JP2023183349A - Solid composition for external use - Google Patents
Solid composition for external use Download PDFInfo
- Publication number
- JP2023183349A JP2023183349A JP2022096927A JP2022096927A JP2023183349A JP 2023183349 A JP2023183349 A JP 2023183349A JP 2022096927 A JP2022096927 A JP 2022096927A JP 2022096927 A JP2022096927 A JP 2022096927A JP 2023183349 A JP2023183349 A JP 2023183349A
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- JP
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- Prior art keywords
- component
- solid
- wax
- present
- mass
- 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
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- 239000008247 solid mixture Substances 0.000 title claims abstract description 25
- 239000007787 solid Substances 0.000 claims abstract description 102
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 22
- 229940088594 vitamin Drugs 0.000 claims abstract description 17
- 229930003231 vitamin Natural products 0.000 claims abstract description 17
- 235000013343 vitamin Nutrition 0.000 claims abstract description 17
- 239000011782 vitamin Substances 0.000 claims abstract description 17
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 15
- 238000002844 melting Methods 0.000 claims abstract description 14
- 230000008018 melting Effects 0.000 claims abstract description 14
- 150000003722 vitamin derivatives Chemical class 0.000 claims abstract description 8
- 239000000203 mixture Substances 0.000 claims description 105
- -1 glycerin fatty acid ester Chemical class 0.000 claims description 41
- 239000001993 wax Substances 0.000 claims description 36
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 14
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 13
- 239000000194 fatty acid Substances 0.000 claims description 13
- 229930195729 fatty acid Natural products 0.000 claims description 13
- 235000011187 glycerol Nutrition 0.000 claims description 10
- 235000010323 ascorbic acid Nutrition 0.000 claims description 9
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- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 claims description 7
- 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 claims description 6
- GHOKWGTUZJEAQD-ZETCQYMHSA-N (D)-(+)-Pantothenic acid Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-ZETCQYMHSA-N 0.000 claims description 6
- 229960005070 ascorbic acid Drugs 0.000 claims description 6
- 229940071097 ascorbyl phosphate Drugs 0.000 claims description 6
- RMRCNWBMXRMIRW-BYFNXCQMSA-M cyanocobalamin Chemical compound N#C[Co+]N([C@]1([H])[C@H](CC(N)=O)[C@]\2(CCC(=O)NC[C@H](C)OP(O)(=O)OC3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)C)C/2=C(C)\C([C@H](C/2(C)C)CCC(N)=O)=N\C\2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O RMRCNWBMXRMIRW-BYFNXCQMSA-M 0.000 claims description 6
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims description 6
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- AUNGANRZJHBGPY-UHFFFAOYSA-N D-Lyxoflavin Natural products OCC(O)C(O)C(O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-UHFFFAOYSA-N 0.000 claims description 4
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- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 claims description 4
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- DBSABEYSGXPBTA-RXSVEWSESA-N (2r)-2-[(1s)-1,2-dihydroxyethyl]-3,4-dihydroxy-2h-furan-5-one;phosphoric acid Chemical compound OP(O)(O)=O.OC[C@H](O)[C@H]1OC(=O)C(O)=C1O DBSABEYSGXPBTA-RXSVEWSESA-N 0.000 claims description 3
- GHOKWGTUZJEAQD-UHFFFAOYSA-N Chick antidermatitis factor Natural products OCC(C)(C)C(O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-UHFFFAOYSA-N 0.000 claims description 3
- MLSJBGYKDYSOAE-DCWMUDTNSA-N L-Ascorbic acid-2-glucoside Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=C1O MLSJBGYKDYSOAE-DCWMUDTNSA-N 0.000 claims description 3
- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 claims description 3
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 claims description 3
- 229910019142 PO4 Inorganic materials 0.000 claims description 3
- 239000004698 Polyethylene Substances 0.000 claims description 3
- 229940072107 ascorbate Drugs 0.000 claims description 3
- 229940067599 ascorbyl glucoside Drugs 0.000 claims description 3
- 235000010385 ascorbyl palmitate Nutrition 0.000 claims description 3
- 229960002685 biotin Drugs 0.000 claims description 3
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- 239000011666 cyanocobalamin Substances 0.000 claims description 3
- 125000002801 octanoyl group Chemical group C(CCCCCCC)(=O)* 0.000 claims description 3
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- 235000019161 pantothenic acid Nutrition 0.000 claims description 3
- 239000011713 pantothenic acid Substances 0.000 claims description 3
- 239000010452 phosphate Substances 0.000 claims description 3
- 229920000573 polyethylene Polymers 0.000 claims description 3
- 235000019171 pyridoxine hydrochloride Nutrition 0.000 claims description 3
- 239000011764 pyridoxine hydrochloride Substances 0.000 claims description 3
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- 241001553290 Euphorbia antisyphilitica Species 0.000 claims description 2
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 claims description 2
- DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 229960000304 folic acid Drugs 0.000 claims description 2
- 239000004137 magnesium phosphate Substances 0.000 claims description 2
- 229960002261 magnesium phosphate Drugs 0.000 claims description 2
- 229910000157 magnesium phosphate Inorganic materials 0.000 claims description 2
- 235000010994 magnesium phosphates Nutrition 0.000 claims description 2
- 229960003495 thiamine Drugs 0.000 claims description 2
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- JZRWCGZRTZMZEH-UHFFFAOYSA-N Thiamine Natural products CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N JZRWCGZRTZMZEH-UHFFFAOYSA-N 0.000 claims 1
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- 150000003839 salts Chemical class 0.000 claims 1
- 235000002639 sodium chloride Nutrition 0.000 claims 1
- 235000019157 thiamine Nutrition 0.000 claims 1
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- KYMBYSLLVAOCFI-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SCN1CC1=CN=C(C)N=C1N KYMBYSLLVAOCFI-UHFFFAOYSA-N 0.000 claims 1
- 230000000694 effects Effects 0.000 description 36
- 239000004615 ingredient Substances 0.000 description 15
- 230000000699 topical effect Effects 0.000 description 12
- 238000009472 formulation Methods 0.000 description 11
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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 8
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 description 8
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- 235000019198 oils Nutrition 0.000 description 8
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 7
- 239000007788 liquid Substances 0.000 description 7
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- 230000003020 moisturizing effect Effects 0.000 description 6
- 235000007586 terpenes Nutrition 0.000 description 6
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 5
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- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 5
- ARIWANIATODDMH-UHFFFAOYSA-N rac-1-monolauroylglycerol Chemical compound CCCCCCCCCCCC(=O)OCC(O)CO ARIWANIATODDMH-UHFFFAOYSA-N 0.000 description 5
- IZHVBANLECCAGF-UHFFFAOYSA-N 2-hydroxy-3-(octadecanoyloxy)propyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)COC(=O)CCCCCCCCCCCCCCCCC IZHVBANLECCAGF-UHFFFAOYSA-N 0.000 description 4
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- 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 4
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- 230000000704 physical effect Effects 0.000 description 1
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- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 description 1
- LKUNXBRZDFMZOK-UHFFFAOYSA-N rac-1-monodecanoylglycerol Chemical compound CCCCCCCCCC(=O)OCC(O)CO LKUNXBRZDFMZOK-UHFFFAOYSA-N 0.000 description 1
- DCBSHORRWZKAKO-UHFFFAOYSA-N rac-1-monomyristoylglycerol Chemical compound CCCCCCCCCCCCCC(=O)OCC(O)CO DCBSHORRWZKAKO-UHFFFAOYSA-N 0.000 description 1
- 229940108325 retinyl palmitate Drugs 0.000 description 1
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- TUNFSRHWOTWDNC-UHFFFAOYSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 description 1
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- HTJNEBVCZXHBNJ-XCTPRCOBSA-H trimagnesium;(2r)-2-[(1s)-1,2-dihydroxyethyl]-3,4-dihydroxy-2h-furan-5-one;diphosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.OC[C@H](O)[C@H]1OC(=O)C(O)=C1O HTJNEBVCZXHBNJ-XCTPRCOBSA-H 0.000 description 1
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- 239000011691 vitamin B1 Substances 0.000 description 1
- 235000019163 vitamin B12 Nutrition 0.000 description 1
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- 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
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Abstract
Description
本発明は、固形外用組成物に関する。 The present invention relates to solid external compositions.
水溶性ビタミンが配合された外用組成物は、皮膚の疾患や症状、状態を治療、予防及び/又は改善する目的で有益である。固形外用組成物に水溶性ビタミンを配合することが試みられてきたが、固形状に成形し、使用感に優れた固形外用組成物の実現には多くの課題があった。 External compositions containing water-soluble vitamins are useful for treating, preventing, and/or improving skin diseases, symptoms, and conditions. Attempts have been made to incorporate water-soluble vitamins into solid compositions for external use, but there have been many problems in realizing solid compositions for external use that can be molded into a solid form and have an excellent feel when used.
ニコチン酸アミド、液状油、油性増粘剤、シリカを含有する油性皮膚外用剤又は油性化粧料において、ニコチン酸アミドを均一に分散し、経時的安定を達成する試みがなされているが(特許文献1)、固体粒子であるシリカを含有する組成物を皮膚に塗布すると、組成物による皮膚の保湿が不十分であった。 Attempts have been made to uniformly disperse nicotinic acid amide and achieve stability over time in oily skin external preparations or oily cosmetics containing nicotinic acid amide, liquid oil, oily thickeners, and silica (Patent Documents 1) When a composition containing solid particles of silica was applied to the skin, the moisturizing of the skin by the composition was insufficient.
本発明の目的は、成形性が良好で、使用感の良い固形外用組成物を提供することにある。 An object of the present invention is to provide a solid composition for external use that has good moldability and is comfortable to use.
本発明者は、(A)融点が40℃以上である固形ワックス、(B)水溶性ビタミン、及び(C)多価アルコールを組み合わせて配合し、水の含有量が2質量%以下となる外用組成物とすることにより、該外用組成物を、固形状に成形することができ、皮膚に適用した場合の使用感が高められることを見出し、本発明を完成するに至った。 The present inventor has formulated a combination of (A) a solid wax with a melting point of 40°C or higher, (B) a water-soluble vitamin, and (C) a polyhydric alcohol, and has developed a method for external use with a water content of 2% by mass or less. The present inventors have discovered that by forming a composition, the external composition can be formed into a solid shape, and the feeling of use when applied to the skin is enhanced, and the present invention has been completed.
すなわち、本発明は、
[1](A)融点が40℃以上である固形ワックス、(B)水溶性ビタミン、及び(C)多価アルコールを含有し、水の含有量が2質量%以下である、固形外用組成物;
[2](D)グリセリン脂肪酸エステルを含有する、[1]に記載の固形外用組成物;
[3](E)テルペノイドを含有する、[1]又は[2]に記載の固形外用組成物;
[4](F)液状油を含有する、[1]から[3]に記載の固形外用組成物;
[5](G)ペースト油を含有する、[1]から[4]に記載の固形外用組成物;
[6]前記(A)がパラフィンワックス、マイクロクリスタリンワックス、ポリエチレンワックス、フィッシャートロプシュワックス、カルナウバロウ及びキャンデリラからなる群より選択される1種以上、並びに、前記(B)がニコチン酸アミド、チアミン塩酸塩、チアミンリン酸塩、リボフラビン、葉酸(プテロイルモノグルタミン酸)、ピリドキシン塩酸塩、シアノコバラミン、ビオチン、パントテン酸、アスコルビン酸、アスコルビルグルコシド、アスコルビルリン酸塩、リン酸アスコルビルマグネシウム、アスコルビン酸エチル、パルミチン酸アスコルビルリン酸塩、イソステアリルアスコルビルリン酸塩及びカプリリル2-グリセリルアスコルビン酸からなる群より選択される1種以上を含有する、[1]から[5]に記載の固形外用組成物;
[7]前記(D)がジイソステアリン酸ポリグリセリルである、[2]に記載の固形外用組成物;
[8]前記(E)が環式テルペンである、[3]に記載の固形外用組成物;
[9]前記(E)がメントール、グリチルレチン酸、パルミチン酸レチノール及びシメン-5-オールからなる群より選択される1種以上である、[8]に記載の固形外用組成物;
[10](A)成分の総含有量1質量部に対して、(B)成分の総含有量が0.001~5質量部である、[1]から[9]に記載の固形外用組成物;
[11](A)成分の総含有量1質量部に対して、(C)成分の総含有量が0.005~2質量部である、[1]から[10]に記載の固形外用組成物;
[12](B)成分の総含有量1質量部に対して、(C)成分の総含有量が0.05~10質量部である、[1]から[11]に記載の固形外用組成物;
[13]25℃における硬度が5g以上である、[1]から[12]に記載の固形外用組成物;
[14]口唇用である、[1]から[13]に記載の固形外用組成物; 等を提供するものである。
That is, the present invention
[1] A solid composition for external use containing (A) a solid wax with a melting point of 40° C. or higher, (B) a water-soluble vitamin, and (C) a polyhydric alcohol, and having a water content of 2% by mass or less ;
[2] (D) The solid external composition according to [1], containing a glycerin fatty acid ester;
[3] (E) The solid external composition according to [1] or [2], containing a terpenoid;
[4] (F) The solid external composition according to [1] to [3], which contains a liquid oil;
[5] (G) The solid external composition according to [1] to [4], containing paste oil;
[6] The above (A) is one or more selected from the group consisting of paraffin wax, microcrystalline wax, polyethylene wax, Fischer-Tropsch wax, carnauba wax, and candelilla, and the above (B) is nicotinamide, thiamine hydrochloride. , thiamine phosphate, riboflavin, folic acid (pteroyl monoglutamic acid), pyridoxine hydrochloride, cyanocobalamin, biotin, pantothenic acid, ascorbic acid, ascorbyl glucoside, ascorbyl phosphate, ascorbyl magnesium phosphate, ethyl ascorbate, ascorbyl palmitate The solid external composition according to [1] to [5], containing one or more selected from the group consisting of phosphate, isostearyl ascorbyl phosphate, and caprylyl 2-glyceryl ascorbic acid;
[7] The solid external composition according to [2], wherein (D) is polyglyceryl diisostearate;
[8] The solid external composition according to [3], wherein (E) is a cyclic terpene;
[9] The solid external composition according to [8], wherein (E) is one or more selected from the group consisting of menthol, glycyrrhetinic acid, retinol palmitate, and cymen-5-ol;
[10] The solid external composition according to [1] to [9], wherein the total content of component (B) is 0.001 to 5 parts by mass relative to 1 part by mass of component (A). thing;
[11] The solid external composition according to [1] to [10], wherein the total content of component (C) is 0.005 to 2 parts by mass with respect to 1 part by mass of component (A). thing;
[12] The solid external composition according to [1] to [11], wherein the total content of component (C) is 0.05 to 10 parts by mass relative to 1 part by mass of component (B). thing;
[13] The solid external composition according to [1] to [12], which has a hardness of 5 g or more at 25°C;
[14] The solid external composition according to [1] to [13], which is for use on the lips.
本発明の固形外用組成物は、(A)融点が40℃以上である固形ワックス、(B)水溶性ビタミン、及び(C)多価アルコールを含有し、水の含有量が2質量%以下であるため、成形性、使用感に優れる。 The solid composition for external use of the present invention contains (A) a solid wax having a melting point of 40°C or higher, (B) a water-soluble vitamin, and (C) a polyhydric alcohol, and has a water content of 2% by mass or less. Therefore, it has excellent moldability and usability.
以下、本発明を実施するための形態について詳細に説明する。ただし、本発明は以下の実施形態に限定されるものではない。 EMBODIMENT OF THE INVENTION Hereinafter, the form for implementing this invention is demonstrated in detail. However, the present invention is not limited to the following embodiments.
〔1.固形外用組成物〕
本実施形態に係る固形外用組成物は、(A)融点が40℃以上である固形ワックスと、(B)水溶性ビタミンと、(C)多価アルコールを含有し、水の含有量が2質量%以下である。
[1. Solid external composition]
The solid composition for external use according to the present embodiment contains (A) a solid wax having a melting point of 40° C. or higher, (B) a water-soluble vitamin, and (C) a polyhydric alcohol, and has a water content of 2 mass % or less.
<(A)成分>
本発明に用いられる融点が40℃以上である固形ワックス(以下、単に(A)成分ともいう)とは、ろう状の物理的性質(具体的には、耐水性、可塑性、光沢性及び/又は不透明性等)を示し、融点が40℃以上であって、常温では固形のものをいい、医薬上、薬理学的に(製薬上)又は生理学的に許容されるものであれば、特に制限されない。本発明に用いる固形ワックスの融点は、40℃以上であれば、本発明の効果を奏し得る限り特に限定されないが、通常40~150℃程度、好ましくは40~130℃程度、より好ましくは40~100℃程度である。具体的には、パラフィンワックス、マイクロクリスタリンワックス等の石油由来のワックス;ポリエチレンワックス、フィッシャートロプシュワックス、硬化ヒマシ油、ポリプロピレンワックス等の合成ワックス;(ステアロキシメチコン/ジメチコン)コポリマー、セテアリルメチコン、アルキル(C30-45)セテアリルジメチコンクロスポリマー等のシリコーンワックス;カルナウバロウ、キャンデリラワックス、木ロウ、米糠ロウ、ハゼロウ、ウルシロウ、サトウキビロウ、パームロウ、オレンジ果皮ロウ、オレンジ花ロウ、オオバナソケイ花ロウ、クチベニスイセン花ロウ、シロヤマモモ果実ロウ、スイートアカシア花ロウ、チューベロース花ロウ等の植物由来のワックス;蜜蝋、サラシミツロウ、鯨蝋、セラック蝋、ラノリン等の動物由来のワックス;モンタンワックス、オゾケライト、セレシンワックス等の鉱物由来のワックス;セチルアルコール(セタノール、パルミチルアルコール等ともいう)、ステアリルアルコール、ベヘニルアルコール等の固形状の高級アルコール;等が挙げられるが、これらに限定されない。(A)成分の中でも本発明による効果をより一層顕著に奏する観点から、石油由来のワックス、植物由来のワックス、高級アルコールが好ましく、石油由来のワックス、植物由来のワックスがより好ましく、パラフィンワックス、マイクロクリスタリンワックスが更に好ましい。本発明の固形外用組成物では、上記(A)成分のうち、1種のみを単独で用いてもよいし、2種以上を組み合わせて用いてもよい。好ましくは、(A)成分を2種類以上組み合わせて用いることで、より一層高い本発明の効果が期待できる 。(A)成分は市販されているものを用いることができる。
<(A) component>
The solid wax used in the present invention with a melting point of 40°C or higher (hereinafter also simply referred to as component (A)) has waxy physical properties (specifically, water resistance, plasticity, gloss and/or It refers to a substance that exhibits opacity, etc.), has a melting point of 40°C or higher, is solid at room temperature, and is not particularly limited as long as it is medicinally, pharmacologically (pharmacologically) or physiologically acceptable. . The melting point of the solid wax used in the present invention is not particularly limited as long as it is 40°C or higher, as long as the effects of the present invention can be achieved, but it is usually about 40 to 150°C, preferably about 40 to 130°C, more preferably about 40 to 130°C. The temperature is about 100°C. Specifically, petroleum-derived waxes such as paraffin wax and microcrystalline wax; synthetic waxes such as polyethylene wax, Fischer-Tropsch wax, hydrogenated castor oil, and polypropylene wax; (stearoxymethicone/dimethicone) copolymer, cetearylmethicone, alkyl (C30-45) Silicone wax such as cetearyl dimethicone crosspolymer; carnauba wax, candelilla wax, wood wax, rice bran wax, hazel wax, sumac wax, sugar cane wax, palm wax, orange peel wax, orange flower wax, staghorn flower wax, cuticle wax Plant-derived waxes such as daffodil flower wax, white bayberry fruit wax, sweet acacia flower wax, and tuberose flower wax; Animal-derived waxes such as beeswax, beeswax, spermaceti, shellac wax, lanolin; Montan wax, ozokerite, ceresin wax solid higher alcohols such as cetyl alcohol (also referred to as cetanol, palmityl alcohol, etc.), stearyl alcohol, and behenyl alcohol; and the like, but are not limited to these. Among component (A), petroleum-derived waxes, plant-derived waxes, and higher alcohols are preferred, petroleum-derived waxes and plant-derived waxes are more preferred, and paraffin waxes, More preferred is microcrystalline wax. In the solid external composition of the present invention, only one type of the above-mentioned (A) components may be used alone, or two or more types may be used in combination. Preferably, by using two or more types of component (A) in combination, even higher effects of the present invention can be expected. As component (A), commercially available products can be used.
本実施形態に係る固形外用組成物における(A)成分の含有量は特に限定されず、(A)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(A)成分の含有量としては、本発明による効果をより顕著に奏する観点から、例えば、固形外用組成物の総量を基準として、(A)成分の総含有量が、0.1~60質量%であってもよく、0.5~50質量%であることが好ましく、1~46量%であることが更に好ましく、2~41量%であることがより好ましく、4~36質量%であることが更により好ましく、6~30質量%であることが特に好ましい。 The content of component (A) in the solid external composition according to the present embodiment is not particularly limited, and includes the type of component (A), the type and content of other ingredients, the use and formulation form of the solid external composition, etc. It is set as appropriate depending on the situation. The content of component (A) should be, for example, from 0.1 to 60% by mass based on the total amount of the solid topical composition, from the viewpoint of achieving more remarkable effects of the present invention. %, preferably from 0.5 to 50% by weight, more preferably from 1 to 46% by weight, more preferably from 2 to 41% by weight, and from 4 to 36% by weight. It is even more preferable that the amount be present, and particularly preferably 6 to 30% by weight.
<(B)成分>
本発明に用いられる水溶性ビタミン(以下、単に(B)成分ともいう)とは、水への溶解度が25℃において、3[g/100g水]以上のものをいい、医薬上、薬理学的に(製薬上)又は生理学的に許容されるものであれば、特に制限されない。本発明に用いる水溶性ビタミンの水への溶解度は、3[g/100g水]以上であれば、本発明の効果を奏し得る限り特に限定されないが、通常5~100[g/100g水]程度、好ましくは10~95[g/100g水]程度、より好ましくは20~90[g/100g水]程度である。具体的には、水溶性ビタミンB、水溶性ビタミンC等が挙げられる。水溶性ビタミンBは、チアミン塩酸塩、チアミンリン酸塩などのビタミンB1;リボフラビンなどのビタミンB2;ピリドキシン塩酸塩などのビタミンB6;シアノコバラミンなどのビタミンB12;ニコチン酸アミドなどのナイアシン;葉酸(プテロイルモノグルタミン酸);パントテン酸;ビオチン等が挙げられるが、これらに限定されない。水溶性ビタミンCは、アスコルビン酸、アスコルビルグルコシド、アスコルビルリン酸塩、リン酸アスコルビルマグネシウム、アスコルビン酸エチル、パルミチン酸アスコルビルリン酸塩、イソステアリルアスコルビルリン酸塩及びカプリリル2-グリセリルアスコルビン酸等が挙げられるが、これらに限定されない。(B)成分の中でも本発明による効果をより一層顕著に奏する観点から、ナイアシン、水溶性ビタミンCが好ましく、ニコチン酸アミドがより好ましい。本発明の固形外用組成物では、上記(B)成分のうち、1種のみを単独で用いてもよいし、2種以上を組み合わせて用いてもよい。好ましくは、(B)成分を2種類以上組み合わせて用いることで、より一層高い本発明の効果が期待できる 。(B)成分は市販されているものを用いることができる。
<(B) component>
The water-soluble vitamin used in the present invention (hereinafter also simply referred to as component (B)) has a solubility in water of 3 [g/100g water] or more at 25°C, and has a pharmaceutically and pharmacologically There are no particular limitations as long as it is (pharmaceutically) or physiologically acceptable. The solubility of the water-soluble vitamins used in the present invention in water is not particularly limited as long as it is 3 [g/100 g water] or more, as long as the effects of the present invention can be achieved, but it is usually about 5 to 100 [g/100 g water]. , preferably about 10 to 95 [g/100g water], more preferably about 20 to 90 [g/100g water]. Specific examples include water-soluble vitamin B, water-soluble vitamin C, and the like. Water-soluble vitamin B includes vitamin B1 such as thiamine hydrochloride and thiamine phosphate; vitamin B2 such as riboflavin; vitamin B6 such as pyridoxine hydrochloride; vitamin B12 such as cyanocobalamin; niacin such as nicotinamide; Examples include, but are not limited to, monoglutamic acid); pantothenic acid; biotin, and the like. Examples of water-soluble vitamin C include ascorbic acid, ascorbyl glucoside, ascorbyl phosphate, magnesium ascorbyl phosphate, ethyl ascorbate, ascorbyl palmitate phosphate, isostearyl ascorbyl phosphate, and caprylyl 2-glyceryl ascorbic acid. However, it is not limited to these. Among component (B), niacin and water-soluble vitamin C are preferred, and nicotinic acid amide is more preferred, from the viewpoint of achieving even more remarkable effects of the present invention. In the solid external composition of the present invention, one type of the above-mentioned component (B) may be used alone, or two or more types may be used in combination. Preferably, by using two or more types of component (B) in combination, even higher effects of the present invention can be expected. As component (B), commercially available products can be used.
本実施形態に係る固形外用組成物における(B)成分の含有量は特に限定されず、(B)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(B)成分の含有量としては、本発明による効果をより顕著に奏する観点から、例えば、固形外用組成物の総量を基準として、(B)成分の総含有量が、0.01~20質量%であることが好ましく、0.05~18質量%であることがより好ましく、0.1~16質量%であることが更に好ましく、0.15~14質量%であることが更により好ましく、0.2~12質量%であることが特に好ましい。 The content of component (B) in the solid external composition according to the present embodiment is not particularly limited, and includes the type of component (B), the type and content of other ingredients, the use and formulation form of the solid external composition, etc. It is set as appropriate depending on the situation. The content of component (B) should be, for example, from 0.01 to 20% by mass based on the total amount of the solid external composition, from the viewpoint of achieving more remarkable effects of the present invention. %, more preferably 0.05 to 18% by mass, even more preferably 0.1 to 16% by mass, even more preferably 0.15 to 14% by mass, Particularly preferred is 0.2 to 12% by weight.
<(C)成分>
本発明に用いられる多価アルコール(以下、単に(C)成分ともいう)とは、2価以上の多価アルコールのものをいい、医薬上、薬理学的に(製薬上)又は生理学的に許容されるものであれば、特に制限されない。本発明に用いる多価アルコールは、本発明の効果を奏し得る限り特に限定されないが、グリコール類、グリセリン類等が挙げられる。具体的には、グリコール類は、エチレングリコール、プロピレングリコール、1,3-ブチレングリコール、ペンチレングリコール、等のアルキレングリコール;ジエチレングリコール、ジプロピレングリコール等のジアルキレングリコール;トリプロピレングリコール、ヘキシレングリコール、カプリリルグリコール、ポリエチレングリコール、ポリプロピレングリコール等のポリアルキレングリコールが挙げられる。グリセリン類は、グリセリン、ジグリセリン、ポリグリセリン等が挙げられる。(C)成分の中でも本発明による効果をより一層顕著に奏する観点から、グリセリンが好ましい。本発明の固形外用組成物では、上記(C)成分のうち、1種のみを単独で用いてもよいし、2種以上を組み合わせて用いてもよい。好ましくは、(C)成分を2種類以上組み合わせて用いることで、より一層高い本発明の効果が期待できる 。(C)成分は市販されているものを用いることができる。
<(C) component>
The polyhydric alcohol used in the present invention (hereinafter also simply referred to as component (C)) refers to a polyhydric alcohol with a valence of 2 or more, which is medicinally, pharmacologically (pharmacologically) or physiologically acceptable. There is no particular restriction as long as it is carried out. The polyhydric alcohol used in the present invention is not particularly limited as long as it can achieve the effects of the present invention, and examples thereof include glycols, glycerin, and the like. Specifically, glycols include alkylene glycols such as ethylene glycol, propylene glycol, 1,3-butylene glycol, and pentylene glycol; dialkylene glycols such as diethylene glycol and dipropylene glycol; tripropylene glycol, hexylene glycol, Examples include polyalkylene glycols such as caprylyl glycol, polyethylene glycol, and polypropylene glycol. Examples of glycerin include glycerin, diglycerin, polyglycerin, and the like. Among component (C), glycerin is preferable from the viewpoint of exhibiting the effects of the present invention even more markedly. In the solid external composition of the present invention, only one type of the above-mentioned component (C) may be used alone, or two or more types may be used in combination. Preferably, by using two or more types of component (C) in combination, even higher effects of the present invention can be expected. As component (C), commercially available products can be used.
本実施形態に係る固形外用組成物における(C)成分の含有量は特に限定されず、(C)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(C)成分の含有量としては、本発明による効果をより顕著に奏する観点から、例えば、固形外用組成物の総量を基準として、(C)成分の総含有量が、0.001~10質量%であることが好ましく、0.005~8質量%であることがより好ましく、0.01~7質量%であることが更に好ましく、0.05~6質量%であることが更により好ましく、0.1~5質量%であることが特に好ましい。 The content of component (C) in the solid external composition according to the present embodiment is not particularly limited, and includes the type of component (C), the type and content of other ingredients, the use and formulation form of the solid external composition, etc. It is set as appropriate depending on the situation. The content of component (C) is, for example, from 0.001 to 10% by mass based on the total amount of the solid topical composition, from the viewpoint of achieving more remarkable effects of the present invention. %, more preferably 0.005 to 8% by mass, even more preferably 0.01 to 7% by mass, even more preferably 0.05 to 6% by mass, Particularly preferred is 0.1 to 5% by weight.
<(D)成分>
本実施形態に係る固形外用組成物は、更に(D)グリセリン脂肪酸エステル(単に「(D)成分」とも表記する。)を含有してもよい。本発明に用いるグリセリン脂肪酸エステルは、モノグリセリン脂肪酸エステル及びポリグリセリン脂肪酸エステルのいずれも含み、医薬上、薬理学的に(製薬上)又は生理学的に許容されるものであれば、特に制限されない。具体的には、モノグリセリン脂肪酸エステルは、モノカプリル酸グリセリル、モノカプリン酸グリセリル、モノラウリン酸グリセリル、モノミリスチン酸グリセリル、モノパルミチン酸グリセリル、モノステアリン酸グリセリル、モノイソステアリン酸グリセリル、モノベヘン酸グリセリル、モノオレイン酸グリセリル、モノエルカ酸グリセリル、セスキオレイン酸グリセリル、ジステアリン酸グリセリル、ジイソステアリン酸グリセリル、ジアラキン酸グリセリル等が挙げられる。ポリグリセリン脂肪酸エステルは、モノカプリル酸ジグリセリル、モノカプリル酸デカグリセリル、モノカプリン酸ヘキサグリセリル、モノラウリン酸テトラグリセリル、モノラウリン酸ヘキサグリセリル、モノラウリン酸デカグリセリル、モノラウリン酸ポリ(4~10)グリセリル、モノミリスチン酸デカグリセリル、モノステアリン酸デカグリセリル、モノイソステアリン酸デカグリセリル、モノステアリン酸ポリ(2~10)グリセリル、モノオレイン酸ジグリセリル、モノオレイン酸ヘキサグリセリル、セスキオレイン酸ジグリセリル、ジイソステアリン酸ポリ(2~10)グリセリル、ジステアリン酸ポリ(6~10)グリセリル、トリイソステアリン酸ジグリセリル、トリステアリン酸ポリ(10)グリセリルが挙げられる。(D)成分の中でも本発明による効果をより一層顕著に奏する観点から、ジイソステアリン酸ジグリセリルが好ましい。固形外用組成物が(D)成分を更に含有することで、本発明による効果がより顕著に奏される。本発明の固形外用組成物では、上記(D)成分のうち、1種のみを単独で用いてもよいし、2種以上を組み合わせて用いてもよい。好ましくは、(D)成分を2種類以上組み合わせて用いることで、より一層高い本発明の効果が期待できる 。(D)成分は市販されているものを用いることができる。
<(D) component>
The solid composition for external use according to the present embodiment may further contain (D) glycerin fatty acid ester (also simply referred to as "component (D)"). The glycerin fatty acid ester used in the present invention includes both monoglycerin fatty acid ester and polyglycerin fatty acid ester, and is not particularly limited as long as it is medicinally, pharmacologically (pharmacologically) or physiologically acceptable. Specifically, monoglycerin fatty acid esters include glyceryl monocaprylate, glyceryl monocaprate, glyceryl monolaurate, glyceryl monomyristate, glyceryl monopalmitate, glyceryl monostearate, glyceryl monoisostearate, glyceryl monobehenate, and monoglyceryl monostearate. Examples include glyceryl oleate, glyceryl monoerucate, glyceryl sesquioleate, glyceryl distearate, glyceryl diisostearate, glyceryl diarachate, and the like. Polyglycerin fatty acid esters include diglyceryl monocaprylate, decaglyceryl monocaprylate, hexaglyceryl monocaprate, tetraglyceryl monolaurate, hexaglyceryl monolaurate, decaglyceryl monolaurate, poly(4-10)glyceryl monolaurate, and monoglyceryl monolaurate. Decaglyceryl myristate, Decaglyceryl monostearate, Decaglyceryl monoisostearate, Poly(2-10)glyceryl monostearate, Diglyceryl monooleate, Hexaglyceryl monooleate, Diglyceryl sesquioleate, Poly(2-10) diisostearate. 2-10) glyceryl, poly(6-10) glyceryl distearate, diglyceryl triisostearate, and poly(10) glyceryl tristearate. Among component (D), diglyceryl diisostearate is preferable from the viewpoint of exhibiting the effects of the present invention more markedly. When the solid external composition further contains component (D), the effects of the present invention are more significantly exhibited. In the solid external composition of the present invention, one type of the above-mentioned component (D) may be used alone, or two or more types may be used in combination. Preferably, by using two or more types of component (D) in combination, even higher effects of the present invention can be expected. As component (D), commercially available products can be used.
本実施形態に係る固形外用組成物における(D)成分の含有量は特に限定されず、(D)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(D)成分の含有量としては、本発明による効果をより顕著に奏する観点から、例えば、固形外用組成物の総量を基準として、(D)成分の総含有量が、0.01~15質量%であることが好ましく、0.05~12質量%であることがより好ましく、0.05~9質量%であることが更に好ましく、0.05~7質量%であることが更により好ましく、0.1~5質量%であることが特に好ましい。 The content of component (D) in the solid external composition according to the present embodiment is not particularly limited, and includes the type of component (D), the type and content of other ingredients, the use and formulation form of the solid external composition, etc. It is set appropriately depending on the situation. The content of component (D) should be, for example, from 0.01 to 15% by mass based on the total amount of the solid external composition, from the viewpoint of achieving more remarkable effects of the present invention. %, more preferably 0.05 to 12% by mass, even more preferably 0.05 to 9% by mass, even more preferably 0.05 to 7% by mass, Particularly preferred is 0.1 to 5% by weight.
<(E)成分>
本実施形態に係る固形外用組成物は、更に(E)テルペノイド(単に「(E)成分」とも表記する。)を含有することで、本発明による効果がより顕著に奏される。本発明に用いるテルペノイドは、分子内に少なくとも1つの環構造を有するテルペノイドである環式テルペンと、分子内に環構造を有しないテルペノイドである非環式テルペンのいずれも含み、医薬上、薬理学的に(製薬上)又は生理学的に許容されるものであれば、特に制限されない。具体的には、メントール、メントン、カンフル、カルボン、ボルネオール、シネオール、アネトール、オイゲノール、テルピネオール、カルバクロール、リモネン、ピネン、シンナミルアルデヒド、チモール、シメン-5-オール、グリチルレチン酸、レチノール、グリチルリチン酸、及びこれらの誘導体等の環式テルペン;ゲラニオール、シトロネロール、リナロール、酢酸リナリル、ネロール、シトラール及びこれらの誘導体等の非環式テルペン等が挙げられるが、これらに限定されない。(E)成分の中でも本発明による効果をより一層顕著に奏する観点から、環式テルペンが好ましく、メントール、シメン-5-オール、グリチルレチン酸、レチノール、及びこれらの誘導体がより好ましい。
<(E) component>
The solid composition for external use according to the present embodiment further exhibits the effects of the present invention by further containing (E) terpenoid (also simply referred to as "component (E)"). The terpenoids used in the present invention include both cyclic terpenes, which are terpenoids that have at least one ring structure in their molecules, and acyclic terpenes, which are terpenoids that do not have a ring structure in their molecules. There are no particular limitations as long as it is pharmaceutically (pharmaceutically) or physiologically acceptable. Specifically, menthol, menthone, camphor, carvone, borneol, cineole, anethole, eugenol, terpineol, carvacrol, limonene, pinene, cinnamyl aldehyde, thymol, cymen-5-ol, glycyrrhetinic acid, retinol, glycyrrhetinic acid, and cyclic terpenes such as derivatives thereof; acyclic terpenes such as geraniol, citronellol, linalool, linalyl acetate, nerol, citral, and derivatives thereof, and the like, but are not limited to these. Among component (E), cyclic terpenes are preferable, and menthol, cymen-5-ol, glycyrrhetinic acid, retinol, and derivatives thereof are more preferable, from the viewpoint of more significantly exerting the effects of the present invention.
テルペノイドはd体、l体及びdl体のいずれでもよく、l-メントール、d-メントール、dl-メントールが例示される。ただし、ゲラニオール等のようにテルペノイドによっては光学異性体が存在しない場合もある。(E)成分は市販されているものを用いることができる。(E)成分は1種を単独で使用してもよく、又は2種以上を組み合わせて使用してもよい。、何れの部位を用いてもよいが Terpenoids may be d-, l-, or dl-menthol, and examples thereof include l-menthol, d-menthol, and dl-menthol. However, some terpenoids, such as geraniol, do not have optical isomers. As component (E), commercially available products can be used. Component (E) may be used alone or in combination of two or more. , any part may be used.
本実施形態に係る固形外用組成物における(E)成分の含有量は特に限定されず、(E)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(E)成分の含有量としては、本発明による効果をより顕著に奏する観点から、例えば、固形外用組成物の総量を基準として、(E)成分の総含有量が、0.001~5質量%であることが好ましく、0.005~4質量%であることがより好ましく、0.01~3質量%であることが更に好ましく、0.05~2質量%であることが更により好ましく、0.1~1質量%であることが特に好ましい。 The content of component (E) in the solid external composition according to the present embodiment is not particularly limited, and includes the type of component (E), the type and content of other ingredients, the use and formulation form of the solid external composition, etc. It is set as appropriate depending on the situation. The content of component (E) should be, for example, from 0.001 to 5% by weight based on the total amount of the solid topical composition, from the viewpoint of exhibiting the effects of the present invention more markedly. %, more preferably 0.005 to 4% by mass, even more preferably 0.01 to 3% by mass, even more preferably 0.05 to 2% by mass, Particularly preferred is 0.1 to 1% by weight.
<(F)成分>
本実施形態に係る固形外用組成物は、更に(F)液状油(単に「(F)成分」とも表記する。)を含有することで、本発明による効果がより顕著に奏される。本発明に用いる液状油は、室温で流動性のあるものを示し、油溶性紫外線吸収剤、トコフェロール、のいずれも含み、医薬上、薬理学的に(製薬上)又は生理学的に許容されるものであれば、特に制限されない。具体的には、パラメトキシケイ皮酸2-エチルヘキシル、ジメチコジエチルベンザルマロネート、オクトクリレン及びサリチル酸オクチルからなる群より選択される1種以上の油溶性紫外線吸収剤;パラフィン、イソパラフィン、スクワランなどの炭化水素油;ホホバ油、オリーブ油、マカデミアナッツ油、アボカド油、ヤシ油、コーン油、大豆油、菜種油、ヒマワリ油などの植物油;ラノリンなどの動物油;オクチルドデカノール、イソステアリルアルコールなどの高級アルコール類;マカデミアナッツ脂肪酸フィトステリル、リンゴ酸ジイソステアリル、トリ(カプリル酸/カプリン酸)グリセリル、エチルヘキサン酸セチル、水添ロジン酸ペンタエリスチル等のエステル油等が挙げられる。(F)成分の中でも本発明による効果をより一層顕著に奏する観点から、パラメトキシケイ皮酸2-エチルヘキシル、パラフィン、スクワラン、オリーブ油、リンゴ酸ジイソステアリルが好ましい。固形外用組成物が(F)成分を更に含有することで、本発明による効果がより顕著に奏される。本発明の固形外用組成物では、上記(F)成分のうち、1種のみを単独で用いてもよいし、2種以上を組み合わせて用いてもよい。好ましくは、(F)成分を2種類以上組み合わせて用いることで、より一層高い本発明の効果が期待できる 。(F)成分は市販されているものを用いることができる。
<(F) component>
When the solid composition for external use according to the present embodiment further contains (F) liquid oil (also simply referred to as "component (F)"), the effects of the present invention are more prominently exhibited. The liquid oil used in the present invention is fluid at room temperature, contains oil-soluble ultraviolet absorbers and tocopherol, and is pharmaceutically, pharmacologically (pharmacologically) or physiologically acceptable. If so, there are no particular restrictions. Specifically, one or more oil-soluble UV absorbers selected from the group consisting of para-methoxycinnamate 2-ethylhexyl, dimethicodiethyl benzalmalonate, octocrylene, and octyl salicylate; paraffin, isoparaffin, squalane, etc. Hydrocarbon oils; vegetable oils such as jojoba oil, olive oil, macadamia nut oil, avocado oil, coconut oil, corn oil, soybean oil, rapeseed oil, and sunflower oil; animal oils such as lanolin; higher alcohols such as octyldodecanol and isostearyl alcohol; Examples include ester oils such as macadamia nut fatty acid phytosteryl, diisostearyl malate, tri(caprylic/capric) glyceryl, cetyl ethylhexanoate, and hydrogenated pentaerythyl rosinate. Among component (F), 2-ethylhexyl paramethoxycinnamate, paraffin, squalane, olive oil, and diisostearyl malate are preferable from the viewpoint of more significantly exerting the effects of the present invention. When the solid composition for external use further contains component (F), the effects of the present invention are more prominently exhibited. In the solid external composition of the present invention, only one type of the above-mentioned (F) components may be used alone, or two or more types may be used in combination. Preferably, by using two or more types of component (F) in combination, even higher effects of the present invention can be expected. As component (F), commercially available products can be used.
本実施形態に係る固形外用組成物における(F)成分の含有量は特に限定されず、(F)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(F)成分の含有量としては、本発明による効果をより顕著に奏する観点から、例えば、固形外用組成物の総量を基準として、(F)成分の総含有量が、1~60質量%であることが好ましく、3~60質量%であることがより好ましく、5~60質量%であることが更に好ましく、5~50質量%であることが更により好ましく、7~45質量%であることが特に好ましい。 The content of component (F) in the solid external composition according to the present embodiment is not particularly limited, and includes the type of component (F), the type and content of other ingredients, the use and formulation form of the solid external composition, etc. It is set as appropriate depending on the situation. The content of component (F) is, for example, from 1 to 60% by mass, based on the total amount of the solid topical composition, from the viewpoint of achieving more remarkable effects of the present invention. It is preferably from 3 to 60% by mass, even more preferably from 5 to 60% by mass, even more preferably from 5 to 50% by mass, and from 7 to 45% by mass. is particularly preferred.
<(G)成分>
本実施形態に係る固形外用組成物は、更に(G)ペースト油(単に「(G)成分」とも表記する。)を含有することで、本発明による効果がより顕著に奏される。本発明に用いるペースト油は、室温で流動性がないものを示し、石油由来、鉱物由来、植物由来、動物由来等、医薬上、薬理学的に(製薬上)又は生理学的に許容されるものであれば、特に制限されない。具体的には、ワセリン、イソパラフィンなどの炭化水素類、シアバター、ココアバター、アボカドバター、アロエバター等の植物由来、ラノリン、ラウロイルグルタミン酸ジ(フィトステリル・オクチルドデシル)、ダイマージリノール酸ダイマージリノレイル、(イソステアリン酸ポリグリセリル-2/ダイマージリノール酸)コポリマー、ヘキサ(ヒドロキシステアリン酸/ステアリン酸/ステアリン酸/ロジン酸)ジペンタエリスリチル、アジピン酸ジグリセリル混合脂肪酸エステル、脂肪酸(C10―30)(コレステロール/ラノステロール)エステルズ等のエステル類等が挙げられる。(G)成分の中でも本発明による効果をより一層顕著に奏する観点から、ワセリン、イソパラフィン、シアバター、ラノリンが好ましい。固形外用組成物が(G)成分を更に含有することで、本発明による効果がより顕著に奏される。本発明の固形外用組成物では、上記(G)成分のうち、1種のみを単独で用いてもよいし、2種以上を組み合わせて用いてもよい。好ましくは、(G)成分を2種類以上組み合わせて用いることで、より一層高い本発明の効果が期待できる 。(G)成分は市販されているものを用いることができる。
<(G) component>
The solid composition for external use according to the present embodiment further exhibits the effects of the present invention by further containing (G) paste oil (also simply referred to as "component (G)"). The paste oil used in the present invention has no fluidity at room temperature, and is medicinally, pharmacologically (pharmacologically) or physiologically derived, such as petroleum-derived, mineral-derived, plant-derived, or animal-derived. If so, there are no particular restrictions. Specifically, hydrocarbons such as petrolatum and isoparaffin, plant-derived products such as shea butter, cocoa butter, avocado butter, and aloe butter, lanolin, di(phytosteryl octyldodecyl) lauroylglutamate, and dimer dilinoleyl dilinoleate. , (polyglyceryl-2 isostearate/dimer dilinoleic acid) copolymer, hexa(hydroxystearic acid/stearic acid/stearic acid/rosin acid) dipentaerythrityl, diglyceryl adipate mixed fatty acid ester, fatty acid (C10-30) (cholesterol/lanosterol) ) esters such as esters. Among component (G), vaseline, isoparaffin, shea butter, and lanolin are preferred from the viewpoint of achieving even more remarkable effects of the present invention. When the solid external composition further contains component (G), the effects of the present invention are more significantly exhibited. In the solid external composition of the present invention, one type of the above-mentioned (G) components may be used alone, or two or more types may be used in combination. Preferably, by using two or more types of component (G) in combination, even higher effects of the present invention can be expected. As component (G), commercially available products can be used.
本実施形態に係る固形外用組成物における(G)成分の含有量は特に限定されず、(G)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(G)成分の含有量としては、本発明による効果をより顕著に奏する観点から、例えば、固形外用組成物の総量を基準として、(G)成分の総含有量が、5~70質量%であることが好ましく、8~65質量%であることがより好ましく、10~60質量%であることが更に好ましく、12~55質量%であることが更により好ましく、20~50質量%であることが特に好ましい。 The content of component (G) in the solid external composition according to the present embodiment is not particularly limited, and includes the type of component (G), the type and content of other ingredients, the use and formulation form of the solid external composition, etc. It is set as appropriate depending on the situation. The content of component (G) is, for example, from 5 to 70% by mass based on the total amount of the solid topical composition, from the viewpoint of achieving more remarkable effects of the present invention. It is preferably from 8 to 65% by mass, even more preferably from 10 to 60% by mass, even more preferably from 12 to 55% by mass, and even more preferably from 20 to 50% by mass. is particularly preferred.
本実施形態に係る固形外用組成物の25℃における硬度は、成形性の観点から、5g以上が好ましく、7g以上がより好ましく、10g以上が更に好ましく、12g以上が更により好ましく、17g以上がより一層好ましく、20g以上が特に好ましい。固形外用組成物の25℃における硬度は、使用感の観点から、60g以下が好ましく、50g以下がより好ましく、45g以下が更に好ましく、38g以下が更により好ましく、35g以下がより一層好ましく、33g以下が特に好ましい。、固形外用組成物の25℃における硬度は、90℃以上にて加熱溶融した化粧料本体をリップスティック用容器(直径約12mm、高さ約40mm)に充填した後、4℃で2時間冷却固化し、25℃で一晩静置し冷、25℃で4時間以上静置した後、上端から約10mmを切り取り、でレオテック社製レオメーターを用いて、直径φ1mmの冶具にてtable speedが2mm/sの速さで冶具を深さ10mmまで針入させたときの最大値を読み取ることによって測定できる。 The hardness at 25°C of the solid composition for external use according to the present embodiment is preferably 5 g or more, more preferably 7 g or more, even more preferably 10 g or more, even more preferably 12 g or more, and even more preferably 17 g or more, from the viewpoint of moldability. More preferably, 20 g or more is particularly preferable. The hardness at 25° C. of the solid external composition is preferably 60 g or less, more preferably 50 g or less, even more preferably 45 g or less, even more preferably 38 g or less, even more preferably 35 g or less, and even more preferably 33 g or less. is particularly preferred. The hardness of the solid topical composition at 25°C is determined by heating and melting the cosmetic main body at 90°C or higher, filling it into a lipstick container (approximately 12 mm in diameter, and approx. 40 mm in height), and then cooling and solidifying it at 4°C for 2 hours. Then, leave it at 25℃ overnight to cool. After leaving it at 25℃ for more than 4 hours, cut off about 10mm from the top, and use a rheometer manufactured by Rheotec to obtain a table speed of 2mm using a jig with a diameter of 1mm. It can be measured by reading the maximum value when the jig is inserted to a depth of 10 mm at a speed of /s.
本実施形態に係る固形外用組成物に用いられる水はイオン交換水や蒸留水等を用いることができる。水の含有量としては、本発明による効果をより顕著に奏する観点から、例えば、固形外用組成物の総量を基準として、水の総含有量が、2質量%以下であることが好ましく、1.5質量%以下であることがより好ましく、1.2質量%以下であることが更に好ましく、1%以下であることがより好ましく、0.8質量%以下であることが更により好ましく、0.6質量%以下であることが特に好ましく、0.4質量%以下であることが特に好ましく、0.2質量%以下であることが特に好ましく、実質的に0質量%であることが最も好ましい。2質量%を超えると、成形性が好ましくない場合がある。 The water used in the solid external composition according to the present embodiment can be ion-exchanged water, distilled water, or the like. As for the water content, from the viewpoint of achieving more remarkable effects of the present invention, for example, the total water content is preferably 2% by mass or less based on the total amount of the solid external composition, and 1. It is more preferably 5% by mass or less, even more preferably 1.2% by mass or less, even more preferably 1% or less, even more preferably 0.8% by mass or less, and even more preferably 0.8% by mass or less. It is particularly preferably 6% by mass or less, particularly preferably 0.4% by mass or less, particularly preferably 0.2% by mass or less, and most preferably substantially 0% by mass. If it exceeds 2% by mass, moldability may be unfavorable.
本実施形態に係る固形外用組成物における、(A)成分に対する(B)成分の含有比率は特に限定されず、(A)成分及び(B)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(A)成分に対する(B)成分の含有比率としては、本発明による効果をより顕著に奏する観点から、例えば、本実施形態に係る水中油型化粧料に含まれる(A)成分の総含有量1質量部に対して、(B)成分の総含有量が、0.001~5質量部であることが好ましく、0.001~3質量部であることがより好ましく、0.005~2質量部であることが更に好ましく、0.005~1質量部であることが特に好ましい。(A)成分に対する(B)成分の含有比率が小さいと使用感が悪くなり、(A)成分に対する(B)成分の含有比率が大きいと成形性が悪くなる。 In the solid external composition according to the present embodiment, the content ratio of component (B) to component (A) is not particularly limited, and the types of component (A) and (B), and the types and contents of other ingredients , is appropriately set depending on the use and formulation form of the solid external composition. The content ratio of component (B) to component (A) is, for example, the total content of component (A) contained in the oil-in-water cosmetic according to the present embodiment, from the viewpoint of achieving more remarkable effects of the present invention. The total content of component (B) per 1 part by mass is preferably 0.001 to 5 parts by mass, more preferably 0.001 to 3 parts by mass, and 0.005 to 2 parts by mass. 1 part by weight is more preferable, and 0.005 to 1 part by weight is particularly preferable. If the content ratio of component (B) to component (A) is small, the usability will be poor, and if the content ratio of component (B) to component (A) is large, moldability will be poor.
本実施形態に係る固形外用組成物における、(A)成分に対する(C)成分の含有比率は特に限定されず、(A)成分及び(C)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(A)成分に対する(C)成分の含有比率としては、本発明による効果をより顕著に奏する観点から、例えば、本実施形態に係る水中油型化粧料に含まれる(A)成分の総含有量1質量部に対して、(C)成分の総含有量が、0.005~2質量部であることが好ましく、0.01~1質量部であることがより好ましく、0.02~0.8質量部であることが更に好ましく、0.025~0.6質量部であることが更により好ましく、0.05~0.5質量部であることが特に好ましい。(A)成分に対する(C)成分の含有比率が小さいと使用感が悪くなり、(A)成分に対する(C)成分の含有比率が大きいと成形性が悪くなる。
In the solid external composition according to the present embodiment, the content ratio of component (C) to component (A) is not particularly limited, and the types of component (A) and (C), and the types and contents of other ingredients. , is appropriately set depending on the use and formulation form of the solid external composition. The content ratio of component (C) to component (A) is, for example, the total content of component (A) contained in the oil-in-water cosmetic according to the present embodiment, from the viewpoint of achieving more remarkable effects of the present invention. The total content of component (C) per 1 part by mass is preferably 0.005 to 2 parts by mass, more preferably 0.01 to 1 part by mass, and 0.02 to 0. It is more preferably 8 parts by weight, even more preferably 0.025 to 0.6 parts by weight, and particularly preferably 0.05 to 0.5 parts by weight. If the content ratio of component (C) to component (A) is small, the usability will be poor, and if the content ratio of component (C) to component (A) is large, moldability will be poor.
本実施形態に係る固形外用組成物における、(B)成分に対する(C)成分の含有比率は特に限定されず、(B)成分及び(C)成分の種類、他の配合成分の種類及び含有量、固形外用組成物の用途及び製剤形態等に応じて適宜設定される。(B)成分に対する(C)成分の含有比率としては、本発明による効果をより顕著に奏する観点から、例えば、本実施形態に係る水中油型化粧料に含まれる(B)成分の総含有量1質量部に対して、(C)成分の総含有量が、0.05~10質量部であることが好ましく、0.1~8質量部であることがより好ましく、0.2~7質量部であることが更に好ましく、0.3~6質量部であることが更により好ましく、1~5質量部であることが特に好ましい。(B)成分に対する(C)成分の含有比率が小さいと(C)成分の溶解や分散が不十分になり、(B)成分に対する(C)成分の含有比率が大きいと使用感が悪くなる。 In the solid external composition according to the present embodiment, the content ratio of component (C) to component (B) is not particularly limited, and the types of component (B) and (C), and the types and contents of other ingredients , is appropriately set depending on the use and formulation form of the solid external composition. The content ratio of component (C) to component (B) is, for example, the total content of component (B) contained in the oil-in-water cosmetic according to the present embodiment, from the viewpoint of achieving more remarkable effects of the present invention. The total content of component (C) is preferably 0.05 to 10 parts by weight, more preferably 0.1 to 8 parts by weight, and 0.2 to 7 parts by weight per 1 part by weight. parts by weight, even more preferably from 0.3 to 6 parts by weight, and particularly preferably from 1 to 5 parts by weight. If the content ratio of component (C) to component (B) is small, the dissolution and dispersion of component (C) will be insufficient, and if the content ratio of component (C) to component (B) is large, the usability will be poor.
本実施形態に係る固形外用組成物は、本発明の効果を妨げない限り、化粧品や医薬部外品や医薬品に使用される公知の成分を含むことができる。上記(A)~(G)成分の他に、例えば、抗酸化剤、美白成分、保湿剤、抗炎症成分、抗菌剤、ビタミン類、アミノ酸類、生物由来抽出物、種々の薬理活性成分や生理活性成分を組み合わせて適当量含有してもよい(但し前記(A)~(G)成分を除く)。また、添加剤、たとえば、界面活性剤、保存剤、pH調整剤、キレート剤、安定化剤、緩衝剤、増粘剤、ゲル化剤、刺激軽減剤、防腐剤、着色剤、香料、ミネラルなどから1種を単独で、または2種以上を組み合わせて添加することができる(但し前記(A)~(G)成分を除く)。また、基剤または担体を1種単独で、または2種以上を含むことができる。これらは公知のものを適宜選択して使用でき、常法を用いて製造することができる。市販されているものを用いることもできる。 The solid composition for external use according to the present embodiment can contain known ingredients used in cosmetics, quasi-drugs, and pharmaceuticals, as long as they do not impede the effects of the present invention. In addition to the above ingredients (A) to (G), for example, antioxidants, whitening ingredients, moisturizers, anti-inflammatory ingredients, antibacterial agents, vitamins, amino acids, biological extracts, various pharmacologically active ingredients, and physiological ingredients. It may contain a suitable amount of a combination of active ingredients (excluding components (A) to (G) above). Additionally, additives such as surfactants, preservatives, pH adjusters, chelating agents, stabilizers, buffers, thickeners, gelling agents, irritation reducers, preservatives, colorants, fragrances, minerals, etc. One kind can be added alone or two or more kinds can be added in combination (excluding the above-mentioned components (A) to (G)). Moreover, one type of base or carrier can be used alone, or two or more types can be included. These can be used by appropriately selecting known ones, and can be manufactured using conventional methods. Commercially available ones can also be used.
本実施形態に係る固形外用組成物は、適用部位に塗布することが可能な形状であれば特に限定されず、円柱状、楕円柱状、三角柱状、四角柱状、多角柱状、変形柱状(花びら型、動物型など)、ドーム型状などの容器に充填されてなる形状を有する。 The solid external composition according to the present embodiment is not particularly limited as long as it has a shape that can be applied to the application site, and can be cylindrical, elliptical, triangular, square, polygonal, modified cylindrical (petal-shaped, (animal-shaped, etc.), or filled in a dome-shaped container.
本実施形態に係る固形外用組成物を充填する容器の内径(直径)は、本発明による効果をより顕著に奏する観点から、3~60mmであることが好ましく、4~55mmであることがより好ましく、5~50mmであることが更に好ましく、6~45mmであることが特に好ましい。内径は、容器に充填した固形外用組成物を容器収容部外へ出した場合に、塗布部と接触する部分の平面の形状において、重心を通る最も短い直線の長さである。容器に充填した固形外用組成物が円柱状の場合は円の直径であり、正四角柱の場合は正方形の一辺の長さである。 The inner diameter (diameter) of the container filled with the solid external composition according to the present embodiment is preferably 3 to 60 mm, more preferably 4 to 55 mm, from the viewpoint of achieving more remarkable effects of the present invention. , more preferably 5 to 50 mm, particularly preferably 6 to 45 mm. The inner diameter is the length of the shortest straight line passing through the center of gravity in the shape of the plane of the part that comes into contact with the application part when the solid external composition filled in the container is taken out of the container accommodating part. When the solid external composition filled in the container is cylindrical, it is the diameter of the circle, and when it is a regular square prism, it is the length of one side of the square.
本実施形態に係る固形外用組成物を充填する容器における、内径(直径)に対する収容部の深さは、本発明による効果をより顕著に奏する観点から、0.3~20であることが好ましく、0.8~12であることがより好ましく、1.2~9であることが更に好ましく、1.4~6であることがより更に好ましく、1.6~3であることが特に好ましい。収容部の深さは、収容部の底面が平面状ではなく傾斜等を有する場合は、深さ方向に最も長い距離のことをいう。 In the container to be filled with the solid external composition according to the present embodiment, the depth of the accommodating portion relative to the inner diameter (diameter) is preferably 0.3 to 20, from the viewpoint of more prominently achieving the effects of the present invention. It is more preferably from 0.8 to 12, even more preferably from 1.2 to 9, even more preferably from 1.4 to 6, and particularly preferably from 1.6 to 3. In the case where the bottom surface of the housing part is not flat but sloped, the depth of the housing part refers to the longest distance in the depth direction.
本実施形態に係る固形外用組成物は、皮膚に適用することができる。皮膚とは体(例えば、顔、頭、耳、首、胸、脇、腹、腰、背中、尻、腕、脚、手、指、デリケートゾーン(陰部)等)の表面だけでなく、粘膜も包含する概念である。 The solid external composition according to this embodiment can be applied to the skin. Skin is not only the surface of the body (e.g., face, head, ears, neck, chest, armpits, abdomen, waist, back, buttocks, arms, legs, hands, fingers, sensitive areas (genital areas), etc.), but also the mucous membranes. It is an inclusive concept.
本実施形態に係る固形外用組成物は、薬剤の形態は特に限定されず、化粧品や医薬部外品や医薬品の形態として公知の形態を採ることができる。このような公知の形態の中でも、たとえば、クリーム剤、ゲル剤、リニメント剤、軟膏剤、パップ剤、リップスティックのようなスティック剤などをあげることができる。また、乳液、クリーム、ボディローション、ボディークリーム、日焼け止めのような基礎化粧品の形態や、ファンデーション、口紅、ほお紅、アイメイク、おしろい、マニキュア、ペディキュア等のメークアップ化粧料の形態でも用いられ得る。好ましくは口唇用リップスティック、スティック状制汗剤、スティック状日焼け止めである。 本実施形態に係る固形外用組成物は、各成分を常法に従って、たとえば、混合撹拌することにより調製できる。 The solid external composition according to the present embodiment is not particularly limited in the form of a drug, and may take any known form as a cosmetic, a quasi-drug, or a pharmaceutical. Among such known forms, examples include creams, gels, liniments, ointments, poultices, and sticks such as lipsticks. It can also be used in the form of basic cosmetics such as emulsions, creams, body lotions, body creams, and sunscreens, and in the form of makeup cosmetics such as foundations, lipsticks, blushers, eye makeup, face powder, manicures, and pedicures. Preferred are lipsticks, stick antiperspirants, and stick sunscreens. The solid composition for external use according to the present embodiment can be prepared by mixing and stirring each component according to a conventional method.
以下、試験例に基づいて本発明を具体的に説明するが、本発明はこれらに限定されるものではない。また、以下の実施例等における配合量は質量%を示す。 The present invention will be specifically explained below based on test examples, but the present invention is not limited thereto. Moreover, the compounding amounts in the following examples and the like indicate mass %.
[試験例1]
下記の表1、2に示す組成を有する固形外用組成物を常法に従って調製し、繰り出し式リップスティック容器(ポリプロピレン製)に充填した。容器内で固形外用組成物は直径12mm、長さ40mmの円柱形状である。保形性、はがれ現象、発汗、使用感を以下の評価基準で評価し、結果を表1、2に示した。
[Test Example 1]
A solid composition for external use having the composition shown in Tables 1 and 2 below was prepared according to a conventional method and filled into a retractable lipstick container (made of polypropylene). Inside the container, the solid external composition has a cylindrical shape with a diameter of 12 mm and a length of 40 mm. Shape retention, peeling phenomenon, sweating, and feeling of use were evaluated using the following evaluation criteria, and the results are shown in Tables 1 and 2.
(保形性の評価基準)
固形外用組成物の長さが30mmとなるようにリップスティック容器の外に繰り出し、水平方向に45度傾けて5秒間静止した後の固形外用組成物の保形性を観察した。
〇:固形外用組成物は水平方向に45度傾いた形状のまま保持される
△:固形外用組成物は水平方向に45度より少し傾き、形状はわずかに曲がる
×:固形外用組成物は水平方向に45度より大きく傾き、形状は曲がる
(Evaluation criteria for shape retention)
The solid composition for external use was drawn out of the lipstick container so that the length of the solid composition for external use was 30 mm, and the shape retention of the solid composition for external use was observed after it was tilted horizontally at 45 degrees and left at rest for 5 seconds.
〇: The solid topical composition is held in a shape tilted at 45 degrees in the horizontal direction △: The solid topical composition is tilted a little more than 45 degrees in the horizontal direction, and the shape is slightly bent ×: The solid topical composition is kept in the horizontal direction tilts more than 45 degrees and the shape bends
(はがれ現象の評価基準)
リップスティック容器に充填した固形外用組成物8個について、容器の外に長さが30mmとなるように繰り出し、固形外用組成物の側面を目視で観察し、はがれ現象の有無を評価した。固形外用組成物の側面の表面において、薄い剥がれ又は欠けを観察した場合に、はがれ現象があると評価した。
◎:8個全て、はがれ現象が無い
〇:8個中1~2個にはがれ現象がある
△:8個中3~5固個にはがれ現象がある
×:8個中6~8個にはがれ現象がある
(Evaluation criteria for peeling phenomenon)
Eight solid external compositions filled in lipstick containers were drawn out of the container to a length of 30 mm, and the sides of the solid external compositions were visually observed to evaluate the presence or absence of peeling phenomenon. When thin peeling or chipping was observed on the side surface of the solid external composition, it was evaluated that there was a peeling phenomenon.
◎: All 8 pieces have no peeling phenomenon ○: 1 to 2 out of 8 pieces have peeling phenomenon △: 3 to 5 out of 8 pieces have peeling phenomenon ×: 6 to 8 out of 8 pieces have peeling phenomenon There is a phenomenon
(発汗の評価基準)
固形外用組成物の長さが30mmとなるようにリップスティック容器の外に繰り出し、固形外用組成物の側面を目視で観察し、液状の滴の有無を評価した。
〇:液状の滴は無い
×:液状の滴がある
(Evaluation criteria for sweating)
The solid external composition was drawn out of the lipstick container to a length of 30 mm, and the side surface of the solid external composition was visually observed to evaluate the presence or absence of liquid droplets.
〇: There are no liquid droplets ×: There are liquid droplets
(使用感の評価基準)
5名の被験者がリップスティック容器に充填した固形外用組成物を2日間、唇に塗布して使用し、唇の皮むけ状態の改善程度により0点から5点の間で評価点を付けた。皮むけの状態に変化はない場合に0点とし、皮むけの状態が改善して皮むけが無くなった場合に5点とした。5名の被験者の評価点の平均点を算出し、下記の基準で評価した。被験者は、口と鼻を覆う不織布マスクを日常的に着用することにより、唇の荒れや皮むけが起こりやすくなったと感じる人を選定した。
◎:3.5点以上
〇:2.0点以上、3.5点未満
△:0点以上、2.0点未満
(Evaluation criteria for usability)
Five subjects used the solid external composition filled in a lipstick container and applied it to their lips for two days, and gave an evaluation score between 0 and 5 depending on the degree of improvement in the peeling condition of the lips. A score of 0 was given when there was no change in the state of peeling, and a score of 5 was given when the state of peeling improved and the peeling disappeared. The average score of the five test subjects was calculated and evaluated based on the following criteria. The subjects were those who felt that their lips were more likely to get chapped or peeled by wearing a non-woven fabric mask that covered their mouth and nose on a daily basis.
◎: 3.5 points or more ○: 2.0 points or more, less than 3.5 points △: 0 points or more, less than 2.0 points
[試験例2]
試験例1で使用した固形外用組成物について、25℃における硬度を測定した。90℃以上で加熱溶融した固形外用組成物をリップスティック容器(直径12mm、高さ40mm)に天面まで充填した後、4℃で2時間冷却固化させ、25℃で一晩静置した後、25℃に4時間以上放置したのちに、天面から11mmを切り取った。レオテック社製レオメーターを用いて、直径φ1mmの冶具をtable speedが2mm/sの速度で深さ10mmまで針入させたときの硬度の最大値を読み取った。各組成物について3回測定を行い、平均値を表1、2に示した。
[Test Example 2]
The hardness of the solid external composition used in Test Example 1 at 25°C was measured. After filling a lipstick container (diameter 12 mm, height 40 mm) up to the top with a solid external composition heated and melted at 90 ° C. or higher, it was cooled and solidified at 4 ° C. for 2 hours, and left to stand at 25 ° C. overnight. After leaving it at 25° C. for 4 hours or more, 11 mm was cut off from the top surface. Using a rheometer manufactured by Rheotech, the maximum value of hardness was read when a jig with a diameter of 1 mm was inserted to a depth of 10 mm at a table speed of 2 mm/s. Each composition was measured three times, and the average values are shown in Tables 1 and 2.
表1に示すとおり、融点が40℃以上である固形ワックス、水溶性ビタミン、多価アルコールを含有する固形外用組成物は、保形性が良く、はがれ現象および発汗が生じず、成形性が良好であった(実施例1)。融点が40℃以上である固形ワックス、水溶性ビタミンを含有し、多価アルコールを含有しない固形外用組成物は、保形性はあるが、わずかに曲がった部分にひび状の割れを観察し、はがれ現象が生じ、成形性は不良だった(比較例1)。さらに、使用感では唇に塗布する時にザラザラとした刺激があり、皮むけの状態に好ましくないと被験者は評価した(比較例1)。融点が40℃以上である固形ワックス、水溶性ビタミン、多価アルコールを含有し、水を2.1質量%含有する固形外用組成物は、保形性が非常に悪く成形性が不良のため、硬度、はがれ、発汗、使用感は評価できなかった(比較例2)。比較例1及び比較例2は製剤における不均一性によるものである可能性が考えられた。
融点が40℃以上である固形ワックス、水溶性ビタミン、多価アルコールを含有し、更にグリセリン脂肪酸エステルを含有する固形外用組成物は、保形性が良く、はがれ現象および発汗が生じず、成形性が良好であった(実施例2)。さらに使用感も非常によく、被験者からは皮がむけて浮き上がった部分に固形外用組成物が密着して膜のように唇を覆う実効感が持続し、硬くなっていた唇の皮が柔らかくなったという意見を得た。固形外用組成物が皮むけの外面や浮き上がった隙間に入りワックスの密着性で上皮全体を乾燥から保護し、水溶性ビタミンの薬効や多価アルコールの保水性により乾燥して硬くなった上皮に浸透し、うるおいを与え、グリセリン脂肪酸エステルにより油性成分と水性成分の均一性の高い組成物であるため、ワックス、水溶性ビタミン、多価アルコールの機能が適用部位で素早く発揮され、皮むけの改善効果が高いと考えられた。さらに皮むけが生じて凹凸のある唇に対して非常に滑らかに塗る事ができるので、塗布の操作をより短時間で素早く行う事が出来るという意見も得た。
As shown in Table 1, the solid topical composition containing solid wax with a melting point of 40°C or higher, water-soluble vitamins, and polyhydric alcohol has good shape retention, no peeling phenomenon or sweating, and good moldability. (Example 1). A solid external composition containing a solid wax with a melting point of 40°C or higher, water-soluble vitamins, and no polyhydric alcohol has shape retention, but cracks are observed in slightly curved parts. Peeling phenomenon occurred and moldability was poor (Comparative Example 1). Furthermore, in terms of feeling of use, the test subjects evaluated that it felt rough and irritating when applied to the lips, which was unfavorable for peeling skin (Comparative Example 1). A solid external composition containing solid wax with a melting point of 40°C or higher, water-soluble vitamins, and polyhydric alcohol, and containing 2.1% by mass of water has very poor shape retention and poor moldability. Hardness, peeling, perspiration, and feeling of use could not be evaluated (Comparative Example 2). It was considered that Comparative Example 1 and Comparative Example 2 may be due to non-uniformity in the formulation.
A solid external composition containing a solid wax with a melting point of 40°C or higher, a water-soluble vitamin, a polyhydric alcohol, and further containing a glycerin fatty acid ester has good shape retention, does not cause peeling or sweating, and has good moldability. was good (Example 2). Furthermore, the feeling of use was very good, and the test subjects reported that the solid topical composition adhered to the areas where the skin had peeled off and it covered the lips like a film, which lasted for a long time, and the hard skin of the lips softened. I received the opinion that The solid topical composition enters the outer surface of peeled skin and the raised gaps and protects the entire epithelium from drying due to the adhesion of wax, and penetrates into the dry and hardened epithelium due to the medicinal properties of water-soluble vitamins and the water-retaining properties of polyhydric alcohol. The composition has a highly uniform composition of oily and aqueous components due to glycerin fatty acid ester, so the functions of the wax, water-soluble vitamins, and polyhydric alcohol are quickly exerted at the application site, improving peeling effects. was considered high. Furthermore, since it can be applied very smoothly to lips that are uneven due to peeling, we received the opinion that the application process can be done more quickly and in a shorter time.
[試験例3]
下記の表3に示す固形外用組成物を常法に従って調製し、繰り出し式リップスティック容器(ポリプロピレン製)に充填した。容器内で固形外用組成物は直径12mm、長さ40mmの円柱形状である。実施例7~12は保形性、はがれ、発汗の評価は良く、成形性は良好な固形外用組成物である。使用感を以下の評価基準で評価し、結果を表3に示した。
[Test Example 3]
A solid external composition shown in Table 3 below was prepared according to a conventional method and filled into a retractable lipstick container (made of polypropylene). Inside the container, the solid external composition has a cylindrical shape with a diameter of 12 mm and a length of 40 mm. Examples 7 to 12 are solid external compositions with good evaluations of shape retention, peeling, and perspiration, and good moldability. The usability was evaluated using the following evaluation criteria, and the results are shown in Table 3.
(使用感の評価基準)
5名の被験者がリップスティック容器に充填した固形外用組成物を唇に塗布し、3時間後の保湿感について、下記の基準で評価点を付けた。5名の被験者の評価点の平均点を表3に示した。
◎:保湿感を感じる。
〇:保湿感を少し感じる。
×:保湿感を感じない。乾燥していると感じる。
(Evaluation criteria for usability)
Five subjects applied the solid external composition filled in a lipstick container to their lips, and evaluated the moisturizing feeling after 3 hours using the following criteria. Table 3 shows the average evaluation scores of the five subjects.
◎: Feels moisturizing.
○: Feels a little moisturizing.
×: No moisturizing feeling. I feel dry.
表3に示すとおり、実施例7~12の固形外用組成物は保湿感が良好であった。 As shown in Table 3, the solid external compositions of Examples 7 to 12 had a good moisturizing feeling.
Claims (6)
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