JP2003012511A - Aerosol composition - Google Patents
Aerosol compositionInfo
- Publication number
- JP2003012511A JP2003012511A JP2001195228A JP2001195228A JP2003012511A JP 2003012511 A JP2003012511 A JP 2003012511A JP 2001195228 A JP2001195228 A JP 2001195228A JP 2001195228 A JP2001195228 A JP 2001195228A JP 2003012511 A JP2003012511 A JP 2003012511A
- Authority
- JP
- Japan
- Prior art keywords
- urea
- stock solution
- aerosol composition
- propellant
- weight
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000443 aerosol Substances 0.000 title claims abstract description 84
- 239000000203 mixture Substances 0.000 title claims abstract description 72
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- 239000004202 carbamide Substances 0.000 claims abstract description 75
- 239000011550 stock solution Substances 0.000 claims abstract description 57
- 239000003380 propellant Substances 0.000 claims abstract description 49
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 31
- 239000007788 liquid Substances 0.000 claims abstract description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 30
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 claims description 22
- 230000003020 moisturizing effect Effects 0.000 claims description 19
- 230000001139 anti-pruritic effect Effects 0.000 claims description 18
- 238000002156 mixing Methods 0.000 claims description 18
- 239000003915 liquefied petroleum gas Substances 0.000 claims description 10
- 239000003908 antipruritic agent Substances 0.000 claims description 8
- 150000005846 sugar alcohols Polymers 0.000 claims description 8
- 230000003110 anti-inflammatory effect Effects 0.000 claims description 7
- 230000000844 anti-bacterial effect Effects 0.000 claims description 6
- 241001465754 Metazoa Species 0.000 claims description 4
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims description 4
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- 230000000202 analgesic effect Effects 0.000 claims description 3
- 230000000694 effects Effects 0.000 abstract description 28
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- 102000011782 Keratins Human genes 0.000 description 19
- 108010076876 Keratins Proteins 0.000 description 19
- 238000002360 preparation method Methods 0.000 description 19
- 238000000354 decomposition reaction Methods 0.000 description 15
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 14
- -1 nitrate ester Chemical class 0.000 description 14
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 13
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 12
- 239000003795 chemical substances by application Substances 0.000 description 11
- 239000000284 extract Substances 0.000 description 11
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 10
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- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 6
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- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
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- 235000011187 glycerol Nutrition 0.000 description 6
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- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 5
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- 239000000126 substance Substances 0.000 description 5
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- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 4
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 4
- 206010016807 Fluid retention Diseases 0.000 description 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 4
- 208000003251 Pruritus Diseases 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 4
- 150000001298 alcohols Chemical class 0.000 description 4
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- DNTGGZPQPQTDQF-XBXARRHUSA-N crotamiton Chemical compound C/C=C/C(=O)N(CC)C1=CC=CC=C1C DNTGGZPQPQTDQF-XBXARRHUSA-N 0.000 description 4
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- 239000003599 detergent Substances 0.000 description 4
- SZXQTJUDPRGNJN-UHFFFAOYSA-N dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 description 4
- 238000004090 dissolution Methods 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
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- 238000002347 injection Methods 0.000 description 4
- 239000007924 injection Substances 0.000 description 4
- NNPPMTNAJDCUHE-UHFFFAOYSA-N isobutane Chemical compound CC(C)C NNPPMTNAJDCUHE-UHFFFAOYSA-N 0.000 description 4
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 description 4
- 230000000717 retained effect Effects 0.000 description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 4
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 4
- 238000009834 vaporization Methods 0.000 description 4
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- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 3
- MPDGHEJMBKOTSU-UHFFFAOYSA-N Glycyrrhetinsaeure Natural products C12C(=O)C=C3C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(C)C MPDGHEJMBKOTSU-UHFFFAOYSA-N 0.000 description 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 3
- 239000002202 Polyethylene glycol Substances 0.000 description 3
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 3
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- 239000004359 castor oil Substances 0.000 description 3
- 235000019438 castor oil Nutrition 0.000 description 3
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- 239000013078 crystal Substances 0.000 description 3
- 235000014113 dietary fatty acids Nutrition 0.000 description 3
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 3
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- 239000000194 fatty acid Substances 0.000 description 3
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- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 3
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- LPLVUJXQOOQHMX-QWBHMCJMSA-N glycyrrhizinic acid Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@@H]1C([C@H]2[C@]([C@@H]3[C@@]([C@@]4(CC[C@@]5(C)CC[C@@](C)(C[C@H]5C4=CC3=O)C(O)=O)C)(C)CC2)(C)CC1)(C)C)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O LPLVUJXQOOQHMX-QWBHMCJMSA-N 0.000 description 3
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- 229920001223 polyethylene glycol Polymers 0.000 description 3
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- 239000001294 propane Substances 0.000 description 3
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- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 description 2
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- SVTBMSDMJJWYQN-UHFFFAOYSA-N 2-methylpentane-2,4-diol Chemical compound CC(O)CC(C)(C)O SVTBMSDMJJWYQN-UHFFFAOYSA-N 0.000 description 2
- IJALWSVNUBBQRA-UHFFFAOYSA-N 4-Isopropyl-3-methylphenol Chemical compound CC(C)C1=CC=C(O)C=C1C IJALWSVNUBBQRA-UHFFFAOYSA-N 0.000 description 2
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- WNIFXKPDILJURQ-UHFFFAOYSA-N stearyl glycyrrhizinate Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C)CCC5(C)CCC(C(=O)OCCCCCCCCCCCCCCCCCC)(C)CC5C4=CC(=O)C3C21C WNIFXKPDILJURQ-UHFFFAOYSA-N 0.000 description 1
- 239000010959 steel Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 229960004718 sulconazole nitrate Drugs 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- 229960002180 tetracycline Drugs 0.000 description 1
- 229930101283 tetracycline Natural products 0.000 description 1
- 235000019364 tetracycline Nutrition 0.000 description 1
- 150000003522 tetracyclines Chemical class 0.000 description 1
- 229960000790 thymol Drugs 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 235000010384 tocopherol Nutrition 0.000 description 1
- 229960001295 tocopherol Drugs 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- FUSNMLFNXJSCDI-UHFFFAOYSA-N tolnaftate Chemical compound C=1C=C2C=CC=CC2=CC=1OC(=S)N(C)C1=CC=CC(C)=C1 FUSNMLFNXJSCDI-UHFFFAOYSA-N 0.000 description 1
- 229960004880 tolnaftate Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229930188428 trichomycin Natural products 0.000 description 1
- ZIBGPFATKBEMQZ-UHFFFAOYSA-N triethylene glycol Chemical compound OCCOCCOCCO ZIBGPFATKBEMQZ-UHFFFAOYSA-N 0.000 description 1
- 229960002703 undecylenic acid Drugs 0.000 description 1
- 150000003672 ureas Chemical class 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019158 vitamin B6 Nutrition 0.000 description 1
- 239000011726 vitamin B6 Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
- 239000003357 wound healing promoting agent Substances 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Landscapes
- Cosmetics (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
【0001】[0001]
【発明の属する技術分野】本発明は、尿素を必須成分と
する原液と噴射剤を含有するエアゾール組成物に関す
る。より詳細には、本発明は尿素を安定な状態で保持す
ることにより、尿素が有する保湿効果、角質軟化効果ま
たは鎮痒効果などといった所望の効果を有効に発揮し、
しかも尿素の分解によって生じる悪臭の発生が有意に抑
制されてなるエアゾール組成物に関する。TECHNICAL FIELD The present invention relates to an aerosol composition containing a stock solution containing urea as an essential component and a propellant. More specifically, the present invention, by holding urea in a stable state, effectively exerts a desired effect such as a moisturizing effect of urea, a keratin softening effect or an antipruritic effect,
Moreover, the present invention relates to an aerosol composition in which the generation of malodor caused by the decomposition of urea is significantly suppressed.
【0002】[0002]
【従来の技術】エアゾール組成物は、主として水性の原
液と噴射剤とから構成され、噴射剤としては、通常、液
化ガスまたは圧縮ガスが用いられている。かかる噴射剤
は、皮膚に塗布した際に皮膚表面から気化熱を奪うこと
によって使用者に冷却感をもたらす効果を発揮する成分
であるため、冷却効果を特徴とするエアゾール組成物に
は必要不可欠な成分である。2. Description of the Related Art An aerosol composition is mainly composed of an aqueous stock solution and a propellant, and a liquefied gas or a compressed gas is usually used as the propellant. Since such a propellant is a component that exerts an effect of giving a cooling sensation to the user by removing heat of vaporization from the skin surface when applied to the skin, it is indispensable for an aerosol composition having a cooling effect. It is an ingredient.
【0003】ところで、従来より保湿作用、角質軟化作
用または鎮痒作用を有する外用剤として尿素を配合した
外用剤が知られている。By the way, conventionally, an external preparation containing urea has been known as an external preparation having a moisturizing action, a keratin softening action or an antipruritic action.
【0004】尿素は、角質の水分保持量を増加させて乾
燥性角化症における角質層の水分保有力の低下を改善さ
せたり、角質を溶解剥離させる作用を有する他、皮膚透
過性亢進作用、殺菌作用、創傷治癒作用、細胞賦活作
用、さらには、乾燥による掻痒の止痒作用といった各種
の作用を有することが知られている。かかる所望の効果
を得るためには製剤中に尿素をある一定濃度以上配合す
る必要があり、その水溶性から水を担体として製剤中に
尿素を溶解保持させているのが一般的である。[0004] Urea has an effect of increasing the water retention of the keratin, improving the decrease in the water retention of the stratum corneum in keratoderma sicca, dissolving and exfoliating the keratin, and enhancing skin permeability. It is known to have various actions such as a bactericidal action, a wound healing action, a cell activation action, and an antipruritic action against pruritus caused by drying. In order to obtain such a desired effect, it is necessary to mix urea in the preparation at a certain concentration or more, and it is general that urea is dissolved and retained in the preparation using water as a carrier due to its water solubility.
【0005】しかしながら、反面、尿素は水溶液中で不
安定であり、加水分解によってアンモニアと二酸化炭素
に分解することが知られている。そして、この分解は熱
によって促進される。かかる分解は、尿素に起因する薬
効の低下のみならず、pH変動に伴う製剤の劣化や着色
またはアンモニア臭の発生による商品価値の低下を招く
ため、尿素含有製剤の開発において解決しなくてはなら
ない重要な問題である。特に、エアゾール剤の場合は、
噴霧というその使用形態から、尿素の分解によって生じ
る僅かなアンモニアが悪臭の原因となって商品価値を著
しく低下させるため、上記問題を解決する意義は大き
い。On the other hand, however, urea is known to be unstable in an aqueous solution and decompose into ammonia and carbon dioxide by hydrolysis. And this decomposition is accelerated by heat. Such decomposition not only lowers the drug efficacy due to urea, but also leads to deterioration of the formulation due to pH fluctuations and reduction in commercial value due to coloration or generation of ammonia odor, and therefore must be resolved in the development of urea-containing formulations. This is an important issue. Especially in the case of aerosols,
From the usage form of spraying, a slight amount of ammonia generated by decomposition of urea causes an offensive odor to significantly reduce the commercial value, and therefore, there is great significance in solving the above problems.
【0006】[0006]
【発明が解決しようとする課題】本発明は、水存在下に
おける尿素の不安定性に伴う尿素含有外用剤の上記問
題、特にエアゾール組成物の問題を解決することを目的
とするものである。詳細には、本発明は、所望の効果を
発揮する量の尿素を安定して保有するエアゾール組成物
を提供することを目的とする。より詳細には、本発明
は、水の存在下において尿素を安定して保有することに
よって、尿素の分解に伴う悪臭の発生が有意に抑制され
てなるエアゾール組成物を提供することを目的とする。SUMMARY OF THE INVENTION It is an object of the present invention to solve the above problems of urea-containing external preparations, particularly aerosol compositions, which are associated with the instability of urea in the presence of water. In particular, the present invention aims to provide an aerosol composition that stably holds an amount of urea that exerts the desired effect. More specifically, it is an object of the present invention to provide an aerosol composition in which urea is stably retained in the presence of water, thereby significantly suppressing the generation of malodor associated with the decomposition of urea. .
【0007】さらに本発明は、水とともに尿素を必須成
分として含有するエアゾール組成物において尿素を安定
に保持する方法、並びに尿素の分解に起因する悪臭の発
生を防止する方法を提供することを目的とするものでも
ある。Further, the present invention aims to provide a method for stably holding urea in an aerosol composition containing urea as an essential component together with water, and a method for preventing generation of a bad odor due to decomposition of urea. It is also something to do.
【0008】[0008]
【課題を解決するための手段】本発明者らは、上記課題
を解決するために鋭意研究を行なった結果、水及び尿素
を必須成分として含有する原液と噴射剤とからなるエア
ゾール組成物において、原液100重量%中に尿素が2
〜30重量%、水が30〜90重量%含まれるように原
液を調製し、該原液を噴射剤に対して、原液:噴射剤=
25:75〜90:10(液体状態、容積比)の割合と
なるように配合することによって、(i)水存在中で尿素
を安定して保有することができること、(ii)尿素の分解
による悪臭の問題が生じないこと、(iii)尿素を有効量
安定して含有することで期待する尿素の有効な効果を十
分に発揮することができること、などを見出した。そし
て、かかるエアゾール組成物が、保湿作用、角質軟化作
用または鎮痒作用を有するエアゾール剤の内容成分とし
て有用であることを確認した。本発明はかかる知見に基
づいて開発されたものである。Means for Solving the Problems As a result of intensive studies to solve the above problems, the present inventors have found that in an aerosol composition comprising a propellant and a stock solution containing water and urea as essential components, 2 urea in 100% by weight stock solution
To 30% by weight and 30 to 90% by weight of water were prepared to prepare a stock solution, and the stock solution was added to a propellant.
By blending so as to have a ratio of 25:75 to 90:10 (liquid state, volume ratio), (i) stable retention of urea in the presence of water, (ii) decomposition of urea It was found that the problem of bad odor does not occur, and (iii) the effective effect of urea that is expected can be sufficiently exhibited by containing a stable amount of urea in an effective amount. Then, it was confirmed that such an aerosol composition is useful as a content component of an aerosol agent having a moisturizing action, a keratin softening action or an antipruritic action. The present invention was developed based on such knowledge.
【0009】すなわち、本発明は下記に掲げるエアゾー
ル組成物である:
(1)噴射剤と、尿素を2〜35重量%及び水を30〜
90重量%の割合で含有する原液とからなるエアゾール
組成物であって、噴射剤と原液との混合容積比が液体状
態で10:90〜75:25であることを特徴とするエ
アゾール組成物。
(2)噴射剤と原液との混合容積比が液体状態でl0:
90〜50:50であることを特徴とする(1)に記載
のエアゾール組成物。
(3)原液100重量%中に含まれる尿素の割合が5〜
30重量%である(1)または(2)に記載のエアゾー
ル組成物。
(4)噴射剤が、ジメチルエーテル及び液化石油ガスの
中から選択される少なくとも1種である(1)乃至
(3)いずれかに記載のエアゾール組成物。
(5)原液中にさらに低級アルコールを0.1〜50重
量%の割合で含有する(1)乃至(4)のいずれかに記
載のエアゾール組成物。
(6) 原液中にさらに多価アルコールを0.1〜30重
量%の割合で含有する(5)に記載のエアゾール組成
物。
(7)原液中にさらに鎮痒成分、消炎鎮痛成分、抗炎症
成分、局所麻酔成分、抗ヒスタミン成分、ステロイド成
分、抗菌成分、保湿成分、ビタミン成分及び動植物エキ
スからなる群から選択される少なくとも1種である
(1)乃至(6)のいずれかに記載のエアゾール組成
物。That is, the present invention is an aerosol composition as follows: (1) A propellant, 2 to 35% by weight of urea and 30 to 30% of water.
An aerosol composition comprising an undiluted solution containing 90% by weight, wherein the mixing volume ratio of the propellant and the undiluted solution is 10:90 to 75:25 in the liquid state. (2) The mixing volume ratio of the propellant and the stock solution is 10 in the liquid state:
90 to 50:50, The aerosol composition according to (1). (3) The proportion of urea contained in 100% by weight of the stock solution is 5 to 5.
The aerosol composition according to (1) or (2), which is 30% by weight. (4) The aerosol composition according to any one of (1) to (3), wherein the propellant is at least one selected from dimethyl ether and liquefied petroleum gas. (5) The aerosol composition according to any one of (1) to (4), which further contains a lower alcohol in a proportion of 0.1 to 50% by weight in the stock solution. (6) The aerosol composition according to (5), wherein the undiluted solution further contains a polyhydric alcohol in a proportion of 0.1 to 30% by weight. (7) At least one selected from the group consisting of an antipruritic component, an antiphlogistic analgesic component, an anti-inflammatory component, a local anesthetic component, an antihistamine component, a steroid component, an antibacterial component, a moisturizing component, a vitamin component and an animal or plant extract in the stock solution. The aerosol composition according to any one of (1) to (6), which is
【0010】さらに本発明は上記のエアゾール組成物を
内容成分として有するエアゾール剤である。当該エアゾ
ール剤は、特に保湿効果、角質軟化効果または鎮痒効果
を有する外用剤(化粧料、医薬品、医薬部外品)として
有用である。よって、本発明は、エアゾール剤の形態を
有する保湿製剤、エアゾール剤の形態を有する角質軟化
製剤、エアゾール剤の形態を有する鎮痒製剤と言い換え
ることもできる。Further, the present invention is an aerosol agent containing the above aerosol composition as a content component. The aerosol is particularly useful as an external preparation (cosmetic, pharmaceutical, quasi drug) having a moisturizing effect, keratin softening effect or antipruritic effect. Therefore, the present invention can be restated as a moisturizing preparation in the form of an aerosol, a keratin softening preparation in the form of an aerosol, and an antipruritic preparation in the form of an aerosol.
【0011】また本発明は、水とともに尿素を必須成分
として含有するエアゾール組成物において尿素を安定に
保持する方法に関する。当該方法は、噴射剤と、尿素を
2〜35重量%及び水を30〜90重量%の割合で含有
する原液とを、液体状態で10:90〜75:25(容
積比)の割合で混合してなるエアゾール組成物を調製す
ることによって実現することができる。The present invention also relates to a method for stably holding urea in an aerosol composition containing urea as an essential component together with water. In this method, a propellant and a stock solution containing urea in an amount of 2 to 35% by weight and water in an amount of 30 to 90% by weight are mixed in a liquid state at a ratio of 10:90 to 75:25 (volume ratio). It can be realized by preparing an aerosol composition as described above.
【0012】さらに本発明は、水とともに尿素を必須成
分として含有するエアゾール組成物において尿素の分解
に起因する悪臭の発生を防止する方法に関する。当該方
法は、噴射剤と、尿素を2〜35重量%及び水を30〜
90重量%の割合で含有する原液とを、液体状態で1
0:90〜75:25(容積比)の割合で混合してなる
エアゾール組成物を調製することによって実現すること
ができる。Further, the present invention relates to a method for preventing the generation of a bad odor due to the decomposition of urea in an aerosol composition containing urea as an essential component together with water. The method comprises 2 to 35% by weight of propellant, urea and 30 to 30% of water.
90% by weight of the stock solution containing 1% in the liquid state
It can be realized by preparing an aerosol composition obtained by mixing at a ratio of 0:90 to 75:25 (volume ratio).
【0013】[0013]
【発明の実施の形態】本発明のエアゾール組成物は、尿
素と水を必須成分として含有する原液、及び噴射剤とか
らなるものである。BEST MODE FOR CARRYING OUT THE INVENTION The aerosol composition of the present invention comprises a stock solution containing urea and water as essential components, and a propellant.
【0014】ここで尿素は、前述するように、製剤中に
一定濃度以上の割合で配合することで角質の水分保持量
を増加させて乾燥性角化症における角質層の水分保有力
の低下を改善させたり、角質を溶解剥離させる作用を有
する他、皮膚透過性亢進作用、殺菌作用、創傷治癒作
用、細胞賦活作用、さらには、乾燥による掻痒の止痒作
用といった各種の作用を有することが知られている。従
って、本発明においてはこれらの尿素の効果を有効に発
揮させるために、エアゾール組成物に配合する原液(薬
液)100重量%中に尿素を2重量%以上の割合で配合
することが好ましい。本発明において、原液中に2重量
%以上の尿素を配合することによって、保湿効果、鎮痒
効果および角質軟化効果を有するエアゾール組成物、中
でも特に保湿効果に優れたエアゾール組成物を調製する
ことができる。また5重量%以上の尿素を配合すること
によって、特に鎮痒効果に優れたエアゾール組成物を調
製することができる。さらに10重量%以上の尿素を配
合することによって、特に角質軟化効果に優れたエアゾ
ール組成物を調製することができる。As described above, urea is added to the preparation at a ratio of a certain concentration or more to increase the water retention of the keratin and reduce the water retention of the stratum corneum in keratosis sicca. It is known that it has various actions such as improving action and dissolving and exfoliating keratin, as well as skin permeability enhancing action, bactericidal action, wound healing action, cell activation action, and further itching action of pruritus due to dryness. Has been. Therefore, in the present invention, in order to effectively bring out the effects of these ureas, it is preferable to add urea in an amount of 2% by weight or more to 100% by weight of the stock solution (chemical solution) to be added to the aerosol composition. In the present invention, by blending 2% by weight or more of urea in the undiluted solution, it is possible to prepare an aerosol composition having a moisturizing effect, an antipruritic effect and a keratin softening effect, and particularly an aerosol composition having an excellent moisturizing effect. . By blending 5% by weight or more of urea, an aerosol composition having a particularly excellent antipruritic effect can be prepared. Further, by blending 10% by weight or more of urea, an aerosol composition having an excellent keratin softening effect can be prepared.
【0015】原液に配合する尿素の上限は、エアゾール
組成物中の尿素の安定性、なかでも特に尿素の分解によ
る悪臭発生防止を考慮して、原液に配合する水の配合割
合、並びに原液と組み合わせて用いられる噴射剤の配合
割合との関係から規定することができる。本発明におい
ては原液(薬液)100重量%に配合する尿素の上限と
して35重量%、好ましくは30 重量%を挙げること
ができる。すなわち、本発明において、尿素を原液10
0重量%中に2〜35重量%、好ましくは5〜30重量
%の範囲で配合することによって、尿素が本来有する所
望の効果を発揮することができ、しかもその安定性に優
れたエアゾール組成物を調製することができる。The upper limit of urea to be added to the stock solution is the proportion of water to be added to the stock solution, and the combination with the stock solution, taking into consideration the stability of urea in the aerosol composition, and in particular, the prevention of generation of a bad odor due to decomposition of urea. Can be specified based on the relationship with the blending ratio of the propellant used. In the present invention, the upper limit of urea to be added to 100% by weight of the stock solution (chemical solution) is 35% by weight, preferably 30% by weight. That is, in the present invention, urea is used as the stock solution 10
By blending in an amount of 2 to 35% by weight, preferably 5 to 30% by weight in 0% by weight, the desired effect inherent to urea can be exhibited, and the aerosol composition is excellent in its stability. Can be prepared.
【0016】原液中に配合する水の配合割合は、尿素の
溶解性、及び安定性、なかでも特に尿素の分解による悪
臭発生防止を考慮して、上記する原液中の尿素の配合割
合、並びに原液と組み合わせて用いられる噴射剤の配合
割合との関係から規定することができる。原液100重
量%中の水の配合割合として通常30〜90重量%、好
ましくは30〜75重量%、より好ましくは30〜60
重量%の範囲を挙げることができる。The proportion of water to be added to the stock solution is such that the solubility and stability of urea and, above all, the prevention of a bad odor due to decomposition of urea can be taken into consideration. It can be specified from the relationship with the blending ratio of the propellant used in combination with. The proportion of water in the stock solution 100% by weight is usually 30 to 90% by weight, preferably 30 to 75% by weight, more preferably 30 to 60% by weight.
A range of weight% can be mentioned.
【0017】本発明のエアゾール組成物に用いられる原
液は、少なくとも上記の尿素及び水を必須成分とするも
のであればよく、本発明の効果を妨げないことを限度と
して他の成分を配合することは何等制限されない。The undiluted solution used in the aerosol composition of the present invention may contain at least the above urea and water as essential components, and may contain other components as long as the effects of the present invention are not impaired. Is not limited in any way.
【0018】かかる他成分として、例えば低級アルコー
ルを挙げることができる。ここで低級アルコールとして
は、例えば、エタノール、プロパノール、イソプロパノ
ール、ブタノールなどの炭素数1〜6の直鎖状若しくは
分岐状のアルコールを挙げることができる。中でも成分
の製剤安定性の面からエタノール、またはイソプロパノ
ールが好ましい。なお、これらの低級アルコールは1種
単独で使用しても、2種以上を任意に組み合わせて使用
することもできる。Examples of such other components include lower alcohols. Here, examples of the lower alcohol include linear or branched alcohols having 1 to 6 carbon atoms such as ethanol, propanol, isopropanol, butanol and the like. Among them, ethanol or isopropanol is preferable from the viewpoint of formulation stability of the components. These lower alcohols may be used alone or in any combination of two or more.
【0019】低級アルコールは、原液またはエアゾール
組成物に対する尿素または他の成分の安定性を高めるの
に有用である。例えば、他成分としてクロタミトンを配
合する場合には、低級アルコールによって溶解性を高
め、安定な製剤とすることができる。また、低級アルコ
ールの配合によってエアゾール組成物を皮膚に塗布した
際、気化熱によって皮膚に冷却感を与え、爽快感を与え
ることができる。さらに低級アルコールは、原液中の水
と噴射剤との相溶性を高め、エアゾール組成物を均質化
するのに有効である。Lower alcohols are useful in enhancing the stability of urea or other ingredients to stock solutions or aerosol compositions. For example, when crotamiton is added as another component, the solubility can be increased by a lower alcohol to make a stable formulation. Further, when an aerosol composition is applied to the skin by blending a lower alcohol, heat of vaporization gives the skin a cooling sensation and a refreshing sensation. Further, the lower alcohol is effective in increasing the compatibility between the water in the stock solution and the propellant and homogenizing the aerosol composition.
【0020】かかる効果を得る目的から、低級アルコー
ルを配合する場合は、原液100重量%中に0.1重量
%以上、好ましくは5重量%以上、より好ましくは10
重量%以上の割合で用いることが好ましい。なお、低級
アルコールの配合は、気化熱の放散によって冷却効果が
得られる反面、同時に皮脂を奪って皮膚の乾燥を招く傾
向があるため、かかる乾燥による悪影響を防止するため
には、原液に対して50重量%、好ましくは40重量%
を上限として配合することが好ましい。When a lower alcohol is blended for the purpose of obtaining such effects, 0.1% by weight or more, preferably 5% by weight or more, and more preferably 10% by weight in 100% by weight of the stock solution.
It is preferably used in a proportion of not less than wt%. It should be noted that the lower alcohol blending has a cooling effect by dissipating the heat of vaporization, but at the same time, tends to deprive sebum and cause skin dryness. 50% by weight, preferably 40% by weight
It is preferable to mix with the upper limit of.
【0021】また他の成分として、多価アルコールを挙
げることができる。ここで多価アルコールとしては、具
体的にはプロピレングリコール、1,3-ブチレングリコー
ル、グリセリン、ジエチレングリコール、トリエチレン
グリコール、ジプロピレングリコール、ヘキシレングリ
コール、ポリエチレングリコール、エトキシジグリコー
ルなどが例示される。なお、これらの多価アルコールは
1種単独で使用しても、2種以上を任意に組み合わせて
使用することもできる。好ましくは、安全性と保湿効果
の点から、プロピレングリコール、1,3-ブチレングリコ
ール、ジプロピレングリコール、ポリエチレングリコー
ル、エトキシジグリコールまたはグリセリンである。As another component, a polyhydric alcohol can be mentioned. Specific examples of the polyhydric alcohol include propylene glycol, 1,3-butylene glycol, glycerin, diethylene glycol, triethylene glycol, dipropylene glycol, hexylene glycol, polyethylene glycol and ethoxydiglycol. These polyhydric alcohols may be used alone or in any combination of two or more. From the viewpoint of safety and moisturizing effect, preferred are propylene glycol, 1,3-butylene glycol, dipropylene glycol, polyethylene glycol, ethoxydiglycol and glycerin.
【0022】多価アルコールの配合は、気化熱の放散に
よって生じる冷却感を緩和したり、脱脂による乾燥から
皮膚を保護するのに有効であることから、上記する低級
アルコールと併用して用いられることが好ましい。Since the polyhydric alcohol is effective in alleviating the cooling sensation caused by the dissipation of the heat of vaporization and protecting the skin from the dryness caused by degreasing, it is used in combination with the above lower alcohol. Is preferred.
【0023】多価アルコールを配合する場合は、原液1
00重量%中に0.1〜30重量%、好ましくは0.1〜
20重量%、より好ましくは3〜10重量%の割合で用
いることができる。When blending a polyhydric alcohol, the stock solution 1
0.1 to 30% by weight in 00% by weight, preferably 0.1 to
It can be used in a proportion of 20% by weight, more preferably 3 to 10% by weight.
【0024】また本発明に用いる原液には、尿素以外の
有効成分を配合することもできる。The stock solution used in the present invention may also contain an active ingredient other than urea.
【0025】このような有効成分としては、外用剤に通
常配合することのできる各種の有効成分を用いることが
できる。好ましくは保湿効果、鎮痒効果、角質軟化効果
を有するか、またこれらの効果を増強する効果を有する
成分が望ましい。具体的には、鎮痒成分、消炎鎮痛成
分、抗炎症成分、局所麻酔成分、抗ヒスタミン成分、ス
テロイド成分、抗菌成分、保湿成分、ビタミン成分、局
所麻痺成分、及び動植物エキスなどを例示することがで
きる。なお、これらの1種もしくは2種以上を組み合わ
せて使用することができる。As such an active ingredient, various active ingredients which can be usually added to an external preparation can be used. A component having a moisturizing effect, antipruritic effect, keratin softening effect, or an effect of enhancing these effects is desirable. Specifically, antipruritic components, antiphlogistic and analgesic components, anti-inflammatory components, local anesthetic components, antihistamine components, steroid components, antibacterial components, moisturizing components, vitamin components, local paralytic components, and animal and plant extracts can be exemplified. . In addition, these 1 type or 2 types or more can be used in combination.
【0026】ここで鎮痒成分としては、クロタミトン、
イクタモール、モクタモールまたはチモール酸などが例
示される。好ましくはクロタミトンである。また、消炎
鎮痛成分としては、インドメタシン、サリチル酸及びこ
れらの誘導体(サリチル酸メチル、サリチル酸モノグリ
コールエステルなど)、ケトプロフェン、フルルビプロ
フェン、ピロキシカム、ジクロフェナック、イブプロフ
ェン、またはメフェナム酸などが例示される。好ましく
はサリチル酸またはその誘導体である。抗炎症成分とし
ては、グアイアズレンまたはその塩、アラントイン、グ
リチルレチン酸またはその誘導体(グリチルレチン酸の
硝酸エステル若しくは酢酸エステルなど)、グリチルリ
チン酸またはその誘導体(グリチルリチン酸の硝酸エス
テル若しくは酢酸エステル、グリチルリチン酸ステアリ
ルなど)が例示される。好ましくは、アラントイン、グ
リチルレチン酸またはその誘導体、グリチルリチン酸ま
たはその誘導体である。局所麻酔成分としては、リドカ
イン、ジブカイン、アミノ酸安息香酸エチル等が例示で
きる。好ましくはリドカインまたはジブカインである。
抗ヒスタミン成分としてはクロルフェニラミン、ジフェ
ンヒドラミン、イソチベンジル及びこれらの誘導体等が
例示できる。ステロイド成分としては、ヒドロコルチゾ
ン、デキサメタゾン、プレドニゾロンまたはこれらの誘
導体等が例示できる。抗菌成分としては、ウンデシレン
酸、ペンタクロールフェノール、クロトリマゾール、ト
ルナフテート、トリコマイシン、ミコナゾール、ヨウ化
カリウム、クロルヘキシジン、アクリノール、ベンザル
コニウム、ペニシリン、テトラサイクリン、フラジオマ
イシン、カナマイシンまたはこれらの誘導体等が例示で
きる。Here, as the antipruritic ingredient, crotamiton,
Ictamol, moctamol, thymol acid, etc. are illustrated. Preferred is crotamiton. Examples of the anti-inflammatory and analgesic components include indomethacin, salicylic acid and derivatives thereof (methyl salicylate, salicylic acid monoglycol ester, etc.), ketoprofen, flurbiprofen, piroxicam, diclofenac, ibuprofen, mefenamic acid and the like. Salicylic acid or a derivative thereof is preferable. As the anti-inflammatory component, guaiazulene or a salt thereof, allantoin, glycyrrhetinic acid or a derivative thereof (such as a nitrate ester or acetic acid ester of glycyrrhetinic acid), glycyrrhizic acid or a derivative thereof (a nitrate ester or acetate ester of glycyrrhizinic acid, stearyl glycyrrhizinate, etc.) Is exemplified. Preferred are allantoin, glycyrrhetinic acid or a derivative thereof, and glycyrrhizic acid or a derivative thereof. Examples of the local anesthetic component include lidocaine, dibucaine, amino acid ethyl benzoate and the like. Lidocaine or dibucaine is preferred.
Examples of the antihistamine component include chlorpheniramine, diphenhydramine, isothibenzyl and derivatives thereof. Examples of the steroid component include hydrocortisone, dexamethasone, prednisolone, and their derivatives. Examples of the antibacterial component include undecylenic acid, pentachlorophenol, clotrimazole, tolnaftate, trichomycin, miconazole, potassium iodide, chlorhexidine, acrinol, benzalkonium, penicillin, tetracycline, fradiomycin, kanamycin or derivatives thereof. .
【0027】また、保湿成分としては、グリセリン、プ
ロピレングリコール、1,3-ブチレングリコール、ジプロ
ピレングリコール等の多価アルコール;スクワラン、流
動パラフィン、アボガド油、大豆油、ヒマシ油、コメ胚
芽油等の液状油;グリシン、アラニン、アスパラギン酸
等のアミノ酸;ソルビトール、マルチトール、トレハロ
ース、グルコースなどの糖類;乳酸またはピロリドンカ
ルボン酸の有機酸を例示することができる。ビタミン成
分としては、NMF成分や肌の損傷を回復したり、炎症
を抑える効果を有するものが好ましく、トコフェロール
などのビタミンE及びその誘導体、ピリドキシンなどの
ビタミンB6及びその誘導体、レチノールなどのビタミ
ンA及びその誘導体、パントテン酸及びその誘導体、ア
スコルビン酸等のビタミンC及びその誘導体、ビオチン
などを例示することができる。局所麻痺成分としては、
トウガラシ、カラシ、カンタリス、カンタリジン、カプ
サイシンなどが例示される。また、動植物エキスとして
は、保湿効果、抗炎症効果、または肌荒れに対して改善
効果のあると言われているものが好ましく、具体的に
は、ケラチン類、コラーゲン類、ヒアルロン酸、コンド
ロイチン硫酸、アロエ抽出物、ハマメリス抽出物、ロー
ズマリー抽出物、マロニエ抽出物、きゅうり抽出物、ト
ウキンセンカ抽出物、ローヤルゼリー抽出物、海藻抽出
物、茶抽出物、ニンジン抽出物、桃抽出物、桃の葉抽出
物、カンゾウ抽出物、オウゴン抽出物、ユーカリ抽出
物、ハッカ抽出物、ラベンダー抽出物、月見草抽出物、
カミツレ抽出物、トウキ抽出物、コメ発酵エキスなどが
挙げられる。As the moisturizing component, polyhydric alcohols such as glycerin, propylene glycol, 1,3-butylene glycol and dipropylene glycol; squalane, liquid paraffin, avocado oil, soybean oil, castor oil, rice germ oil, etc. Examples include liquid oils; amino acids such as glycine, alanine and aspartic acid; sugars such as sorbitol, maltitol, trehalose and glucose; organic acids such as lactic acid and pyrrolidonecarboxylic acid. As the vitamin component, those having an effect of recovering NMF component or skin damage and suppressing inflammation are preferable. Vitamin E and its derivatives such as tocopherol, vitamin B6 and its derivatives such as pyridoxine, vitamin A such as retinol and the like. Examples thereof include derivatives thereof, pantothenic acid and derivatives thereof, vitamin C such as ascorbic acid and derivatives thereof, biotin and the like. As a local paralysis component,
Examples include capsicum, mustard, cantharis, cantharidin, capsaicin and the like. In addition, as the animal and plant extract, those which are said to have a moisturizing effect, an anti-inflammatory effect, or an effect of improving skin roughness are preferred, and specifically, keratins, collagens, hyaluronic acid, chondroitin sulfate, aloe. Extract, hamamelis extract, rosemary extract, horse chestnut extract, cucumber extract, quince extract, royal jelly extract, seaweed extract, tea extract, carrot extract, peach extract, peach leaf extract , Licorice extract, sardine extract, eucalyptus extract, peppermint extract, lavender extract, evening primrose extract,
Examples thereof include chamomile extract, Japanese citrus extract, and fermented rice extract.
【0028】なお、前述する各具体的な成分には、その
薬学上許容される塩、特に外用を目的に当業界で通常使
用される薬学上許容される塩も包含される。The above-mentioned specific components include pharmaceutically acceptable salts thereof, particularly pharmaceutically acceptable salts usually used in the art for the purpose of external use.
【0029】本発明で用いる原液は、通常pH2〜10
の液性を備えていればよいが、皮膚に対する低刺激性、
及び皮膚使用感のよさという観点から、好ましくはpH
3〜9、より好ましくはpH5〜8の弱酸性〜中性であ
ることが望ましい。The stock solution used in the present invention usually has a pH of 2 to 10.
It should have the liquid property of
Also, from the viewpoint of good feeling on skin use, pH is preferable.
It is preferably 3 to 9, more preferably weakly acidic to neutral with a pH of 5 to 8.
【0030】また、原液の粘度が0.5cSt 未満である
とエアゾール組成物の皮膚付着性が低下し、また粘度が
20cSt を超えると皮膚にべたつき感が残る傾向があ
る。このため、良好な使用感を得るという点からは、原
液の粘度を、通常1cSt 〜20cStの範囲に調整するこ
とが望ましい。なお、ここで粘度は、BL粘度計(BL
アダプタ使用、回転数30rpm、測定温度29℃、密度
測定:ピクノメーター使用)で測定した動粘度を意味す
る。好ましくは1cSt 〜10cSt、より好ましくは1cSt
〜5cStである。If the viscosity of the undiluted solution is less than 0.5 cSt, the adhesion of the aerosol composition to the skin tends to be low, and if the viscosity exceeds 20 cSt, the skin tends to be sticky. Therefore, from the viewpoint of obtaining a good feeling in use, it is desirable to adjust the viscosity of the stock solution to a range of usually 1 cSt to 20 cSt. In addition, the viscosity here is a BL viscometer (BL
It means the kinematic viscosity measured by using an adapter, rotation speed 30 rpm, measuring temperature 29 ° C., density measurement: using pycnometer). Preferably 1 cSt to 10 cSt, more preferably 1 cSt
~ 5 cSt.
【0031】本発明のエアゾール組成物は、前述する原
液に噴射剤を配合して調製することができる。The aerosol composition of the present invention can be prepared by blending the above-mentioned stock solution with a propellant.
【0032】本発明で用いられる噴射剤としては、前述
する原液に対して相溶性を有するものであればよく、具
体的には液化石油ガス(例えばエタン、プロパン、エチ
レン、イソブタン、ノルマルブタン、プロピレンなどの
ように容易に液化するガス、これらの混合ガス[例え
ば、イソブタンとプロパン、プロパンとブタンの混合ガ
ス等])、エーテル系噴射剤(ジメチルエーテル等)、
フロロカーボン(例えば、フロロカーボン、クロロフロ
ロカーボン、ブロモクロロフロロカーボン)、圧縮ガス
(二酸化炭素、空気またはこれらの混合ガス名等)、ま
たはフロンガス(モノクロロジフルオロエタン、テトラ
フルオロエタン等)を例示することができる。なお、こ
れらの噴射剤は1種単独で使用しても2種以上を任意に
組み合わせて使用することもできる。好ましくはジメチ
ルエーテル、または液化石油ガスであり、特に好ましく
は、冷却感を含めた使用感に優れるジメチルエーテル、
またはジメチルエーテルと液化石油ガスとの混合ガスで
ある。The propellant used in the present invention may be any propellant having compatibility with the above-mentioned stock solution, and specifically, liquefied petroleum gas (eg, ethane, propane, ethylene, isobutane, normal butane, propylene). Such as a gas that easily liquefies, a mixed gas thereof [eg, a mixed gas of isobutane and propane, a mixed gas of propane and butane], an ether propellant (such as dimethyl ether),
Examples thereof include fluorocarbon (for example, fluorocarbon, chlorofluorocarbon, bromochlorofluorocarbon), compressed gas (carbon dioxide, air, mixed gas names thereof, etc.), or CFC gas (monochlorodifluoroethane, tetrafluoroethane, etc.). In addition, these propellants may be used alone or in any combination of two or more. Preferred is dimethyl ether, or liquefied petroleum gas, and particularly preferred is dimethyl ether, which has excellent usability including cooling feeling.
Alternatively, it is a mixed gas of dimethyl ether and liquefied petroleum gas.
【0033】本発明のエアゾール組成物における原液と
噴射剤の混合比は、液体状態における容量基準で原液:
噴射剤=25:75 〜90:10(容積比)であるこ
とが好ましい。より好ましくは原液:噴射剤=50:5
0 〜90:10である。エアゾール組成物中に配合さ
れる原液の割合が25容量%未満では、尿素の安定性が
十分に保持されない傾向があり、一方、噴射剤の割合が
25容量%未満であると、エアゾール剤として使用した
場合に有効成分と含む原液の全てを最後まで使用するこ
とができず、容器中に残液してしまう傾向がある。The mixing ratio of the undiluted solution and the propellant in the aerosol composition of the present invention is based on the volume of the undiluted solution:
It is preferable that the propellant is 25:75 to 90:10 (volume ratio). More preferably stock solution: propellant = 50: 5
It is 0 to 90:10. If the proportion of the undiluted solution blended in the aerosol composition is less than 25% by volume, the stability of urea tends not to be sufficiently maintained, while if the proportion of the propellant is less than 25% by volume, it is used as an aerosol agent. In such a case, all of the stock solution containing the active ingredient cannot be used to the end, and there is a tendency that the solution remains in the container.
【0034】本発明のエアゾール組成物には、必要に応
じて、清涼剤、溶解補助剤、界面活性剤、キレート剤、
pH調整剤、防腐剤、抗酸化剤、または香料等が配合さ
れていてもよい。In the aerosol composition of the present invention, if necessary, a cooling agent, a solubilizing agent, a surfactant, a chelating agent,
A pH adjuster, a preservative, an antioxidant, a fragrance, or the like may be added.
【0035】なかでも、清涼剤は、冷却感を増加させる
効果があり、使用感に優れるのみならず、痒みを即効的
に抑制する効果を有するため鎮痒を目的としたエアゾー
ル剤の調製には有用である。清涼剤としては、l- メン
トールや3- L- メトキシプロパン- 1,2- ジオールが好
ましい。とくに、l- メントールまたはl−メントール
を含有する精油が好ましい。Among them, the cooling agent has the effect of increasing the cooling sensation and not only excels in the feeling of use, but also has the effect of immediately suppressing the itch, which is useful for the preparation of an aerosol for the purpose of antipruritus. Is. As the cooling agent, l-menthol and 3-L-methoxypropane-1,2-diol are preferable. Particularly, 1-menthol or an essential oil containing 1-menthol is preferable.
【0036】また、溶解補助剤としては、アジピン酸ジ
イソプロピル、ミリスチン酸イソプロピル、1,3−ブ
チレングリコール、プロピレングリコール、ポリエチレ
ングリコール、グリセリン、乳酸、水酸化ナトリウム
等;界面活性剤としては、ポリオキシエチレンソルビタ
ン脂肪酸エステル、ソルビタン脂肪酸エステル、ポリオ
キシエチレン硬化ヒマシ油、ポリオキシエチレンポリオ
キシプロピレンアルキルエーテル、ポリオキシエチレン
セチルエーテル、モノステアリン酸グリセリル等;キレ
ート剤としてはエデト酸類、ヒドロキシエタンジホスホ
ン酸類、フィチン酸等;防腐剤としてはパラベン、安息
香酸塩、イソプロピルメチルフェノール等;抗酸化剤と
しては酢酸トコフェロール、ジブチルヒドロキシトルエ
ン、ブチルヒドロキシトルエン等が例示できる。As the solubilizing agent, diisopropyl adipate, isopropyl myristate, 1,3-butylene glycol, propylene glycol, polyethylene glycol, glycerin, lactic acid, sodium hydroxide and the like; as the surfactant, polyoxyethylene Sorbitan fatty acid ester, sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene cetyl ether, glyceryl monostearate, etc .; chelating agents edetic acids, hydroxyethanediphosphonic acids, phytin Acids and the like; preservatives such as paraben, benzoate, isopropylmethylphenol and the like; antioxidants such as tocopherol acetate, dibutylhydroxytoluene and butylhydroxy Toluene and the like.
【0037】本発明のエアゾール組成物は、原液と噴射
剤をスチールまたはアルミなどのエアゾール容器に公知
の方法により充填してエアゾール形態として使用され
る。本発明の目的が損なわれない限り、原液の組成のみ
ならず、内容物の噴射量または噴霧・噴射状態は、エア
ゾール容器内の圧力やエアゾール容器のバルブにおける
噴射孔径またはステム通路の径等を適宜設定することに
よって目的に応じて適宜選択して使用することができ
る。The aerosol composition of the present invention is used in the form of an aerosol by filling a stock solution and a propellant into an aerosol container such as steel or aluminum by a known method. As long as the object of the present invention is not impaired, not only the composition of the undiluted solution, but also the injection amount or spraying / injection state of the content, the pressure in the aerosol container, the injection hole diameter in the valve of the aerosol container, the diameter of the stem passage, etc. are appropriately set. By setting, it can be appropriately selected and used according to the purpose.
【0038】本発明のエアゾール組成物は、例えば、フ
ァンデーション、口紅、及び美爪料等のメーキャップ化
粧料や基礎化粧料;洗顔料やクレンジング、ボディ洗浄
料などの洗浄料;腋臭防止剤、水虫治療剤、鎮痒剤、創
傷治癒剤、消炎鎮痛剤、にきび治療剤、殺菌消毒剤、美
白剤、紫外線防御剤、保湿剤、角質軟化剤などの、化粧
品、外用医薬品または外用医薬部外品の分野に属する各
種の外用用途にエアゾール剤として使用することができ
る。本発明は、尿素の効果である保湿効果、角質軟化効
果または鎮痒効果を有するエアゾール剤として調製され
ることが好ましい。具体的には、保湿効果、角質軟化効
果または鎮痒効果を有するエアゾール剤形態の化粧料ま
たは洗浄料、エアゾール剤の形態を有する鎮痒製剤、保
湿製剤または角質軟化製剤を例示することができる。The aerosol composition of the present invention can be applied to makeup cosmetics such as foundations, lipsticks, and nail enamel, and basic cosmetics; cleansing agents such as face cleansing agents, cleansing agents, and body wash agents; armpit deodorants, athlete's foot remedies. In the field of cosmetics, topical drugs or quasi-drugs such as agents, antipruritic agents, wound healing agents, anti-inflammatory analgesics, acne treatment agents, antiseptic agents, whitening agents, UV protectants, moisturizers, keratin softeners, etc. It can be used as an aerosol for various external applications to which it belongs. The present invention is preferably prepared as an aerosol agent having a moisturizing effect, a keratin softening effect or an antipruritic effect which is the effect of urea. Specific examples include cosmetics or detergents in the form of an aerosol having a moisturizing effect, keratin softening effect or antipruritic effect, and an antipruritic preparation, a moisturizing preparation or a keratin softening preparation in the form of an aerosol.
【0039】[0039]
【実施例】以下に本発明を実施例及び試験例に基づいて
さらに詳細に説明するが、本発明はこれら実施例等に限
定されるものではない。なお、下記の各処方において%
とは、特に言及しない限り、重量(W/W)%を意味する
ものとする。EXAMPLES The present invention will be described below in more detail based on Examples and Test Examples, but the present invention is not limited to these Examples and the like. In each prescription below,%
Unless otherwise specified, it means% by weight (W / W).
【0040】 実施例1 保湿製剤 <原液> 尿素 10.0(%) ビタミンE 5.0 1,3−ブチレングリコール 5.0 エタノール 40.0 精製水 40.0 合 計 100.0% <噴射剤> ジメチルエーテル 100.0% <原液>:<噴射剤>=70:30(容積比) Example 1 Moisturizing preparation <stock solution> Urea 10.0 (%) Vitamin E 5.0 1,3-butylene glycol 5.0 Ethanol 40.0 Purified water 40.0 Total 100.0% <Propellant > Dimethyl ether 100.0% <stock solution>: <propellant> = 70:30 (volume ratio)
【0041】 実施例2 化粧料 <原液> 尿素 5.0(%) グリセリン 5.0 乳酸 1.5 エタノール 30.0 香料 0.1 精製水 58.4 合 計 100.0% <噴射剤> 液化石油ガス 100.0% <原液:噴射剤>=60:40(容積比)。 Example 2 Cosmetic <Undiluted solution> Urea 5.0 (%) Glycerin 5.0 Lactic acid 1.5 Ethanol 30.0 Fragrance 0.1 Purified water 58.4 Total 100.0% <Propellant> Liquefaction Petroleum gas 100.0% <stock solution: propellant> = 60:40 (volume ratio).
【0042】 実施例3 皮膚保護フォーム <原液> 尿素 7.0(%) ヒドロキシエチルセルロース 0.3 キサンタンガム 0.1 プロピレングリコール 5.0 スクワラン 1.0 セタノール 1.0 モノステアリン酸グリセリル 0.2 ポリオキシエチレンセチルエーテル 0.3 KSG16(信越化学) 0.5 ラウリルメチルタウリンNa 3.0 エタノール 1.0 香料 0.2 精製水 80.4 合 計 100.0% <噴射剤> ジメチルエーテル 50.0 液化石油ガス 50.0 100.0% <原液:噴射剤>=55:45(容積比)。 Example 3 Skin Protective Foam <Undiluted solution> Urea 7.0 (%) Hydroxyethyl cellulose 0.3 Xanthan gum 0.1 Propylene glycol 5.0 Squalane 1.0 Cetanol 1.0 Glyceryl monostearate 0.2 Polyoxy Ethylene cetyl ether 0.3 KSG16 (Shin-Etsu Chemical) 0.5 Laurylmethyl taurine Na 3.0 Ethanol 1.0 Perfume 0.2 Purified water 80.4 Total 100.0% <Propellant> Dimethyl ether 50.0 Liquefied petroleum Gas 50.0 100.0% <stock solution: propellant> = 55:45 (volume ratio).
【0043】 実施例4 シェービングフォーム <原液> 尿素 15.0(%) ステアリン酸ポリグリセリド 1.0 ジプロピレングリコール 20.0 ステアリン酸 0.5 セタノール 2.0 パラフィン 0.5 ポリオキシエチレン硬化ヒマシ油 1.0 シリコーンKF-96A(20cs)(信越化学) 1.0 ヒドロキシエチルセルロース 0.4 水酸化ナトリウム(pH7に調整) 0〜0.1 精製水 58.5〜58.6 合 計 100.0% <噴射剤> 液化石油ガス 100.0% <原液:噴射剤>=95:5(容積比)。 Example 4 Shaving foam <stock solution> Urea 15.0 (%) Stearic acid polyglyceride 1.0 Dipropylene glycol 20.0 Stearic acid 0.5 Cetanol 2.0 Paraffin 0.5 Polyoxyethylene hydrogenated castor oil 1.0 Silicone KF-96A (20cs) (Shin-Etsu Chemical) 1.0 Hydroxyethyl cellulose 0.4 Sodium hydroxide (adjusted to pH 7) 0-0.1 Purified water 58.5-58.6 Total 100.0% <Propellant> Liquefied petroleum gas 100.0% <Undiluted solution: propellant> = 95: 5 (volume ratio).
【0044】 実施例5 鎮痒製剤 <原液> 尿素 8.0(%) マレイン酸クロルフェニラミン 1.0 クロタミトン 5.0 プレドニゾロン 0.1 アラントイン 0.1 イソプロピルメチルフェノール 0.1 l−メントール 0.2 エタノール 40.0 精製水 45.5 合 計 100.0% <噴射剤> 液化石油ガス:ジメチルエーテル=50:50 <原液:噴射剤>=80:20(容積比)。 Example 5 Antipruritic preparation <stock solution> Urea 8.0 (%) Chlorpheniramine maleate 1.0 Crotamiton 5.0 Prednisolone 0.1 Allantoin 0.1 Isopropylmethylphenol 0.1 l-Menthol 0.2 Ethanol 40.0 Purified water 45.5 Total 100.0% <propellant> Liquefied petroleum gas: dimethyl ether = 50:50 <stock solution: propellant> = 80:20 (volume ratio).
【0045】 実施例6 水虫用製剤 <原液> 尿素 5.0(%) 硝酸スルコナゾール 0.5 塩酸ジブカイン 0.1 エタノール 3.0 精製水 91.4 合 計 100.0% <噴射剤> ジメチルエーテル:液化石油ガス=90:10 <原液:噴射剤>=50:50(容積比)。 Example 6 Preparation for athlete's foot <stock solution> Urea 5.0 (%) Sulconazole nitrate 0.5 Dibucaine hydrochloride 0.1 Ethanol 3.0 Purified water 91.4 Total 100.0% <Propellant> Dimethyl ether: Liquefied petroleum gas = 90:10 <stock solution: propellant> = 50:50 (volume ratio).
【0046】 実施例7 角質軟化製剤 <原液> 尿素 25.0(%) ポリオキシエチレンソルビタン脂肪酸エステル 1.0 グリセリン 3.0 ホホバ油 5.0 精製水 66.0 合 計 100.0%。 <噴射剤> ジメチルエーテル:液化石油ガス=40:60 <原液:噴射剤>=80:15(容積比)。 Example 7 Keratin softening preparation <stock solution> urea 25.0 (%) polyoxyethylene sorbitan fatty acid ester 1.0 glycerin 3.0 jojoba oil 5.0 purified water 66.0 total 100.0%. <Propellant> dimethyl ether: liquefied petroleum gas = 40:60 <stock solution: propellant> = 80:15 (volume ratio).
【0047】試験例1 エアゾール組成物における尿素
の安定性
表1に記載する処方に従って、尿素と水を所定量の割合
で含有する原液を調製し、次いでこの原液と噴射剤を所
定の割合で混合し、エアゾール缶に充填し、40℃の恒
温槽に1ヶ月間保存して、尿素の安定性(耐分解性、溶
解安定性)を確認した(実施例8〜16、比較例1〜
4)。 Test Example 1 Stability of Urea in Aerosol Composition According to the formulation shown in Table 1, a stock solution containing urea and water at a predetermined ratio was prepared, and then this stock solution and a propellant were mixed at a predetermined ratio. Then, it was filled in an aerosol can and stored in a constant temperature bath at 40 ° C. for 1 month to confirm the stability of urea (decomposition resistance, dissolution stability) (Examples 8 to 16 and Comparative Examples 1 to 1).
4).
【0048】(1)安定性(耐分解性)
エアゾール組成物(実施例8〜16、比較例1〜4)の
安定性(耐分解性)は、尿素は分解するとアンモニアを
発生することを利用して、1.5秒間スプレーした際の
噴霧物のアンモニア臭の有無から評価した。(1) Stability (decomposition resistance) The stability (decomposition resistance) of aerosol compositions (Examples 8 to 16 and Comparative Examples 1 to 4) is based on the fact that urea decomposes to generate ammonia. Then, the presence or absence of ammonia odor in the sprayed product when sprayed for 1.5 seconds was evaluated.
【0049】アンモニア臭の強さを下記に示す5段階で
評価した。
− アンモニア臭を感じない
+ 微量感じる
++ 有意に感じる
+++ かなり感じる
++++ 強く感じる
+++++ 不快なほど強く感じる。The strength of ammonia odor was evaluated according to the following 5 grades. − Do not feel the smell of ammonia + Feel a slight amount ++ Significantly feel ++++ Feel strongly ++++ Feel strongly ++++++ Feel uncomfortably strong.
【0050】(2)溶解安定性
エアゾール組成物(実施例8〜16、比較例1〜4)の
溶解安定性は、エアゾール缶の内容物(エアゾール組成
物)の状態を顕微鏡で観察して沈殿物若しくは結晶析出
の有無を調べることによって評価した。さらに、噴霧
後、エアゾール缶を室温に1日間放置した後の該缶の噴
射口における結晶析出の有無を目視で観察した。結晶析
出の有無については有りを+、無しを−で評価した。結
果を表1に合わせて示す。(2) Dissolution stability The dissolution stability of the aerosol compositions (Examples 8 to 16 and Comparative Examples 1 to 4) was determined by observing the state of the contents of the aerosol can (aerosol composition) with a microscope and causing precipitation. It was evaluated by examining the presence or absence of a substance or crystal precipitation. Further, after spraying, the aerosol can was left at room temperature for 1 day, and then the presence or absence of crystal precipitation at the injection port of the can was visually observed. The presence / absence of crystal precipitation was evaluated as "+" for existence and "-" for absence. The results are also shown in Table 1.
【0051】[0051]
【表1】 [Table 1]
【0052】表1の結果からわかるように、本発明の処
方からなるエアゾール組成物は、いずれも熱安定性(耐
分解性、溶解安定性)に優れており、この結果から長期
保存においても尿素を安定して保有することが示され
た。As can be seen from the results in Table 1, all of the aerosol compositions having the formulations of the present invention have excellent thermal stability (decomposition resistance, dissolution stability), and the results show that even after long-term storage, urea composition Have been shown to be stably held.
【0053】[0053]
【発明の効果】本発明のエアゾール組成物は、尿素と水
を特定の割合で含有する原液を特定の割合で噴射剤と配
合して調製されてなることを特徴とするものである。か
かる処方によって調製された本発明のエアゾール組成物
によれば、水の共存下でも尿素を長期にわたり安定して
保有するため、配合した量に応じて尿素の所望の効果
(保湿効果、角質軟化硬化、鎮痒効果)を発揮できると
ともに、尿素の分解による悪臭の発生がないため噴霧吐
出して使用されるエアゾール剤(噴霧剤)の内容組成物
として適している。また本発明のエアゾール組成物は、
長期保存によっても尿素が析出したり沈殿することなく
安定して保有されるため、エアゾール容器の吐出口に詰
まるなどといった不都合も生じず、エアゾール剤(噴霧
剤)の内容組成物として有用に使用することができる。The aerosol composition of the present invention is characterized by being prepared by blending a stock solution containing urea and water in a specific ratio with a propellant in a specific ratio. According to the aerosol composition of the present invention prepared by such a formulation, urea is stably retained for a long period of time even in the coexistence of water, and therefore, the desired effect of urea (moisturizing effect, keratin softening and hardening) is obtained according to the blended amount. It is suitable as a content composition of an aerosol agent (spray agent) to be used by spray discharge because it can exert an antipruritic effect) and does not generate a bad odor due to decomposition of urea. Further, the aerosol composition of the present invention,
Since urea is stably retained without precipitation or precipitation even after long-term storage, it does not cause inconveniences such as clogging of the discharge port of an aerosol container, and is useful as a content composition of an aerosol agent (spray agent). be able to.
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.7 識別記号 FI テーマコート゛(参考) A61K 7/00 A61K 7/00 S 9/12 9/12 45/00 45/00 47/06 47/06 47/10 47/10 A61P 17/00 A61P 17/00 17/04 17/04 17/16 17/16 Fターム(参考) 4C076 AA24 BB31 CC04 CC18 CC20 DD34 DD37 DD38 DD39 FF57 FF70 4C083 AB032 AC011 AC012 AC022 AC072 AC101 AC102 AC111 AC122 AC152 AC171 AC172 AC182 AC242 AC302 AC392 AC432 AC681 AC682 AC792 AD042 AD112 AD282 AD352 AD662 CC21 DD08 EE10 EE12 4C084 AA02 AA03 AA16 AA27 CA13 CA17 CA59 MA02 MA13 MA63 NA05 ZA082 ZA212 ZA902 ZA912 ZB112 ZC132 4C206 AA01 HA27 MA01 MA02 MA05 MA83 NA05 ZA89 ZA91 ─────────────────────────────────────────────────── ─── Continued Front Page (51) Int.Cl. 7 Identification Code FI Theme Coat (Reference) A61K 7/00 A61K 7/00 S 9/12 9/12 45/00 45/00 47/06 47/06 47/10 47/10 A61P 17/00 A61P 17/00 17/04 17/04 17/16 17/16 F term (reference) 4C076 AA24 BB31 CC04 CC18 CC20 DD34 DD37 DD38 DD39 FF57 FF70 4C083 AB032 AC011 AC012 AC022 AC072 AC101 AC102 AC111 AC122 AC152 AC171 AC172 AC182 AC242 AC302 AC392 AC432 AC681 AC682 AC792 AD042 AD112 AD282 AD352 AD662 CC21 DD08 EE10 EE12 4C084 AA02 AA03 AA16 AA27 CA13 CA17 CA59 MA02 MA13 MA63 NA05 ZA082 ZA212 ZA902 ZA912 ZB112 ZC132 4C206 AA01 HA27 MA01 MA02 MA05 MA83 NA05 ZA89 ZA91
Claims (7)
30〜90重量%の割合で含有する原液とからなるエア
ゾール組成物であって、噴射剤と原液との混合容積比が
液体状態で10:90〜75:25であることを特徴と
するエアゾール組成物。1. An aerosol composition comprising a propellant and a stock solution containing urea in an amount of 2 to 35% by weight and water in an amount of 30 to 90% by weight, wherein a mixing volume ratio of the propellant to the stock solution is 1. An aerosol composition, which is 10:90 to 75:25 in a liquid state.
l0:90〜50:50であることを特徴とする請求項
1に記載のエアゾール組成物。2. The aerosol composition according to claim 1, wherein the mixing volume ratio of the propellant and the stock solution is 10:90 to 50:50 in the liquid state.
が5〜30重量%である請求項1または2に記載のエア
ゾール組成物。3. The aerosol composition according to claim 1, wherein the proportion of urea contained in 100% by weight of the stock solution is 5 to 30% by weight.
ガスの中から選択される少なくとも1種である請求項1
乃至3のいずれかに記載のエアゾール組成物。4. The propellant is at least one selected from dimethyl ether and liquefied petroleum gas.
The aerosol composition according to any one of 1 to 3.
50重量%の割合で含有する請求項1乃至4のいずれか
に記載のエアゾール組成物。5. A lower alcohol is further added to the stock solution in an amount of 0.1 to 1.
The aerosol composition according to any one of claims 1 to 4, which is contained in a proportion of 50% by weight.
30重量%の割合で含有する請求項5に記載のエアゾー
ル組成物。6. A polyhydric alcohol is further added to the stock solution in an amount of 0.1 to 10.
The aerosol composition according to claim 5, which is contained in a proportion of 30% by weight.
抗炎症成分、局所麻酔成分、抗ヒスタミン成分、ステロ
イド成分、抗菌成分、保湿成分、ビタミン成分及び動植
物エキスからなる群から選択される少なくとも1種であ
る請求項1乃至6のいずれかに記載のエアゾール組成
物。7. An antipruritic component, an anti-inflammatory analgesic component in the stock solution,
The aerosol according to any one of claims 1 to 6, which is at least one selected from the group consisting of an anti-inflammatory component, a local anesthetic component, an antihistamine component, a steroid component, an antibacterial component, a moisturizing component, a vitamin component and an animal or plant extract. Composition.
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