprising at least one oily base, to a skin external solid substrate according to any one of the first aspect to the seventh aspect.
　As a ninth aspect, further comprising at least one organic acid, to a skin external solid substrate according to any one of the first aspect to the eighth aspect.
　A tenth aspect, a cosmetic or pharmaceutical, to a skin external solid substrate according to any one of the first aspect to the ninth aspect.
　An eleventh aspect, a stick, to the skin external solid material according to any one of the first aspect to the tenth aspect.
　As a twelfth aspect, a surfactant and water, and the equation (1) to the compound represented by formula (3) or lipid peptide-type compound consisting of at least one of its pharmaceutically usable salts, carbon and a monohydric alcohol of at least one saturated or unsaturated atoms 8 to 30, relates to an aqueous composition.
　As a thirteenth aspect, 1,2-alkane further comprising a diol or 1,3-alkanediol, an aqueous composition according to the twelfth aspect.
　As a fourteenth aspect, further comprising at least one fatty acid, an aqueous composition according to the twelfth aspect or the thirteenth aspect.
　As a fifteenth aspect, wherein different from the 1,2-alkanediol or 1,3-alkanediols, further comprising a polyhydric alcohol of at least one, related to the aqueous composition according to the thirteenth aspect or the fourteenth aspect.
　As a sixteenth aspect, the surfactant is, ethylene glycol alkyl ethers, phospholipids, one or more compounds selected from the group consisting of polyglycerol fatty acid esters and polyoxyethylene polyoxypropylene alkyl ether, a twelfth aspect or an aqueous composition according to any one of the fifteenth aspect.
　As a seventeenth aspect, a premix for the preparation of a skin external solid substrate, an aqueous composition according to any one of the twelfth aspect to the sixteenth aspect.
　As eighteenth aspect, comprising a surfactant and water, and the equation (1) to the compound represented by formula (3) or at least one consisting of a lipid peptide-type compound of the pharmaceutically usable salts heating step of the mixed system is heated to a temperature below room temperature over 100 ° C.,
followed by the heated said mixing system with the addition of monohydric alcohol of at least one saturated or unsaturated carbon atoms 8 to 30, the 12 aspect to the preparation step of preparing an aqueous composition according to any one of the seventeenth aspect,
the aqueous phase is heated to a temperature below 100 ° C. above room temperature, it was added an aqueous composition prepared above, mixing to, or to the aqueous composition prepared above, was added an aqueous phase which is heated to a temperature below room temperature or above 100 ° C., mixed, the mixing step, and
the mixture obtained in the mixing step is cooled, the gel cooling step to form
Including method of skin external solid substrate according to the first aspect.
　As a nineteenth aspect, in the mixing step, further adding solution of the drug, a method of manufacturing according to the eighteenth aspect.
Effect of the invention
[0008]
　It can provide skin external solid substrate excellent in thermal stability by the present invention. As And further effect, a 1,2-alkanediol or 1,3 alkane diol as a solubilizer of a lipid peptide-type compound, by further adding a surfactant, has a much higher breaking strength than conventional gel is obtained. A preferred embodiment of the present invention, the strength as compared with conventional aqueous gel base material is high and can provide a weakly acidic skin external solid substrate of about pH 5.
　The present invention is a gel-like substrate that can achieve a high water content that approximately 90 wt%, also an effect that the oil component can also be compounded simultaneously.
[0009]
　The lipid peptide compounds contained in the skin external solid substrate of the present invention is a highly safe artificial low molecular compound composed of only lipid and a peptide. Also the compounds, for example it is possible to form an aqueous gel without the use of a previously proposed crosslinking agent was required during the formation of the synthetic polymer gel are such, non-in the resulting skin external solid substrate problem remaining unreacted substances such as reaction of the crosslinking agent does not occur.
　In addition, each main component of the additives in skin external solid substrate of the present invention is a food and cosmetics, a general-purpose additives as an additive for pharmaceuticals.
　That is, the skin external solid substrate of the present invention has high biological safety, in particular, a medical material, or from the viewpoint of high safety required in cosmetic materials, very useful in the above applications.
　Skin external solid substrates Moreover the present invention, since good coolness, also without or broken or deformed, be a stretch good substrate is expected when applied to the human skin, such as cosmetics as use base or pharmaceutical base material, in particular very useful as a stick-shaped substrate.
[0010]
　Further, the present invention is suitable as a premix material of the skin external solid substrate for, it is possible to provide an aqueous composition.
　The present invention by using the above aqueous composition, in particular, in the case of large amount of organic acids, such as ascorbic acid also a gel-like skin external solid substrate having a strength required as a stick-shaped substrate It can be provided.
　The present invention, by appropriate amounts of alkyl alcohol, even better able to maintain a solid state at high temperature that may occur in daily life, can provide a solid base material which is excellent in storage stability.
DESCRIPTION OF THE INVENTION
[0011]
　The present invention includes a surfactant and water, and the lipid peptide-type compound consisting of at least one of the following formulas (1) to the compound represented by formula (3) or a pharmaceutically usable salt, heat stable at least comprises one saturated or unsaturated monohydric alcohols (also referred to hereinafter alkyl alcohol), 1,2-alkanediol or 1,3-alkanediol according to the desired carbon number 8 to 30 as agent, fatty acids, polymeric compounds, oily base, an organic acid, to a skin external solid substrates include other additives.
　The present invention, the surfactant, water, the lipid peptide-type compound comprises an alkyl alcohol as a heat stabilizer, optionally 1,2-alkanediol or 1,3-alkanediols, fatty acid, polymer compound , oily base, an organic acid, also aqueous composition may include other additives interest.
　Skin external solid substrate of the present invention is suitable for cosmetic or for pharmaceutical, it may be particularly applicable as a stick-shaped substrate. Note the stick-shaped substrate in the present invention refers to a rod-shaped substrate having a strength which is a (shape can be maintained during i.e. coated) and maintaining the rod-like shape can be applied to the skin or the like. The strength required as a stick base, for example breaking strength: 0.4 × 10 5 Pa ~ 8.0 × 10 5 is Pa, preferably × 10 1.0 5 Pa ~ 7.0 × 10 5 in Pa There, more preferably × 10 1.0 5 Pa ~ 6.0 × 10 5 is Pa.
　Especially skin external solid substrate of the present invention is envisaged in actual use and storage situations said solid substrate may be applied, it is possible to maintain the solid state even at high temperature above 50 ° C., ie thermal stability also in storage conditions of at 50 ° C. under as a reference, it is possible to maintain the stable solid state.
　The following describes each component.
[0012]
[Lipid Peptide type compound]
　As the lipid peptide-type compound used in the skin external solid substrate or the aqueous composition of the present invention, the following equation (1) to the compound represented by formula (3) (lipid peptide), or a pharmaceutically it can be used usable salts (low molecular compound having a peptide portion is a lipid portion and a hydrophilic portion is a hydrophobic moiety) to.
[0013]
[Chemical Formula 4]

[0014]
　In the above formula (1), R 1 represents an aliphatic group having a carbon number of 9 to 23, preferably, R 1 is an unsaturated bond from 0 to linear 2 carbon atoms which may have 11 to 23 it is desirable that the aliphatic group.
　R 1 is and lipid portion constituted by the adjacent carbonyl group Examples of the (acyl groups), lauroyl group, a dodecyl group, a myristoyl group, tetradecyl group, palmitoyl group, Marugaroiru group, oleoyl group, elaidoyl group, linoleoyl group, a stearoyl group, vaccenoyl group, an octadecyl group, arachidoyl group, eicosyl group, behenoyl group, Erukanoiru group, docosyl group, Rigunoseiru group, can be exemplified Nerubonoiru group, particularly preferable ones , lauroyl group, myristoyl group, palmitoyl group, Marugaroiru group, stearoyl group, oleoyl group, and an elaidoyl group and a behenoyl group.
[0015]
　In the above formula (1), R is included in the peptide portion 2 represents a hydrogen atom, or a branched chain may have alkyl group having a carbon number of 1 to 4 carbon atoms 1 or 2.
　The alkyl group having 1 to 4 carbon atoms can have a branched chain of the carbon atoms 1 or 2, a main-chain carbon atoms 1 to 4, and the branched carbon atoms having 1 or 2 means may have an alkyl group, specific examples thereof include a methyl group, an ethyl group, n- propyl group, i- propyl, n- butyl group, i- butyl, sec- butyl or tert- butyl and the like.
　It said R 2 is preferably a hydrogen atom or an alkyl group having a carbon number of 1 to 3 may have a branched chain of carbon atoms 1, more preferably a hydrogen atom.
　The alkyl group having 1 to 3 carbon atom may have one branched carbon atoms, a main-chain carbon atoms of 1 to 3, and the alkyl group which may have 1 branched carbon atoms means, examples thereof include a methyl group, an ethyl group, n- propyl group, i- propyl group, etc. i- butyl group or sec- butyl group, preferably a methyl group, i- propyl group, is i- butyl or sec- butyl group.
[0016]
　In the above formula (1), R 3 is - (CH 2 represents a) n-X group. The - (CH 2 ) in n-X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 has may 5-membered cyclic It represents a group or 6-membered cyclic group, or a 5-membered ring condensed heterocyclic groups consisting of 6-membered ring.
　Said R 3 represents a - (CH 2 in) n-X group, X is preferably an amino group, a guanidino group, a carbamoyl group (-CONH 2 group), a pyrrole group, an imidazole group, a pyrazole group or indole group, more preferably an imidazole group. Further, the - (CH 2 in) n-X group, n is preferably 1 or 2, more preferably 1.
　Accordingly, the - (CH 2 ) n-group, preferably an amino methyl group, 2-aminoethyl group, 3-aminopropyl group, 4-aminobutyl group, a carbamoylmethyl group, 2-carbamoyl-ethyl group, 3- carbamoyl butyl group, 2-guanidino ethyl group, 3-guanidino-butyl group, a pyrrole methyl group, 4-imidazolylmethyl group, pyrazole methyl group, or a 3-indole methyl group, more preferably 4-aminobutyl group, a carbamoylmethyl group , 2-carbamoylethyl group, 3-guanidino-butyl group, a 4-imidazolylmethyl group or a 3-indole methyl group, more preferably a 4-imidazolylmethyl group.
[0017]
　In the compound represented by the above formula (1), as a particularly preferred lipid peptide as a lipid peptide-type compound, it is a compound formed from the lipid portion and a peptide portion (amino collecting portion). Note The abbreviation of amino acids include alanine (Ala), asparagine (Asn), glutamine (Gln), glycine (Gly), histidine (His), Isoroshin (Ile), leucine (Leu), lysine (Lys), tryptophan (Trp ), it represents the valine (Val). : Lauroyl -Gly-His, lauroyl -Gly-Gln, lauroyl -Gly-Asn, lauroyl -Gly-Trp, lauroyl -Gly-Lys, lauroyl -Ala-His, lauroyl -Ala-Gln, lauroyl -Ala-Asn, lauroyl -Ala-Trp, lauroyl -Ala-Lys; myristoyl -Gly-His, myristoyl -Gly-Gln, myristoyl -Gly-Asn, myristoyl -Gly-Trp, myristoyl -Gly-Lys, myristoyl -Ala-His, myristoyl -Ala -Gln, myristoyl -Ala-Asn, myristoyl -Ala-Trp, myristoyl -Ala-Lys; palmitoyl -Gly-His, palmitoyl -Gly-Gln, palmitoyl -Gly-A n, palmitoyl -Gly-Trp, palmitoyl -Gly-Lys, palmitoyl -Ala-His, palmitoyl -Ala-Gln, palmitoyl -Ala-Asn, palmitoyl -Ala-Trp, palmitoyl -Ala-Lys; stearoyl -Gly-His, stearoyl -Gly-Gln, stearoyl -Gly-Asn, stearoyl -Gly-Trp, stearoyl -Gly-Lys, stearoyl -Ala-His, stearoyl -Ala-Gln, stearoyl -Ala-Asn, stearoyl -Ala-Trp, stearoyl - Ala-Lys.
[0018]
　Most preferred are lauroyl -Gly-His, lauroyl -Ala-His-myristoyl -Gly-His, myristoyl -Ala-His; palmitoyl -Gly-His, palmitoyl -Ala-His; stearoyl -Gly-His, stearoyl -Ala -His, and the like.
[0019]
[Formula 5]

[0020]
　In the above formula (2), R 4 represents an aliphatic group having a carbon number of 9 to 23, preferred embodiments, R of supra 1 include the same groups as those defined.
　In the above formula (2), R 5 to R 7 are each independently hydrogen atom, or a branched chain may have alkyl group having a carbon number of 1 to 4 carbon atoms 1 or 2, or - ( CH 2 represents a) n-X group, and R 5 to R 7 at least one of the - (CH 2 represents a) n-X group. n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 has may 5-membered cyclic group or a 6-membered cyclic group, or a 5-membered ring Expressing fused heterocyclic group composed of 6-membered ring. Wherein R 5 to R 7 Preferred examples of, R supra 2 and R 3 include the same groups as those defined.
[0021]
　In the compound represented by the formula (2), suitable lipids peptide is a compound formed from the lipid portion and a peptide portion (amino collecting portion). Myristoyl -Gly-Gly-His, myristoyl -Gly-Gly-Gln, myristoyl -Gly-Gly-Asn, myristoyl -Gly-Gly-Trp, myristoyl -Gly-Gly-Lys, myristoyl -Gly-Ala-His, myristoyl - Gly-Ala-Gln, myristoyl -Gly-Ala-Asn, myristoyl -Gly-Ala-Trp, myristoyl -Gly-Ala-Lys, myristoyl -Ala-Gly-His, myristoyl -Ala-Gly-Gln, myristoyl -Ala- Gly-Asn, myristoyl -Ala-Gly-Trp, myristoyl -Ala-Gly-Lys, myristoyl -Gly-His-Gly, myristoyl -His-Gly-Gly, palmitoyl -Gly Gly-His, palmitoyl -Gly-Gly-Gln, palmitoyl -Gly-Gly-Asn, palmitoyl -Gly-Gly-Trp, palmitoyl -Gly-Gly-Lys, palmitoyl -Gly-Ala-His, palmitoyl -Gly-Ala- Gln, palmitoyl -Gly-Ala-Asn, palmitoyl -Gly-Ala-Trp, palmitoyl -Gly-Ala-Lys, palmitoyl -Ala-Gly-His, palmitoyl -Ala-Gly-Gln, palmitoyl -Ala-Gly-Asn, palmitoyl -Ala-Gly-Trp, palmitoyl -Ala-Gly-Lys, palmitoyl -Gly-His-Gly, palmitoyl -His-Gly-Gly.
[0022]
　Of these, most preferred are lauroyl -Gly-Gly-His, myristoyl -Gly-Gly-His, palmitoyl -Gly-Gly-His, palmitoyl -Gly-His-Gly, palmitoyl -His-Gly-Gly, stearoyl -Gly-Gly-His and the like.
[0023]
[Formula 6]

[0024]
　In the above formula (3), R 8 represents an aliphatic group having a carbon number of 9 to 23, preferred embodiments, R of supra 1 include the same groups as those defined.
　In the above formula (3), R 9 to R 12 are each independently hydrogen atom, or a branched chain may have alkyl group having a carbon number of 1 to 4 carbon atoms 1 or 2, or - ( CH 2 represents a) n-X group, and R 9 through R 12 at least one of the - (CH 2 represents a) n-X group. n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 has may 5-membered cyclic group or a 6-membered cyclic group, or a 5-membered ring Expressing fused heterocyclic group composed of 6-membered ring. Wherein R 9 to R 12 Preferred examples of, R supra 2 and R 3 include the same groups as those defined.
[0025]
　Thus, in the compounds represented by the formula (3), suitable lipid peptide-type compound, as a particularly preferred lipid peptide, lauroyl -Gly-Gly-Gly-His, myristoyl -Gly-Gly-Gly-His, palmitoyl -Gly-Gly-Gly-His, palmitoyl -Gly-Gly-His-Gly, palmitoyl -Gly-His-Gly-Gly, palmitoyl -His-Gly-Gly-Gly, stearoyl -Gly-Gly-Gly-His, etc. and the like.
[0026]
　In the present invention, the amount of lipid peptide-type compound, based on the total weight of the resulting skin external solid substrate, for example, 1 to 20 wt%, preferably 1 to 10 wt%, more preferably 3 to 7 mass it is%.
　In the present invention, the amount of lipid peptide-type compound, based on the total weight of the resulting aqueous composition, for example, 5 to 40 wt%, preferably 10 to 30 wt%.
　Note lipid peptide-type compound used in the present invention comprises at least one of the above formulas (1) to the compound represented by formula (3) (lipid peptide), or a pharmaceutical usable salts, hydrogelling these compounds alone or may be used in combination of two or more as agents.
[0027]
Surfactant
　as surfactants used in skin external solid substrate or the aqueous composition of the present invention have a hydrophilic part and a hydrophobic part in the molecule and a compound said hydrophilic portion having a betaine structure (hereinafter, also referred to as betaine compound), ethylene glycol alkyl ethers, polyglycerin fatty acid ester, or polyoxyethylene polyoxypropylene alkyl ethers can be preferably used.
[0028]
　As the betaine compound as described above, such as N- alkyl -N and lauryl dimethylamino acetic acid betaine (lauryl betaine), N- dimethylamino acid betaine; cocamidopropyl betaine, fatty acid amidoalkyl -N such lauramidopropylbetaine , N- dimethylamino acid betaine; sodium cocoamphoacetate, imidazoline betaines, such as sodium lauroamphoacetate; lauryl hydroxy sulfobetaine, alkyl sulfobetaine and alkyl taurate, alkyl dimethylaminoethanol sulfate type betaines, such as sulfates, alkyl dimethylaminoethanol phosphoric acid betaines such as phosphoric acid esters, etc., known betaine compounds can be used as amphoteric surfactants.
　Further, as the betaine compound, phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, phosphatidylglycerol, diphosphatidylglycerol (cardiolipin), glycerophospholipids such as phosphatidic acid; lysophosphatidylcholine (lysolecithin), lysophosphatidylethanolamine, lysophosphatidylserine sphingophospholipids such as sphingomyelin; serine, lysophosphatidylinositol, lysophosphatidylglycerol, Rizoguriserorin lipids such as lysophosphatidic acid etc. and hydrogenated products thereof. These phospholipids, soybean, may be derived from plants and animals such as egg yolk, it may be one synthesized by chemical or enzymatic methods.
　Among the betaine compounds, preferably, lauryl betaine, lauric acid amidopropyl betaine, lauryl hydroxy sulfobetaine, stearyl betaine, lysophosphatidylcholine (lysolecithin), lysophosphatidylethanolamine, lysophosphatidylserine, lysophosphatidylinositol, lyso phosphatidyl glycerol, lysophosphatidic acid and the like, and preferable, lysophosphatidylcholine (lysolecithin) and the like.
[0029]
　Examples of the ethylene glycol alkyl ethers, polyoxyethylene alkyl ethers, polyoxyethylene lauryl ether, polyoxyethylene palmitate Toys ether, polyoxyethylene stearyl ether, and the like. The ethylene glycol alkyl ether is obtained by using also commercial products, examples of such products, for example, Kao Corporation Emulgen (registered trademark) series and Emanon ® of series, Emulgen 102 kg, Emulgen 103, Emulgen 104P , Emulgen 105, Emulgen 106, Emulgen 108, Emulgen 109P, Emulgen 120, Emulgen 123P, Emulgen 130K, Emulgen 147, Emulgen 150, Emulgen 210P, Emulgen 220, Emulgen 306P, Emulgen 320P, Emulgen 350, Emulgen 404, Emulgen 408, Emulgen 409PV, Emulgen 420, Emulgen 430, Emulgen 705, Emulgen 707, Emulgen 709, Emulgen 1108, Emulgen 1118S-70, Emulgen 1135S-70, Emulgen 1150S-60, Emulgen 4085, Emulgen 2020G-HA, Emulgen 2025G, Emanon 1112, Emano 3199V, Emanon 3299V, Emanon 3299RV, include the Emanon 4110. More preferably, Emulgen 103 manufactured by Kao Corp., Emulgen 104P, Emulgen 105, Emulgen 106, Emulgen 108, Emulgen 109P, Emulgen 210P, Emulgen 306P, Emulgen 320P, Emulgen 404, Emulgen 408, Emulgen 409PV, Emulgen 420, Emulgen 705 , Emulgen 707, Emulgen 709, Emulgen 1108, Emulgen 2020G-HA, Emanon 1112, include Emanon 4110. More preferably, Emulgen 104P Kao Corporation, Emulgen 105, Emulgen 106, Emulgen 108, Emulgen 210P, Emulgen 306P, Emulgen 408, Emulgen 409PV, Emulgen 705, Emulgen 707, Emulgen 709, Emulgen 1108, Emulgen 2020G-HA, Emanon 1112, include the Emanon 4110. Other This, NIKKOL of Nikko Chemicals Co., Ltd. (registered trademark) from the series may be appropriately selected. For example, NIKKOL BT-5, NIKKOL BT-7, NIKKOL BT-9, NIKKOL BT-12.
[0030]
　As the polyglycerol fatty acid ester, glyceryl stearate, glyceryl isostearate, palmitic acid, glyceryl myristate, glyceryl oleate, coconut oil fatty acid glyceryl, mono cottonseed fatty acid glycerin, Monoeruka glyceryl sesquioleate glycerol, alpha, alpha '- oleic acid pyroglutamic acid glycerin, glycerin fatty acid partial esters such as glyceryl monostearate malate; polyglyceryl stearate -2, 3, 4, 5, 6, the 8, the 10, polyglyceryl distearate - 6, the 10, tristearate polyglyceryl-2, Dekasutearin polyglyceryl -10, polyglyceryl-2 isostearate, 3, 4, 5, 6, the 8, the 10 diisostearate poly Riseriru 2 (diglyceryl diisostearate), 3, 10 (diisostearate decaglyceryl), triisostearate polyglyceryl-2, tetra isostearate polyglyceryl-2, big triisostearic acid polyglyceryl-10, polyglyceryl oleate -2, the 3, 4, 5, 6, the 8, the 10 dioleate polyglyceryl -6 trioleate polyglyceryl-2, polyglyceryl-10 etc. Dekaorein acid.
[0031]
　As the polyoxyethylene polyoxypropylene alkyl ether, Emulgen (registered trademark) LS-106 of Kao Corporation, Emulgen LS-110, Emulgen LS-114, Emulgen MS-110, and NIKKOL (registered Nikko Chemicals Co. TM) PBC-31, NIKKOL PBC-33, NIKKOL PBC-34, NIKKOL PBC-41, NIKKOL PBC-44, NIKKOL PBN-4612, NIKKOL PBN-4620, NIKKOL PBN-4630 and the like. More preferably, Emulgen LS-106, Emulgen LS-110, Emulgen LS-114, include Emulgen MS-110. More preferably, Emulgen LS-106, Emulgen LS-110, include Emulgen MS-110.
[0032]
　As the surfactant used in the present invention, it is possible that HLB of (Hydrophile-Lipophile Balance) value is preferably used those which are 8 to 20. More preferably, HLB value of 8 to 14.
　Such surfactants, such as sorbitan isostearate, steareth -8, beheneth-10, laureth -5, ceteth -7, oleth -8, isostearic acid PEG-8 glyceryl, cholestyramine -10, PEG-10BG isostearate triisostearate PEG-30 glyceryl triisostearate PEG-30 glyceryl trioleate PEG-30 glyceryl triisostearate PEG-30 trimethylolpropane, PEG-30 hydrogenated castor oil laurate, PCA isostearate PEG- 30 hydrogenated castor oil, Okuchirudodesesu -10 dilaurate PEG-12, tetraoleate sorbeth -40, polyglyceryl diisostearate -10 (diisostearate decaglyceryl) diisostearate PE -20 glyceryl isostearate PEG-8 isostearate PEG-10 glyceryl triisostearate PEG-60 hydrogenated castor oil, PPG-2-Desesu -7, oleth-10, hydrogenated die merge Reno less -20, coconut fatty sorbitan, isosteareth-10, steareth -11 trimyristate PEG-30 trimethylolpropane, PEG-40 hydrogenated castor oil isostearate, isostearate PEG-40 hydrogenated castor oil, PEG-40 hydrogenated castor PCA isostearate oil, laureth-7, isoceteth -10, ceteth-10, isostearate PEG-10, PEG-10 stearate, oleic acid PEG-10, stearic acid PEG-10 glyceryl, oleth-12, decyltetradeceth -15, correspondent -15, di Gaulin acid PEG-16, PEG-30 hydrogenated castor oil triisostearate PEG-40 glyceryl trioleate PEG-40 glyceryl triisostearate PEG-40 trimethylolpropane, PEG-40 hydrogenated castor oil laurate, such as lauric acid PEG-12 and the like.
[0033]
　In the present invention, the amount of surfactant relative to the total weight of the resulting skin external solid substrate, e.g., 0.5 to 20 wt%, preferably 0.5 to 10 wt%, more preferably 0 .5 to a 5 mass%.
　In the present invention, the amount of surfactant relative to the total weight of the resulting aqueous composition, for example, 1 to 20 wt%, preferably, 2 to 20 wt%.
　Note surfactant used in the present invention is at least one surfactant groups mentioned above, they can be used surfactants alone, or in combination of two or more.
[0034]
[Of at least one saturated or unsaturated carbon atoms 8 to 30 monohydric alcohol]
　in skin external solid substrate or aqueous compositions of the present invention, at least one saturated or unsaturated carbon atoms 8 to 30 When formulating the monohydric alcohol, the thermal stability of the substrate is greatly improved. In the present specification, also simply referred to as "alkyl alcohol" monohydric alcohols of at least one saturated or unsaturated carbon atoms 8 to 30.
　These alkyl alcohols, many of the raw materials, including the derivative is or are synthesized or are commercially available, in the compositions of the present invention is preferably at least one saturated carbon atoms of the alkyl group is 8 to 30 or obtained monohydric alcohols unsaturated are used, more preferably obtained using the monohydric alcohol saturated is 12 to 22, among them, lauryl alcohol (12 carbon atoms), cetanol (carbon atoms 16), stearyl alcohol (18 carbon atoms), behenyl alcohol (22 carbon atoms) is particularly preferred versatile. When the number of carbon atoms in the alkyl alcohol is too short, can not be obtained sufficient thermal stability, and an excessively long, does not dissolve in an aqueous solution, it is that the composition is not uniform.
　In the present invention, the amount of alkyl alcohol, based on the total weight of the obtained skin external solid substrate, e.g., 0.1 to 10 wt%, preferably 0.25 to 5 wt%, more preferably 0. 5 to a 3% by weight.
　In the present invention, the amount of alkyl alcohol, based on the total weight of the aqueous composition obtained, for example, 1 to 10 wt%, preferably 1 to 5 wt%, more preferably 1 to 3 wt%.
　Note the alkyl alcohol used in the present invention is at least one alkyl alcohol groups described above can be used in combination these alone, or two or more kinds.
[0035]
[1,2-alkanediol or 1,3-alkanediols]
　The skin external solid substrate or the aqueous composition of the present invention may contain a 1,2-alkanediol or 1,3-alkanediols. These alkanediols has the function of promoting the solubility of the lipid peptide-type compound.
　Specific examples of the 1,2-alkanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octane diol and 1,2-decanediol and the like. Preferably, 1,2-pentanediol, 1,2-hexanediol, and 1,2-octanediol. More preferably, 1,2-pentanediol or 1,2-hexanediol. 1,2-alkanediol used in the present invention is at least one of the above-described 1,2-alkanediol groups.
　Specific examples of the above 1,3-alkanediols, 1,3-propanediol, 2-methyl-1,3-propanediol, 1,3-butanediol, 3-methyl-1,3-butanediol, 1 , 3-pentanediol, 1,3-hexanediol, 2-ethyl-1,3-hexanediol, 2-ethyl-1,3-octanediol and 1,3-decanediol and the like. Preferably, 1,3-pentanediol, 1,3-hexanediol, 2-ethyl-1,3-hexanediol, and 2-ethyl-1,3-octanediol. More preferably, 2-ethyl-1,3-hexanediol, 2-ethyl-1,3-octanediol. 1,3 alkane diols for use in the present invention is at least one of the above-described 1,3-alkanediol groups.
　These 1,2-alkanediols or 1,3-alkane diols alone or may be used in combination of two or more.
[0036]
　In the present invention, 1,2-amount of alkane diol or or 1,3 alkane diol, based on the total weight of the skin external solid substrate obtained, for example, 0.5 to 20 wt%, preferably, 1 to 10 wt%, more preferably 1 to 5 wt%.
　In the present invention, the amount of 1,2-alkanediol or 1,3 alkane diol, based on the total weight of the resulting aqueous composition, for example, 2 to 20 wt%, preferably, 2 to 10 wt% is there.
[0037]
[Fatty]
　skin external solid substrate or the aqueous composition of the present invention may further include a fatty acid. Fatty acids used in the present invention is preferably at least one selected from the group consisting of salts of saturated fatty acids and unsaturated fatty acids and their fatty acid having a carbon number 10 to 20, for example, the fatty acid capric acid, undecanoic acid, lauric acid, tridecanoic acid, myristic acid, pentadecanoic acid, palmitic acid, stearic acid. More preferably, capric acid, lauric acid, myristic acid, palmitic acid, and stearic acid, among others stearic acid is preferred.
　In the present invention, the amount of the fatty acid used is based on the total weight of the resulting skin external solid substrate, e.g., 0.1 to 2.0 wt%, preferably 0.2 to 1.0 mass% is there.
　In the present invention, the amount of fatty acid relative to the total weight of the resulting aqueous composition, for example 0.5 to 5 wt%, preferably, 0.5 to 3 wt%.
　Note fatty acids used in the present invention is at least one selected from the fatty acid group, these may be used fatty acid alone or in combination of two or more.
[0038]
[Oily base]
　skin external solid substrate of the present invention may further contain an oily base. Also in the aqueous composition of the present invention may contain an oleaginous base. Examples of the oily base materials used in the present invention, oleyl alcohol, jojoba alcohol, chimyl alcohol, selachyl alcohol, batyl alcohol, hexyl decanol, isostearyl alcohol, 2-octyldodecanol, higher (multivalent) and dimer diol alcohols; aralkyl alcohols and their derivatives such as benzyl alcohol; isostearic acid, behenic acid, undecylenic acid, 12-hydroxystearic acid, palmitoleic acid, oleic acid, linoleic acid, linolenic acid, erucic acid, docosahexaenoic acid, eicosapentaenoic acid, isohexadecane acid, anteisoalkyl Heng equalization San acids, long chain branched fatty dimer acid, and hydrogenated dimer acid; liquid paraffin (mineral oil), heavy liquid isoparaffin, light liquid Isopara Fin, alpha-olefin oligomers, polyisobutene, hydrogenated polyisobutene, polybutene, squalane, olive-derived squalane, squalene, vaseline, hydrocarbons such as solid paraffin; candelilla wax, carnauba wax, rice wax, Japan wax, beeswax, montan wax, ozokerite, ceresin, paraffin wax, microcrystalline wax, petrolatum, Fischer-Tropsch wax, polyethylene wax, waxes such as ethylene-propylene copolymers; coconut oil, palm oil, palm kernel oil, safflower oil, olive oil, castor oil , avocado oil, sesame oil, tea oil, evening primrose oil, wheat germ oil, macadamia nut oil, hazelnut oil, kukui nut oil, rose hip oil, meadowfoam oil, persic oil, Tea tree oil, peppermint oil, corn oil, rapeseed oil, sunflower oil, wheat germ oil, linseed oil, cottonseed oil, soybean oil, peanut oil, rice bran oil, cacao butter, shea butter, hydrogenated coconut oil, hydrogenated castor oil, jojoba oils, vegetable fats such as hydrogenated jojoba oil; beef tallow, milk fat, horse fat, egg yolk oil, mink oil, animal fats and oils turtle oil; spermaceti, lanolin, animal waxes such as orange roughy oil; liquid lanolin, reduced lanolin, adsorption purified lanolin, lanolin acetate, acetic acid liquid lanolin, hydroxy lanolin, polyoxyethylene lanolin, lanolin fatty acid, hard lanolin fatty acid, lanolin alcohol, acetic acid lanolin alcohol, lanolin acetate such as (cetyl Ranoriru) ester ; cholesterol, dihydrocholesterol, lanosterol, dihydro Rano sterol Le, phytosterols, sterol such as cholate; sapogenins; saponins; acid cholesteryl, cholesteryl nonanoate, cholesteryl stearate, cholesteryl isostearate, cholesteryl oleate, N- lauroyl -L- glutamic acid di (cholesteryl / behenyl / octyl dodecyl), N- lauroyl -L- glutamic acid di (cholesteryl / octyldodecyl), N- lauroyl -L- glutamic acid di (phytosteryl / behenyl / octyldodecyl), N- lauroyl -L- glutamic acid di (phytosteryl / octyldodecyl) N- lauroyl sarcosine acyl sarcosine alkyl esters of isopropyl etc., 12-hydroxystearic acid cholesteryl, macadamia nut oil fatty acid cholesteryl, Makademiana Tsu oil fatty phytosteryl, phytosteryl isostearate, soft lanolin fatty acid cholesteryl, hard lanolin fatty acid cholesteryl, long chain branched fatty acid cholesteryl, sterol esters and long-chain α- hydroxy fatty acid cholesteryl; phospholipid-cholesterol complex, phospholipid-phytosterol complex lipid complexes of the body such as; octyldodecyl myristate, myristic acid hexyl decyl isostearate octyldodecyl, cetyl palmitate, octyldodecyl, cetyl octanoate, hexyldecyl, isotridecyl isononanoate, isononyl isononanoate, isononyl octyl, isotridecyl isononanoate, isodecyl neopentanoate, neopentanoate, isotridecyl neopentanoate, isostearyl, Odekan octyldodecyl, oleyl oleate, octyldodecyl oleate, ricinoleic acid octyldodecyl, lanolin fatty acid octyldodecyl, hexyldecyl dimethyloctanoate, erucic acid octyldodecyl isostearate hydrogenated castor oil, ethyl oleate, avocado oil fatty acid ethyl, isopropyl myristate, isopropyl palmitate, octyl palmitate, isopropyl isostearate, isopropyl lanolate, sebacic acid diethyl sebacate, diisopropyl sebacate, dioctyl diisopropyl adipate, sebacic acid dibutyl octyl, diisobutyl adipate, dioctyl succinate, citric monoalcohol-carboxylic acid esters such as triethyl citrate; cetyl lactate, diisostearyl malate Oxyacid esters such as monoisostearate Sansui添castor oil; glyceryl trioctanoate (glyceryl tri-2-ethylhexanoate), trioleate glyceryl, glyceryl triisostearate, diisostearate, glyceryl tri (caprylate / caprate), glyceryl , tri (caprylic acid / capric acid / myristic acid / stearic acid) glyceryl, hydrogenated rosin triglyceride (hydrogenated ester gum), rosin triglyceride (ester gum), behenic acid eicosane diacid glyceryl trioctanoate trimethylolpropane triisostearate trimethylolpropane, neopentyl glycol dioctanoate, neopentyl glycol dicaprate, 2-butyl-2-ethyl-1,3-propanediol dioctanoate, Jiorei Phosphate propylene glycol, tetramethylene octanoate pentaerythrityl hydrogenated rosin pentaerythrityl tri ethylhexanoate ditrimethylolpropane, (isostearic acid / sebacic acid) ditrimethylolpropane, tri-ethylhexanoate pentaerythrityl, (hydroxystearic acid / stearic acid / rosin acid) dipentaerythrityl, diglyceryl diisostearate, tetra isostearate polyglyceryl, nona isostearate polyglyceryl-10, deca (erucic acid / isostearic acid / ricinoleic acid) polyglyceryl -8, (hexyldecanoate / sebacic acid) diglyceryl oligoester , glycol distearate (ethylene glycol distearate), Jineopentan acid 3-methyl-1,5-Pentanjio , Polyhydric alcohol fatty acid esters such as Jineopentan acid 2,4-diethyl-1,5-pentanediol; dimerdilinoleic diisopropyl, dimerdilinoleic diisostearyl, dimerdilinoleic di (isostearyl / phytosteryl), dimerdilinoleic acid (phytosteryl / behenyl) dimer dilinoleate (phytosteryl / isostearyl / cetyl / stearyl / behenyl), dimer dilinoleate die merge linoleyl diisostearate die merge linoleyl, die merge linoleyl hydrogenated rosin condensate, dimer dilinoleate hardened castor oil, hydroxyalkyl die merge derivatives of dimer acids or dimer diol linoleyl ether; coconut oil fatty acid monoethanolamide (cocamide MEA), Shea oil fatty acid diethanolamide (cocamide DEA), lauric acid monoethanolamide (lauramide MEA), lauric diethanolamide (lauramide DEA), lauric acid monoisopropanolamide (lauramide MIPA), palmitic monoethanolamide (Parutamido MEA), palmitic acid diethanolamide (Parutamido DEA), fatty acid alkanol amides such as coconut oil fatty acid methyl ethanolamide (Kokamidomechiru MEA); dimethicone (dimethyl polysiloxane), high polymerization dimethicone (highly polymerized dimethylpolysiloxane), cyclomethicone (a cyclic dimethyl siloxanes, decamethylcyclopentasiloxane (simply both cyclopentasiloxane)), phenyl trimethicone, diphenyl dimethicone, phenyl dimethicone , Stearoxy propyl dimethylamine (aminoethyl aminopropyl methicone / dimethicone) copolymer, dimethiconol, dimethiconol crosspolymer, silicone resin, silicone rubber, amino-modified silicones such as aminopropyl dimethicone and amodimethicone, cation-modified silicone, dimethicone copolyols such as polyether-modified silicones, polyglycerin-modified silicone, sugar-modified silicone, carboxylic acid-modified silicones, phosphoric acid-modified silicones, sulfate-modified silicones, alkyl-modified silicone, fatty acid-modified silicones, alkyl ether-modified silicones, amino-modified silicone, peptide-modified silicone, fluorine-modified silicones, cationic-modified and polyether-modified silicones, amino-modified and polyether-modified silicon Over emissions, alkyl-modified and polyether-modified silicones, silicones such as polysiloxane polyoxyalkylene copolymer; perfluorodecane, perfluorooctane, fluorine-based oils such as perfluoropolyether may be mentioned as preferred.
[0039]
　In the present invention, the amount of oily base, based on the total weight of the resulting skin external solid substrate, for example, 1 to 50 wt%, preferably 5 to 50 wt%, more preferably 10 to 50 wt% it is.
　In the present invention, when the aqueous composition comprises an oily base, the amount thereof, for example, 50 to 1% by weight relative to the total weight of the aqueous composition, preferably, 30 to 1 wt%.
　Note the oily base to be used in the present invention is at least one oil base group described above may be used alone these oily base, or in combination of two or more.
[0040]
[Organic acid]
　skin external solid substrate of the present invention may further comprise an organic acid. Also in the aqueous composition of the present invention may comprise an organic acid.
　Examples of the organic acids, ascorbic acid, citric acid, lactic acid, glycolic acid, succinic acid, acetic acid, malic acid, tartaric acid, fumaric acid, and the like. Among them preferably ascorbic acid, citric acid, lactic acid and the like, in particular ascorbic acid, citric acid.
　In the present invention, the amount of organic acid, based on the total weight of the resulting skin external solid substrate, for example, 1 to 20 wt%, preferably, 1 to 10 wt%.
　In the present invention, when the aqueous composition comprises an organic acid, the amount thereof, for example, 1 to 20% by weight relative to the total weight of the aqueous composition, preferably, 1 to 10 wt%.
[0041]
[Polyalcohol]
　skin external solid substrate or the aqueous composition of the present invention may contain a polyhydric alcohol. The polyhydric alcohols are the polyhydric alcohol different from the 1,2-alkanediol or 1,3-alkane diols listed above, specific examples thereof are glycerin, propylene glycol and polyethylene glycol, and the like. By including the polyhydric alcohol, it is possible to improve the temporal stability of the skin external solid substrate. Note The above polyethylene glycol, for example can be preferably used those having an average molecular weight of 1,000 to 4,000.
　In the present invention, the amount of the polyhydric alcohol, based on the total mass of the skin external solid substrate obtained, for example, 1 to 80 wt%, preferably, may be 1 to 60 wt%.
　In the present invention, when the aqueous composition comprises a polyhydric alcohol, the amount thereof, for example, 1 to 40% by weight relative to the total weight of the aqueous composition, preferably, may be 1 to 20 wt% .
[0042]
[Other Additives]
　The skin external solid substrate or the aqueous composition of the present invention, generally cosmetic additives as necessary, additives that can be used as additives and pharmaceutical additives quasi-drugs it can be formulated. Cosmetics, as the additive component such as a physiologically active substance and the functional substance to be incorporated into quasi drugs or skin external preparation such as a pharmaceutical, for example humectants, feel improvers, surfactants other than the above polymer, increasing tacky gelling agents, solvents, propellants, antioxidants, reducing agents, oxidizing agents, preservatives, antibacterial agents, fungicides, chelating agents, pH adjusting agents, acids, alkalis, powder, an inorganic salt, an ultraviolet absorber , whitening, vitamins and derivatives thereof, hair growth agents, blood circulation promoters, stimulants, hormones, anti-wrinkle agents, anti-aging agents, tightening agents, cooling agents, warming agents, wound healing promoters, irritation emollients, analgesics, cell activators, plants, animals, microbial extract, antipruritic agents, desquamating-dissolving agents, antiperspirants, coolants, astringents, enzymes, nucleic acids, perfumes, pigments, colorants, dyes, pigments anti-inflammatory agents, anti-inflammatory agents, anti-asthmatic, anti-chronic obstructive pulmonary disease, anti-allergic, immune Seizai, anti-infective agents and antifungal agents.
　The amounts of these other additives include, but may variously vary depending on the type, relative to the total weight of the obtained skin external solid substrate, e.g., 0.1 to 20 wt%, or 0.5 to about 10 wt% it can be.
[0043]
　The humectants, feel improvers, glycerol, trimethylolpropane, pentaerythritol, hexylene glycol, diglycerin, polyglycerin, diethylene glycol, dipropylene glycol, polypropylene glycols, polyols such as ethylene glycol, propylene glycol copolymer and the polymer; diethylene glycol monoethyl ether (ethoxydiglycol), ethylene glycol monoethyl ether, ethylene glycol monobutyl ether, glycol alkyl ethers such as diethylene glycol dibutyl ether; (eicosadioate / tetradecanedioic acid) polyglyceryl-10, tetradecanedioic soluble esters such as polyglyceryl -10; sorbitol, xylitol, erythritol, Man'ni Lumpur, sugar alcohols such as maltitol, glucose, fructose, galactose, mannose, threose, xylose, arabinose, fucose, ribose, deoxyribose, maltose, trehalose, lactose, raffinose, gluconic acid, glucuronic acid, cyclodextrins ( alpha-, beta-, .gamma.-cyclodextrin, and, maltosyl reduction, modified cyclodextrins, such as hydroxyalkylated), beta-glucan, chitin, chitosan, heparin and derivatives, pectin, arabinogalactan, dextrin, dextran, glycogen, ethyl glucoside, sugars and derivatives thereof such as methacrylic acid glucosyl ethyl polymers or copolymers thereof; hyaluronic acid, sodium hyaluronate; sodium chondroitin sulfate; mucoitin Sulfate, charonic sulfate, keratosulfate, dermatan sulfate; white fungus extract, white fungus polysaccharide; fucoidan; Chuberosu polysaccharide or naturally occurring polysaccharide; citric acid, tartaric acid and salts thereof such as lactic acid; urea and derivatives thereof; 2 - pyrrolidone-5-carboxylic acid and salts thereof such as sodium; betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, tyrosine, beta-alanine, threonine, glutamic acid, glutamine, asparagine , aspartic acid, cysteine, cysteine, methionine, leucine, isoleucine, valine, tryptophan, histidine, amino acids and salts thereof such as taurine; collagen, fish-derived collagen, atelocollagen, gelatin Elastin, collagen degradation peptides, hydrolyzed collagen, hydroxypropyl ammonium hydrolyzed collagen chloride, elastin hydrolysates, keratin hydrolysates, hydrolyzed keratin, conchiolin hydrolysates, hydrolyzed conchiolin, silk protein hydrolysates, hydrolyzed silk, lauroyl hydrolyzed silk sodium, soy protein hydrolysates, wheat protein hydrolysates, hydrolyzed wheat protein, casein hydrolysates, proteins peptides and their derivatives such as acylated peptides; palmitoyl oligopeptide, palmitoyl pentapeptide, acylated peptides, such as palmitoyl tetrapeptide s; silylated peptides; lactic acid bacteria culture fluid, yeast extract, shell membrane proteins, bovine submaxillary mucin, hypotaurine, lignan glycosides, glutathione, A Albumin, whey; choline chloride, phosphoryl choline; placental extract, Earasuchin, collagen, aloe extract, hamamelis water, loofah water, Kamomiraekisu, licorice extract, comfrey extract, silk extract, Izayoi rose extract, yarrow extract, eucalyptus extract animal and vegetable extract component such melilot extract, natural ceramide (type 1,2,3,4,5,6), hydroxy ceramides, pseudoceramides, sphingoglycolipids, ceramides such as ceramide and sugar ceramide containing extract It is mentioned as preferred.
[0044]
　As the surfactant, anionic surfactants, nonionic surfactants, cationic surfactants, amphoteric surfactants include as polymeric surfactants are preferred. To illustrate preferred as a surfactant, as the anionic surfactant, potassium laurate, fatty acid salts such as potassium myristate; sodium lauryl sulfate, triethanolamine lauryl sulfate, alkyl sulfate ester salts such as ammonium lauryl sulfate; sodium laureth sulfate, polyoxyethylene alkyl sulfates such as laureth sulfate triethanolamine; cocoyl methyl taurate, sodium cocoyl methyl taurine potassium, lauroyl methyl taurate, sodium, myristoyl methyl taurine sodium, lauroyl methylalanine sodium, lauroyl sarcosine sodium, lauroyl sarcosine triethanolamine ethanolamine, acyl N- methyl amino acids salts such as lauroyl glutamate methylalanine sodium; cocoyl Polyoxyethylene alkyl ethers such as sodium laureth acetate; sodium glutamic acid, cocoyl glutamate, triethanolamine, sodium lauroyl glutamate, myristoyl sodium glutamate, sodium stearoyl glutamate, palmitoyl aspartate ditriethanolamine, acylamino acid salts such as cocoyl alanine triethanolamine fatty acid alkanolamides ether carboxylates; acyl lactates, polyoxyethylene fatty amine sulfates; fatty acid alkanolamide sulfates; hydrogenated coconut oil fatty acid glycerin sodium sulfate succinate salts such as lauroyl sodium monoethanolamide succinate; acetate fatty acid glycerides sulfates and the like; alkylbenzenes polyoxyethylene sulfates; alpha--olefin Olefin sulfonates such as sodium Insuruhon acid; lauryl disodium sulfosuccinate, alkyl sulfosuccinates such as dioctyl sodium sulfosuccinate; laureth disodium sulfosuccinate, mono lauroyl monoethanolamide polyoxyethylene sodium sulfosuccinate, lauryl polypropylene glycol sulfosuccinate sodium tetradecyl benzene sulfonate, alkyl benzene sulfonate such as tetradecyl benzene sulfonate triethanolamine; alkyl ether sulfosuccinates such as sodium alkyl naphthalene sulfonate; alkane sulfonates; alpha-sulfo fatty acid methyl ester salts; acyl isethionates, alkyl glycidyl ether sulfonates, alkyl sulfo acetates; laureth Sodium caseinate; alkyl aryl ether phosphate; fatty amides alkyl phosphate salts such as potassium lauryl phosphate; sodium phosphate, sodium Jirauresurin acid, trisodium laureth phosphate, alkyl ether phosphate salts such as sodium Monooresurin acid ether phosphates; phosphatidyl glycerol, phospholipids such as phosphatidylinositol, phosphatidic acid; carboxylic acid-modified silicones, phosphoric acid-modified silicones, and silicone-based anionic surfactants such as sulfuric acid-modified silicone; non-ionic surfactant the laureth (polyoxyethylene-lauryl ether) s, ceteth (polyoxyethylene cetyl ethers), steareth (polyoxyethylene stearyl ether) s, beheneth (Porioki Shi ethylene behenyl ethers), isosteareth (polyoxyethylene isostearyl ethers), Okuchirudodesesu (various polyoxyethylene addition number of the polyoxyethylene alkyl ethers, polyoxyethylene octyl dodecyl ether) and the like; polyoxyethylene alkyl phenyl ethers; polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil monoisostearate, polyoxyethylene hydrogenated castor oil triisostearate, polyoxyethylene hydrogenated castor oil mono-pyroglutamic acid monoisostearate diester , castor oil and hardened castor oil derivatives such as polyoxyethylene hydrogenated castor oil maleic acid, polyoxyethylene phytosterol, polyoxyethylene cholesterol Polyoxyethylene cholestanol, polyoxyethylene lanolin, polyoxyethylene reduced lanolin; polyoxyethylene-polyoxypropylene cetyl ether, polyoxyethylene-polyoxypropylene 2-decyltetradecyl ether, polyoxyethylene-polyoxypropylene monobutyl ether , polyoxyethylene-polyoxypropylene hydrogenated lanolin, polyoxyethylene polyoxypropylene alkyl ethers of polyoxyethylene-polyoxypropylene glycerin ether; polyoxyethylene-polyoxypropylene glycol; PPG-9 diglyceryl etc. ( poly) glycerol polyoxypropylene glycol; glyceryl stearate, glyceryl isostearate, palmitic acid, glyceryl millimeter Chin acid, glyceryl oleate, coconut oil fatty acid glyceryl, mono cottonseed fatty acid glycerin, Monoeruka glyceryl sesquioleate glycerol, alpha,. Alpha .'- oleate pyroglutamate, glyceryl fatty acid partial esters, such as glyceryl monostearate malate s; polyglyceryl stearate -2, 3, 4, 5, 6, the 8, the 10, polyglyceryl distearate -6, the 10, tristearate polyglyceryl-2, Dekasutearin polyglyceryl -10, isostearate acid polyglyceryl-2, 3, 4, 5, 6, the 8, the 10, polyglyceryl diisostearate 2 (diglyceryl diisostearate), 3, 10, triisostearate

claims

[Claim 1]A surfactant and water, and the following formula (1) to the compound represented by formula (3) or lipid peptide-type compound consisting of at least one of its pharmaceutically usable salts, 8 to 30 carbon atoms at least one saturated or unsaturated and a monohydric alcohol, the skin external solid substrate.
[Chemical formula 1]

(In the formula, R 1 represents an aliphatic group having a carbon number of 9 to 23, R 2 is a hydrogen atom, or a number of 1 to carbon atoms which may have a branched chain carbon atoms 1 or 2 represents 4 alkyl, R 3 is - (CH 2 ) n represents an -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom 1 or represents a fused heterocyclic ring composed of three 5-membered may have ring or 6-membered ring or 5-membered ring and 6-membered ring.)
[formula 2]

(wherein, R 4 is a carbon number of 9 to 23 represents an aliphatic group, R 5 to R 7 each independently represent hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain carbon atoms 1 or 2, or - (CH 2 ) n represents -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 Yes From then may 5- or 6-membered ring or 5-membered ring and 6-membered ring represents a fused heterocyclic ring composed.)
[Formula 3]

(wherein, R 8 is an aliphatic group having a carbon number of 9 to 23 represents, R 9 to R 12 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain carbon atoms 1 or 2, or - (CH 2 ) n a -X group represents, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or 5-membered nitrogen atom may have 1 to 3 rings or 6-membered ring or 5-membered ring and 6-membered It represents a fused heterocyclic ring composed of ring.)
[Claim 2]
1,2 alkane further comprising a diol or 1,3-alkanediol, a skin external solid substrate according to claim 1.
[Claim 3]
Further comprising at least one fatty acid, according to claim 1 or skin external solid substrate according to claim 2.
[Claim 4]
The 1,2-alkanediol or different from the 1,3-alkanediol, further comprising a polyhydric alcohol of at least one dermatological solid substrate according to claim 2 or claim 3.
[Claim 5]
The surfactant, ethylene glycol alkyl ethers, phospholipids, is one or more compounds selected from the group consisting of polyglycerol fatty acid esters and polyoxyethylene polyoxypropylene alkyl ethers, of claims 1 to 4 among skin external solid substrate according to any one.
[Claim 6]
It said fatty acid is stearic acid, according to claim 3 or skin external solid substrate according to any one of claims 5.
[Claim 7]
The polyhydric alcohol is glycerin, propylene glycol or polyethylene glycol, claim 4 or skin external solid substrate according to any one of claims 6.
[8.]
Further comprising at least one oily base dermatological solid substrate according to any one of claims 1 to 7.
[Claim 9]
Further comprising at least one organic acid, a skin external solid substrate according to any one of claims 1 to 8.
[Claim 10]
Is a cosmetic or pharmaceutical, claims 1 to skin external solid substrate according to any one of claims 9.
[Claim 11]
A stick, according to claim 1 to skin external solid material according to any one of claims 10.
[Claim 12]
A surfactant and water, and the following formula (1) to the compound represented by formula (3) or lipid peptide-type compound consisting of at least one of its pharmaceutically usable salts, 8 to 30 carbon atoms at least one saturated or unsaturated and a monohydric alcohol, the aqueous composition.
[Formula 4]

(wherein, R 1 represents an aliphatic group having a carbon number of 9 to 23, R 2 is a hydrogen atom, or a number of 1 to carbon atoms which may have a branched chain carbon atoms 1 or 2 represents 4 alkyl, R 3 is - (CH 2 ) n represents an -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom 1 or represents a fused heterocyclic ring composed of three 5-membered may have ring or 6-membered ring or 5-membered ring and 6-membered ring.)
[Chemical formula 5]

(wherein, R 4 is a carbon number of 9 to 23 represents an aliphatic group, R 5 to R 7 each independently represent hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain carbon atoms 1 or 2, or - (CH 2 ) n represents -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 Yes From then may 5- or 6-membered ring or 5-membered ring and 6-membered ring represents a fused heterocyclic ring composed.)
[Formula 6]

(wherein, R 8 is an aliphatic group having a carbon number of 9 to 23 represents, R 9 to R 12 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain carbon atoms 1 or 2, or - (CH 2 ) n a -X group represents, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or 5-membered nitrogen atom may have 1 to 3 rings or 6-membered ring or 5-membered ring and 6-membered It represents a fused heterocyclic ring composed of ring.)
[Claim 13]
Further comprising a 1,2-alkanediol or 1,3-alkanediol, an aqueous composition according to claim 12.
[Claim 14]
Further comprising at least one fatty acid, the aqueous composition according to claim 12 or claim 13.
[Claim 15]
The 1,2-alkane different from the diol or 1,3-alkanediols, further comprising a polyhydric alcohol of at least one, according to claim 13 or an aqueous composition according to claim 14.
[Claim 16]
The surfactant, ethylene glycol alkyl ethers, phospholipids, is one or more compounds selected from the group consisting of polyglycerol fatty acid esters and polyoxyethylene polyoxypropylene alkyl ethers, of claims 12 to claim 15 of the aqueous composition of any one.
[Claim 17]
Is a premix for the preparation of a skin external solid substrate according to claim 12 or the aqueous composition according to any one of claims 16.
[Claim 18]
A surfactant and water, formula (1) through (3) a compound or above room temperature a mixed system containing at least one consisting of a lipid peptide-type compound of the pharmaceutically usable salt thereof heating step of heating to a temperature below 100 ° C.,
followed by the heated said mixing system with the addition of monohydric alcohol of at least one saturated or unsaturated carbon atoms 8 to 30, claims 12 to claim preparation step of preparing an aqueous composition according to any one of 17,
the aqueous phase is heated to a temperature below room temperature or above 100 ° C., was added an aqueous composition prepared above, is mixed, or the in the prepared aqueous composition, the addition of the aqueous phase which has been heated to a temperature below room temperature or above 100 ° C., mixed, the mixing step, and
cooling the mixture obtained in the mixing step, the cooling step to form a gel,
including, claim 1 Method for producing a skin external solid substrate according.
[Chemical Formula 7]

(wherein, R 1 represents an aliphatic group having a carbon number of 9 to 23, R 2 is a hydrogen atom, or a number of 1 to carbon atoms which may have a branched chain carbon atoms 1 or 2 represents 4 alkyl, R 3 is - (CH 2 ) n represents an -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom 1 or represents a fused heterocyclic ring composed of three 5-membered may have ring or 6-membered ring or 5-membered ring and 6-membered ring.)
[formula 8]

(wherein, R 4 is a carbon number of 9 to 23 represents an aliphatic group, R 5 to R 7 each independently represent hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain carbon atoms 1 or 2, or - (CH 2 ) n represents -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 Yes From then may 5- or 6-membered ring or 5-membered ring and 6-membered ring represents a fused heterocyclic ring composed.)
[Chemical Formula 9]

(wherein, R 8 is an aliphatic group having a carbon number of 9 to 23 represents, R 9 to R 12 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain carbon atoms 1 or 2, or - (CH 2 ) n a -X group represents, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or 5-membered nitrogen atom may have 1 to 3 rings or 6-membered ring or 5-membered ring and 6-membered It represents a fused heterocyclic ring composed of ring.)
[Claim 19]
In the mixing step, further adding solution of the drug, method according to claim 18.