JP2005263793A - Skin lotion - Google Patents
Skin lotion Download PDFInfo
- Publication number
- JP2005263793A JP2005263793A JP2005041503A JP2005041503A JP2005263793A JP 2005263793 A JP2005263793 A JP 2005263793A JP 2005041503 A JP2005041503 A JP 2005041503A JP 2005041503 A JP2005041503 A JP 2005041503A JP 2005263793 A JP2005263793 A JP 2005263793A
- Authority
- JP
- Japan
- Prior art keywords
- glycol
- acid
- ether
- skin
- external preparation
- 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
- 239000006210 lotion Substances 0.000 title abstract description 7
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims abstract description 105
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 70
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 claims abstract description 50
- 239000007788 liquid Substances 0.000 claims abstract description 37
- 239000004094 surface-active agent Substances 0.000 claims abstract description 33
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims abstract description 31
- 239000010696 ester oil Substances 0.000 claims abstract description 14
- 238000002360 preparation method Methods 0.000 claims description 69
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 56
- 235000011187 glycerol Nutrition 0.000 claims description 34
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 claims description 21
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 15
- 239000003921 oil Substances 0.000 claims description 15
- SZXQTJUDPRGNJN-UHFFFAOYSA-N dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 claims description 13
- 238000002156 mixing Methods 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 10
- 238000010521 absorption reaction Methods 0.000 abstract description 3
- 239000002552 dosage form Substances 0.000 abstract description 2
- 238000005470 impregnation Methods 0.000 abstract 1
- -1 diol diester Chemical class 0.000 description 82
- 210000003491 skin Anatomy 0.000 description 68
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 description 40
- 235000014113 dietary fatty acids Nutrition 0.000 description 29
- 239000000194 fatty acid Substances 0.000 description 29
- 229930195729 fatty acid Natural products 0.000 description 29
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 26
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 19
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 description 19
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 19
- 150000004665 fatty acids Chemical class 0.000 description 17
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 17
- 239000004973 liquid crystal related substance Substances 0.000 description 17
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 16
- 239000000284 extract Substances 0.000 description 16
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 15
- 230000000694 effects Effects 0.000 description 15
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 14
- OBETXYAYXDNJHR-UHFFFAOYSA-N alpha-ethylcaproic acid Natural products CCCCC(CC)C(O)=O OBETXYAYXDNJHR-UHFFFAOYSA-N 0.000 description 14
- 239000004530 micro-emulsion Substances 0.000 description 14
- 229960002446 octanoic acid Drugs 0.000 description 14
- 229920001223 polyethylene glycol Polymers 0.000 description 14
- CXMXRPHRNRROMY-UHFFFAOYSA-N sebacic acid Chemical compound OC(=O)CCCCCCCCC(O)=O CXMXRPHRNRROMY-UHFFFAOYSA-N 0.000 description 14
- 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 description 13
- 239000005635 Caprylic acid (CAS 124-07-2) Substances 0.000 description 13
- 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 13
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 12
- OVBJJZOQPCKUOR-UHFFFAOYSA-L EDTA disodium salt dihydrate Chemical compound O.O.[Na+].[Na+].[O-]C(=O)C[NH+](CC([O-])=O)CC[NH+](CC([O-])=O)CC([O-])=O OVBJJZOQPCKUOR-UHFFFAOYSA-L 0.000 description 12
- 239000000203 mixture Substances 0.000 description 12
- FBUKVWPVBMHYJY-UHFFFAOYSA-N nonanoic acid Chemical compound CCCCCCCCC(O)=O FBUKVWPVBMHYJY-UHFFFAOYSA-N 0.000 description 12
- 239000008213 purified water Substances 0.000 description 12
- 229920001296 polysiloxane Polymers 0.000 description 11
- 229940037001 sodium edetate Drugs 0.000 description 11
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 10
- 239000004359 castor oil Substances 0.000 description 10
- 235000019438 castor oil Nutrition 0.000 description 10
- 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 10
- 235000021314 Palmitic acid Nutrition 0.000 description 9
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical class OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 9
- 229920001577 copolymer Polymers 0.000 description 9
- 150000002148 esters Chemical class 0.000 description 9
- 229930195733 hydrocarbon Natural products 0.000 description 9
- 150000002430 hydrocarbons Chemical class 0.000 description 9
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 9
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 8
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 8
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 8
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 8
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 8
- 239000005642 Oleic acid Substances 0.000 description 8
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 8
- 239000002202 Polyethylene glycol Substances 0.000 description 8
- 235000021355 Stearic acid Nutrition 0.000 description 8
- ZJCCRDAZUWHFQH-UHFFFAOYSA-N Trimethylolpropane Chemical compound CCC(CO)(CO)CO ZJCCRDAZUWHFQH-UHFFFAOYSA-N 0.000 description 8
- 239000002253 acid Substances 0.000 description 8
- 238000013329 compounding Methods 0.000 description 8
- 150000001875 compounds Chemical class 0.000 description 8
- 239000004220 glutamic acid Substances 0.000 description 8
- 235000013922 glutamic acid Nutrition 0.000 description 8
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 description 8
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 8
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 8
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 8
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 8
- 235000021313 oleic acid Nutrition 0.000 description 8
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 description 8
- 239000008117 stearic acid Substances 0.000 description 8
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 8
- OBETXYAYXDNJHR-SSDOTTSWSA-M (2r)-2-ethylhexanoate Chemical compound CCCC[C@@H](CC)C([O-])=O OBETXYAYXDNJHR-SSDOTTSWSA-M 0.000 description 7
- OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 description 7
- 229940058015 1,3-butylene glycol Drugs 0.000 description 7
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 7
- XFBOJHLYDJZYSP-UHFFFAOYSA-N 2,8-dioxoadenine Chemical compound N1C(=O)N=C2NC(=O)NC2=C1N XFBOJHLYDJZYSP-UHFFFAOYSA-N 0.000 description 7
- ATVJXMYDOSMEPO-UHFFFAOYSA-N 3-prop-2-enoxyprop-1-ene Chemical compound C=CCOCC=C ATVJXMYDOSMEPO-UHFFFAOYSA-N 0.000 description 7
- XZOYHFBNQHPJRQ-UHFFFAOYSA-N 7-methyloctanoic acid Chemical compound CC(C)CCCCCC(O)=O XZOYHFBNQHPJRQ-UHFFFAOYSA-N 0.000 description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 7
- 239000001361 adipic acid Substances 0.000 description 7
- 235000011037 adipic acid Nutrition 0.000 description 7
- 235000019437 butane-1,3-diol Nutrition 0.000 description 7
- 150000003839 salts Chemical class 0.000 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 description 6
- LCZVSXRMYJUNFX-UHFFFAOYSA-N 2-[2-(2-hydroxypropoxy)propoxy]propan-1-ol Chemical compound CC(O)COC(C)COC(C)CO LCZVSXRMYJUNFX-UHFFFAOYSA-N 0.000 description 6
- SVTBMSDMJJWYQN-UHFFFAOYSA-N 2-methylpentane-2,4-diol Chemical compound CC(O)CC(C)(C)O SVTBMSDMJJWYQN-UHFFFAOYSA-N 0.000 description 6
- 239000004215 Carbon black (E152) Substances 0.000 description 6
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 229920002125 Sokalan® Polymers 0.000 description 6
- OEWBEINAQKIQLZ-CMRBMDBWSA-N [(2s)-2-[(2r)-3,4-bis(2-hexyldecanoyloxy)-5-oxo-2h-furan-2-yl]-2-(2-hexyldecanoyloxy)ethyl] 2-hexyldecanoate Chemical compound CCCCCCCCC(CCCCCC)C(=O)OC[C@H](OC(=O)C(CCCCCC)CCCCCCCC)[C@H]1OC(=O)C(OC(=O)C(CCCCCC)CCCCCCCC)=C1OC(=O)C(CCCCCC)CCCCCCCC OEWBEINAQKIQLZ-CMRBMDBWSA-N 0.000 description 6
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Abstract
Description
本発明は、高温安定性が向上した皮膚外用剤に関する。 The present invention relates to a skin external preparation having improved high-temperature stability.
皮膚や粘膜に適用する外用剤には貼付剤、軟膏剤、クリーム剤、ローション剤、固形状製剤など、様々な剤型のものがあり、これらの外用剤には界面活性剤を配合しているものが多い。界面活性剤には大きく分けて合成化合物と天然由来のものがあり、外用剤には乳化剤として合成化合物の非イオン性界面活性剤が広く用いられている。非イオン性界面活性剤(合成)は比較的皮膚刺激性が低いと言われているが、個人差が大きいため刺激感などの問題を生じる場合もある。
一方、天然界面活性剤は天然の動植物中に存在するものに起源を持ち、そのほとんどが食品にも使用できる安全性の高いものであり、利用促進が期待される。しかし、合成界面活性剤と比較すると乳化力が弱いため十分な量の油分を配合できなかったり、本質的に不安定である分散系を長時間安定に保つことができないという問題点がある。特に、液晶は高温における安定性が悪いこと、またマイクロエマルジョンは界面活性剤を多量に必要とすることから天然界面活性剤を用いての調製が難しい。
天然界面活性剤を配合した皮膚外用剤としては、非水ゲル化粧料(特許文献1:特開平5-4911号公報)やオルガノゲル(特許文献2:特開2001-114643号公報)等が知られているが、高濃度のグリセリンと特定の油分の組み合わせについては開示されていない。
さらに、皮膚外用剤は、適用部位に直接塗布して用いられることが多いため、製剤の安定性のみならず、肌への馴染みやすさ等の機能に優れた製剤が望まれている。
There are various types of external preparations applied to the skin and mucous membranes, such as patches, ointments, creams, lotions, solid preparations, etc. These external preparations contain a surfactant. There are many things. Surfactants are roughly classified into synthetic compounds and those derived from nature, and nonionic surfactants of synthetic compounds are widely used as external emulsifiers as emulsifiers. Nonionic surfactants (synthetic) are said to have relatively low skin irritation, but may cause problems such as irritation due to large individual differences.
On the other hand, natural surfactants originate from those present in natural animals and plants, and most of them are safe and can be used in foods, and are expected to promote their use. However, there is a problem that a sufficient amount of oil cannot be blended because the emulsifying power is weak as compared with a synthetic surfactant, and a dispersion system that is essentially unstable cannot be kept stable for a long time. In particular, liquid crystals have poor stability at high temperatures, and microemulsions require a large amount of surfactant, so that they are difficult to prepare using a natural surfactant.
Non-aqueous gel cosmetics (Patent Document 1: Japanese Patent Laid-Open No. 5-4911), organogels (Patent Document 2: Japanese Patent Laid-Open No. 2001-114643) and the like are known as external preparations for skin containing a natural surfactant. However, it does not disclose a combination of high concentration of glycerin and a specific oil.
Furthermore, since an external preparation for skin is often used by directly applying to an application site, a preparation excellent not only in the stability of the preparation but also in functions such as ease of adapting to the skin is desired.
本発明は、高温安定性が向上した皮膚外用剤を提供することを課題とする。 An object of the present invention is to provide an external preparation for skin having improved high-temperature stability.
本発明者らは、上記の目的を達成すべく鋭意研究を行った結果、天然界面活性剤、グリコールまたはグリセリン、油分を含有する組成物に、グリコールエーテルを加えると、高温安定性が顕著に向上することを見出し、本発明を完成した。
すなわち本発明は、下記(1)〜(9)に掲げる皮膚外用剤である。
(1)(A)天然界面活性剤、(B)グリコールまたはグリセリン、(C)液状エステル油、および(D)グリコールエーテルを含有する皮膚外用剤。
(2)グリコールエーテルが、エチレングリコールモノエーテル、エチレングリコールジエーテル、プロピレングリコールモノエーテル、プロピレングリコールジエーテル、ブチレングリコールモノエーテル、ブチレングリコールジエーテル、ジエチレングリコールモノエーテル、ジエチレングリコールモノエーテル、ジエチレングリコールジエーテル、ジプロピレングリコールモノエーテル、ジプロピレングリコールジエーテル、ジブチレングリコールモノエーテルおよびジブチレングリコールジエーテルよりなる群から選択される1種または2種以上である(1)に記載の皮膚外用剤。
(3)天然界面活性剤が、リン脂質および糖脂質である(1)または(2)に記載の皮膚外用剤。
(4)液状エステル油が、分子内に遊離水酸基を持たない液状モノアルコールモノエステル、液状ジオールジエステル、液状トリオールトリエステル、液状テトラオールテトラエステル、液状ペンタオールペンタエステルである(1)〜(3)に記載の皮膚外用剤。
(5)さらに炭化水素またはシリコーンを含有する(1)〜(4)に記載の皮膚外用剤。
(6)さらに水を含有する(1)〜(5)に記載の皮膚外用剤。
(7)皮膚外用剤が液晶型皮膚外用剤である(1)〜(6)に記載の皮膚外用剤。
(8)皮膚外用剤がマイクロエマルジョン型皮膚外用剤である(1)〜(7)に記載の皮膚外用剤。
(9)実質的に合成界面活性剤を含有しない(1)〜(8)に記載の皮膚外用剤。
また、本発明は以下の方法をも包含する。
(10)(A)天然界面活性剤、(B)グリコールまたはグリセリン、および(C)液状油を含有する皮膚外用剤に、グリコールエーテルを配合することによる、皮膚外用剤の安定性向上方法。
As a result of intensive studies to achieve the above object, the inventors of the present invention significantly improved high-temperature stability when a glycol ether is added to a composition containing a natural surfactant, glycol or glycerin, and oil. The present invention has been completed.
That is, this invention is a skin external preparation listed to following (1)-(9).
(1) A skin external preparation containing (A) a natural surfactant, (B) glycol or glycerin, (C) liquid ester oil, and (D) glycol ether.
(2) glycol ether is ethylene glycol monoether, ethylene glycol diether, propylene glycol monoether, propylene glycol diether, butylene glycol monoether, butylene glycol diether, diethylene glycol monoether, diethylene glycol monoether, diethylene glycol diether, di The skin external preparation according to (1), which is one or more selected from the group consisting of propylene glycol monoether, dipropylene glycol diether, dibutylene glycol monoether and dibutylene glycol diether.
(3) The external preparation for skin according to (1) or (2), wherein the natural surfactant is a phospholipid and a glycolipid.
(4) The liquid ester oil is a liquid monoalcohol monoester, liquid diol diester, liquid triol triester, liquid tetraol tetraester, or liquid pentaol pentaester having no free hydroxyl group in the molecule (1) to (3 ) External preparation for skin.
(5) The external preparation for skin according to (1) to (4), further containing a hydrocarbon or silicone.
(6) The external preparation for skin according to (1) to (5), further containing water.
(7) The skin external preparation according to any one of (1) to (6), wherein the skin external preparation is a liquid crystal type skin external preparation.
(8) The external preparation for skin according to (1) to (7), wherein the external preparation for skin is a microemulsion type external preparation for skin.
(9) The external preparation for skin according to (1) to (8), which contains substantially no synthetic surfactant.
The present invention also includes the following methods.
(10) A method for improving the stability of an external preparation for skin by blending glycol ether with an external preparation for skin containing (A) a natural surfactant, (B) glycol or glycerin, and (C) a liquid oil.
本発明は、天然界面活性剤、グリコールまたはグリセリン、液状エステル油、およびグリコールエーテルを含有することで、皮膚外用剤を安定に保つことができる。また、剤型によっては経皮吸収性を良くすることができるため、有用成分の肌への効率的な浸透を期待することができる。 This invention can keep a skin external preparation stable by containing a natural surfactant, glycol or glycerin, liquid ester oil, and glycol ether. Moreover, since transdermal absorbability can be improved depending on the dosage form, efficient penetration of useful components into the skin can be expected.
本発明の皮膚外用剤は、(A)天然界面活性剤、(B)グリコールまたはグリセリン、(C)液状エステル油、および(D)グリコールエーテルを含有することを特徴とする。 The external preparation for skin of the present invention comprises (A) a natural surfactant, (B) glycol or glycerin, (C) liquid ester oil, and (D) glycol ether.
本発明に用いる天然界面活性剤は、主に動物または植物起源の界面活性効果を有する物質であれば特に制限されず、動植物から抽出、精製した天然物であっても、これらの天然物を細胞学的に培養合成、遺伝子工学的合成、あるいは化学合成したものであっても良く、水素添加、水酸化処理などをの加工を施しても良い。また市販品を用いても良い。
本発明において天然界面活性剤とは、主に動物または植物の由来の界面活性効果を有する物質であれば特に制限されず、リン脂質、糖脂質、セラミド(スフィンゴ脂質)、コレステロール、アルキルポリグリコシド、アシル化コラーゲン、グリチルリチン酸塩、カゼイン塩、アルブミン、ビオチン、グルテン、ペクチン、ムチン、サポニン、コンドロイチン硫酸塩、ヒアルロン酸塩、デオキシリボ核酸塩、エラスチン加水分解物、コラーゲン加水分解物、N−アシルグルタミン酸塩、メントール、ボルネオール、胆汁酸等が挙げられ、好ましくはリン脂質または糖脂質である。
The natural surfactant used in the present invention is not particularly limited as long as it is a substance having a surface-active effect mainly of animal or plant origin. Even if it is a natural product extracted and purified from animals and plants, these natural products are converted into cells. It may be chemically synthesized, genetically engineered, or chemically synthesized, and may be subjected to processing such as hydrogenation or hydroxylation. Commercial products may also be used.
In the present invention, the natural surfactant is not particularly limited as long as it is a substance having a surface-active effect mainly derived from animals or plants. Phospholipid, glycolipid, ceramide (sphingolipid), cholesterol, alkylpolyglycoside, Acylated collagen, glycyrrhizinate, caseinate, albumin, biotin, gluten, pectin, mucin, saponin, chondroitin sulfate, hyaluronate, deoxyribonucleic acid salt, elastin hydrolyzate, collagen hydrolyzate, N-acyl glutamate , Menthol, borneol, bile acid and the like, preferably phospholipid or glycolipid.
また、天然界面活性剤は、薬学上許容される塩としても使用でき、例えば、有機塩基との塩(例えば、トリメチルアミン塩、トリエチルアミン塩、モノエタノールアミン塩、トリエタノールアミン塩、ピリジン塩などの第3級アミンとの塩、アルギニンなどの塩基性アンモニウム塩など)、無機塩基との塩(例えば、アンモニウム塩、ナトリウム塩、カリウム塩などのアルカリ金属塩、カルシウム塩、マグネシウム塩などのアルカリ土類金属塩、アルミニウム塩など)などが挙げられ、特に好ましい塩は、ナトリウム塩、カリウム塩である。具体的には、グリチルリチン酸ナトリウム、カゼインナトリウム、コンドロイチン硫酸ナトリウム、ヒアルロン酸ナトリウム、デオキシリボ核酸ナトリウム、N−アシルグルタミン酸ナトリウム、胆汁酸ナトリウム等が挙げられる。 Natural surfactants can also be used as pharmaceutically acceptable salts, for example, salts with organic bases (for example, trimethylamine salts, triethylamine salts, monoethanolamine salts, triethanolamine salts, pyridine salts, etc.). Salts with tertiary amines, basic ammonium salts such as arginine), salts with inorganic bases (for example, alkali metal salts such as ammonium, sodium and potassium salts, alkaline earth metals such as calcium and magnesium salts) Salt, aluminum salt and the like), and particularly preferable salts are sodium salt and potassium salt. Specific examples include sodium glycyrrhizinate, sodium caseinate, sodium chondroitin sulfate, sodium hyaluronate, sodium deoxyribonucleic acid, sodium N-acyl glutamate, sodium bile acid and the like.
本発明における天然界面活性剤の例としてリン脂質および糖脂質が挙げられるが、これらは細胞膜等の構成成分として用いられている物質で、グリセロリン脂質、グリセロ糖脂質、スフィンゴ脂質、スフィンゴ脂質、スフィンゴリン脂質、スフィンゴ糖脂質などが存在している。前記脂質のうち、界面活性効果を有するものであれば良い。
グリセロリン脂質は、グリセロリン酸骨格を有する物質で、親油基として脂肪酸エステル、長鎖アルキルエーテル、ビニルエーテルなどを有している。具体的には、ホスファチジルコリン(レシチン)、ホスファチジルエタノールアミン、ホスファチジルセリン、ホスファジイルイノシトール、ホスファチジルイノシトールポリリン酸、ジホスファチジルグリセロール(カルジオリピン)、ホスファチジン酸、リゾリン脂質が挙げられ、好ましくはレシチンである。レシチンは大豆または卵黄等から抽出・精製して得られる。また、レシチンは、水素添加や水酸化されている、水素添加レシチン、水酸化レシチンなどであっても良い。
グリセロ糖脂質は、親水基として炭水化物、コリンリン酸、2−アミノグリセロールなどを有し、親油基としてジアシルグリセロール、ジアルキルグリセロール、アルキルアシルグリセロール、アルケニルアシルグリセロールを有している。
スフィンゴ脂質は、スフィンゴシン、フィトスフィンゴシンなどの長鎖塩基または長鎖脂肪酸と、脂肪酸がアミド結合したものであり、セラミド1、セラミド2、セラミド3、セラミド4、セラミド5、セラミド6などが挙げられ、好ましくはセラミド3、セラミド6である。
スフィンゴリン脂質は、スフィンゴシン、フィトスフィンゴシンなどの長鎖塩基または長鎖脂肪酸と、リン酸またはホスホン酸を有しており、セラミド1−リン酸誘導体(スフィンゴミエリンなど)、セラミド1−ホスホン酸誘導体(セラミドアミノエチルホスホン酸など)が挙げられる。
スフィンゴ糖脂質は、スフィンゴシン、フィトスフィンゴシンなどの長鎖塩基または長鎖脂肪酸と糖を有しており、セレブロシド、スルファチド、セラミドオリゴヘキソシド、グロボシド、ガングリオシド、ショ糖脂肪酸エステルなどが挙げられ、好ましくはセラミドオリゴヘキソシド、ショ糖脂肪酸エステルである。
これらの天然界面活性物質は、1種または2種以上を使用することができる。
Examples of natural surfactants in the present invention include phospholipids and glycolipids, and these are substances used as components such as cell membranes. Glycerophospholipids, glyceroglycolipids, sphingolipids, sphingolipids, sphingolines Lipids, glycosphingolipids, etc. exist. Any lipid that has a surface-active effect may be used.
Glycerophospholipid is a substance having a glycerophosphoric acid skeleton, and has a fatty acid ester, a long-chain alkyl ether, a vinyl ether or the like as a lipophilic group. Specific examples include phosphatidylcholine (lecithin), phosphatidylethanolamine, phosphatidylserine, phosphadiylinositol, phosphatidylinositol polyphosphate, diphosphatidylglycerol (cardiolipin), phosphatidic acid, and lysophospholipid, preferably lecithin. Lecithin is obtained by extraction and purification from soybean or egg yolk. The lecithin may be hydrogenated or hydroxylated, hydrogenated lecithin, hydroxylated lecithin or the like.
The glyceroglycolipid has a carbohydrate, choline phosphate, 2-aminoglycerol and the like as a hydrophilic group, and has diacylglycerol, dialkylglycerol, alkylacylglycerol, and alkenylacylglycerol as a lipophilic group.
Sphingolipids are long-chain bases or long-chain fatty acids such as sphingosine and phytosphingosine, and fatty acids in an amide bond, and include ceramide 1, ceramide 2, ceramide 3, ceramide 4, ceramide 5, ceramide 6 and the like. Ceramide 3 and ceramide 6 are preferable.
Sphingophospholipids have long-chain bases or long-chain fatty acids such as sphingosine and phytosphingosine, and phosphoric acid or phosphonic acid. Ceramide 1-phosphate derivatives (such as sphingomyelin), ceramide 1-phosphonic acid derivatives ( Ceramide aminoethylphosphonic acid and the like).
Glycosphingolipids have long-chain bases or long-chain fatty acids such as sphingosine and phytosphingosine and sugars, and include cerebroside, sulfatide, ceramide oligohexoside, globoside, ganglioside, sucrose fatty acid ester, etc. Is ceramide oligohexoside, sucrose fatty acid ester.
These natural surfactants can be used alone or in combination of two or more.
本発明で用いる天然界面活性物質の配合量は、本発明の効果を奏すれば特に制限されないが、皮膚外用剤全体として、0.001〜10重量%、好ましくは0.01〜5重量%、特に好ましくは0.1〜5重量%であれば良い。0.001重量%より少ないと製剤化が困難になり、10重量%を超えると使用感が低下する傾向が強くなるため好ましくない。 The blending amount of the natural surfactant used in the present invention is not particularly limited as long as the effects of the present invention are exerted, but as a whole external preparation for skin, 0.001 to 10% by weight, preferably 0.01 to 5% by weight, particularly preferably 0.1. It should be ~ 5% by weight. If the amount is less than 0.001% by weight, it becomes difficult to formulate, and if it exceeds 10% by weight, the feeling of use tends to decrease, which is not preferable.
本発明においてグリコールとは、30℃で液体である多価アルコールであれば良く、具体的にはエチレングリコール、プロピレングリコール、トリメチレングリコール、1,2−ブチレングリコール、1,3−ブチレングリコール、2,3−ブチレングリコール、ペンタメチレングリコール、ヘキシレングリコール、オクチレングリコールなどが挙げられ、好ましくはプロピレングリコール、1,3−ブチレングリコールである。
また、グリセリンは、皮膚外用剤などに頻用されている公知の化合物である。
これらのグリコールまたはグリセリンは、1種又は2種以上組み合わせて使用できる。
In the present invention, the glycol may be any polyhydric alcohol that is liquid at 30 ° C., specifically, ethylene glycol, propylene glycol, trimethylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 2 1,3-butylene glycol, pentamethylene glycol, hexylene glycol, octylene glycol and the like, and propylene glycol and 1,3-butylene glycol are preferable.
Glycerin is a known compound that is frequently used in external preparations for skin.
These glycols or glycerin can be used alone or in combination of two or more.
本発明で用いるグリコールまたはグリセリンの配合量は、本発明の効果を奏すれば特に制限されないが、皮膚外用剤全体として、1〜85重量%、好ましくは5〜85重量%、特に好ましくは10〜80重量%であれば良い。1重量%より少ないと製剤化が困難になり、85重量%を超えると使用感が低下する傾向が強くなるため好ましくない。 The blending amount of glycol or glycerin used in the present invention is not particularly limited as long as the effects of the present invention are exhibited, but as a whole skin external preparation, 1 to 85% by weight, preferably 5 to 85% by weight, particularly preferably 10 to 80% by weight is sufficient. If the amount is less than 1% by weight, preparation becomes difficult, and if it exceeds 85% by weight, the feeling of use tends to decrease.
本発明で用いる液状エステル油は、エステル結合を有し30℃で液状である油であれば特に限定されず、例えばモノアルコールモノエステル、ジオールモノエステル、ジオールジエステル、トリオールジエステル、トリオールトリエステル、テトラオールトリエステル、テトラオールテトラエステル、ペンタオールテトラエステル、ペンタオールペンタエステルなどが挙げられ、好ましくは分子内に遊離の水酸基を持たないモノアルコールモノエステル、ジオールジエステル、トリオールトリエステル、テトラオールテトラエステル、ペンタオールペンタエステルである。 The liquid ester oil used in the present invention is not particularly limited as long as it has an ester bond and is liquid at 30 ° C. For example, monoalcohol monoester, diol monoester, diol diester, triol diester, triol triester, tetra Examples include all triesters, tetraol tetraesters, pentaol tetraesters, pentaol pentaesters, preferably monoalcohol monoesters, diol diesters, triol triesters, tetraol tetraesters having no free hydroxyl groups in the molecule. , Pentaol pentaester.
モノアルコールモノエステルとしては、酢酸dl−α−トコフェロール、酢酸d−α−トコフェロール、酢酸−β−トコフェロール、酢酸γ−トコフェロール、酢酸δ−トコフェロール、C2以上のモノアルコールとC8以上の直鎖または分岐脂肪酸とのエステルが好ましく、C2以上のアルコールとしては、エタノール、プロパノール、イソプロパノール、ブタノール、イソブタノール、ペンタノール、ヘキサノール、オクタノール、2−エチルヘキサノール、ノニルアルコール、イソノニルアルコール、デシルアルコール、イソデシルアルコール、トリデシルアルコール、イソトリデシルアルコール、ミリスチルアルコール、セタノール、イソセタノール、2−ヘキシルデシルアルコール、ステアリルアルコール、イソステアリルアルコール、2−ヘプチルウンデシルアルコール、2−オクチルドデシルアルコールなどが挙げられ、C8以上の直鎖または分岐脂肪酸としては、カプリル酸、オクタン酸、2−エチルヘキサン酸、ノナン酸、イソノナン酸、カプリン酸、ジメチルオクタン酸、ミリスチン酸、パルミチン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、アジピン酸、グルタミン酸、セバシン酸などが挙げられる。
具体的には、オクタン酸セチル、オクタン酸イソセチル、オクタン酸セトステアリル、オクタン酸ステアリル、オクタン酸イソステアリル、2−エチルヘキサン酸セチル、ジメチルオクタン酸ヘキシルデシル、ミリスチン酸イソプロピル、ミリスチン酸イソステアリル、ミリスチン酸イソセチル、ミリスチン酸オクチルドデシル、ミリスチン酸ミリスチル、ミリスチン酸2−ヘキシルデシル、パルミチン酸イソプロピル、パルミチン酸イソステアリル、パルミチン酸2−ヘキシルデシル、パルミチン酸2−ヘプチルウンデシル、パルミチン酸オクチル、パルミチン酸2−エチルヘキシル、ステアリン酸エチル、ステアリン酸ブチル、ラウリン酸エチル、ラウリン酸ヘキシル、ジメチルオクタン酸ヘキシルデシル、ステアリン酸イソセチル、イソステアリン酸イソプロピル、イソステアリン酸イソセチル、イソステアリン酸イソステアリル、イソノナン酸イソノニル、イソノナン酸トリデシル、イソノナン酸イソデシル、イソノナン酸イソトリデシル、オレイン酸オレイル、オレイン酸エチル、オレイン酸デシル、オレイン酸オクチルドデシル、リノール酸エチル、リノール酸イソプロピル、アジピン酸2−ヘキシルデシル、アジピン酸ジイソブチル、アジピン酸ジ−2−ヘプチルウンデシル、セバシン酸ジ−2−エチルヘキシル、セバシン酸ジイソプロピル等が挙げられる。
Monoalcohol monoesters include dl-α-tocopherol acetate, d-α-tocopherol acetate, acetic acid-β-tocopherol, acetic acid γ-tocopherol, acetic acid δ-tocopherol, C2 or more monoalcohol and C8 or more linear or branched. Esters with fatty acids are preferred, and C2 or higher alcohols include ethanol, propanol, isopropanol, butanol, isobutanol, pentanol, hexanol, octanol, 2-ethylhexanol, nonyl alcohol, isononyl alcohol, decyl alcohol, isodecyl alcohol , Tridecyl alcohol, isotridecyl alcohol, myristyl alcohol, cetanol, isocetanol, 2-hexyldecyl alcohol, stearyl alcohol, isostearyl alcohol , 2-heptylundecyl alcohol, 2-octyldodecyl alcohol, etc., and C8 or higher linear or branched fatty acids include caprylic acid, octanoic acid, 2-ethylhexanoic acid, nonanoic acid, isononanoic acid, capric acid, Examples include dimethyloctanoic acid, myristic acid, palmitic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, adipic acid, glutamic acid, and sebacic acid.
Specifically, cetyl octoate, isocetyl octoate, cetostearyl octoate, stearyl octoate, isostearyl octoate, cetyl 2-ethylhexanoate, hexyldecyl dimethyloctanoate, isopropyl myristate, isostearyl myristate, myristic Isocetyl acid, octyldodecyl myristate, myristyl myristate, 2-hexyldecyl myristate, isopropyl palmitate, isostearyl palmitate, 2-hexyldecyl palmitate, 2-heptyl undecyl palmitate, octyl palmitate, palmitic acid 2 -Ethylhexyl, ethyl stearate, butyl stearate, ethyl laurate, hexyl laurate, hexyl decyl dimethyloctanoate, isocetyl stearate, Isopropyl stearate, isocetyl isostearate, isostearyl isostearate, isononyl isononanoate, tridecyl isononanoate, isodecyl isononanoate, isotridecyl isononanoate, oleyl oleate, ethyl oleate, decyl oleate, octyldodecyl oleate, ethyl linoleate, Examples include isopropyl linoleate, 2-hexyldecyl adipate, diisobutyl adipate, di-2-heptylundecyl adipate, di-2-ethylhexyl sebacate, diisopropyl sebacate and the like.
ジオールモノエステルとしては、グリコールとC8以上の直鎖または分岐脂肪酸のエステルが好ましく、グリコールとしては、エチレングリコール、プロピレングリコール、トリメチレングリコール、1,2−ブチレングリコール、1,3−ブチレングリコール、2,3−ブチレングリコール、ペンタメチレングリコール、ヘキシレングリコール、ネオペンチレングリコール、オクチレングリコールなどが挙げられ、C8以上の直鎖または分岐脂肪酸としては、カプリル酸、オクタン酸、2−エチルヘキサン酸、ノナン酸、イソノナン酸、カプリン酸、ジメチルオクタン酸、ミリスチン酸、パルミチン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、アジピン酸、グルタミン酸、セバシン酸等が挙げられる。
具体的には、モノカプリル酸プロピレングリコールなどが挙げられる。
The diol monoester is preferably an ester of glycol and a C8 or higher straight chain or branched fatty acid. Examples of the glycol include ethylene glycol, propylene glycol, trimethylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 2 , 3-butylene glycol, pentamethylene glycol, hexylene glycol, neopentylene glycol, octylene glycol, etc., and C8 or higher linear or branched fatty acids include caprylic acid, octanoic acid, 2-ethylhexanoic acid, Nonanoic acid, isononanoic acid, capric acid, dimethyloctanoic acid, myristic acid, palmitic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, adipic acid, glutamic acid, sebacic acid and the like.
Specific examples include propylene glycol monocaprylate.
ジオールジエステルとしては、グリコールとC8以上の直鎖または分岐脂肪酸のエステルが好ましく、グリコールとしては、エチレングリコール、プロピレングリコール、トリメチレングリコール、1,2−ブチレングリコール、1,3−ブチレングリコール、2,3−ブチレングリコール、ペンタメチレングリコール、ヘキシレングリコール、ネオペンチレングリコール、オクチレングリコールなどが挙げられ、C8以上の直鎖または分岐脂肪酸としては、カプリル酸、オクタン酸、2−エチルヘキサン酸、ノナン酸、イソノナン酸、カプリン酸、ジメチルオクタン酸、ミリスチン酸、パルミチン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、アジピン酸、グルタミン酸、セバシン酸等が挙げられる。
具体的には、ジ−2−エチルヘキサン酸エチレングリコール、モノイソステアリン酸N−アルキルグリコール、ジイソノナン酸プロピレングリコール、ジ−2−エチルヘキサン酸ネオペンチレングリコール、ジカプリン酸プロピレングリコール、ジカプリル酸プロピレングリコール、ジノナン酸プロピレングリコール、ジ(カプリル・カプリン酸)プロピレングリコール、ジステアリン酸プロピレングリコール、ジイソステアリン酸プロピレングリコール、ジオレイン酸プロピレングリコール、ジイソノナン酸エチレングリコール、ジカプリン酸ネオペンチルグリコール、ジカプリン酸ネオペンチルグリコール等が挙げられる。
The diol diester is preferably an ester of glycol and a C8 or higher linear or branched fatty acid. As the glycol, ethylene glycol, propylene glycol, trimethylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 2, Examples include 3-butylene glycol, pentamethylene glycol, hexylene glycol, neopentylene glycol, and octylene glycol. Examples of the C8 or higher linear or branched fatty acid include caprylic acid, octanoic acid, 2-ethylhexanoic acid, and nonane. Examples include acids, isononanoic acid, capric acid, dimethyloctanoic acid, myristic acid, palmitic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, adipic acid, glutamic acid, sebacic acid and the like.
Specifically, ethylene glycol di-2-ethylhexanoate, N-alkyl glycol monoisostearate, propylene glycol diisononanoate, di-2-ethylhexanoate neopentylene glycol, propylene glycol dicaprate, propylene glycol dicaprylate, Propylene glycol dinonanoate, propylene glycol di (capryl / capric acid), propylene glycol distearate, propylene glycol diisostearate, propylene glycol dioleate, ethylene glycol diisononanoate, neopentyl glycol dicaprate, neopentyl glycol dicaprate, etc. .
トリオールジエステルとしては、C3以上のトリオールとC8以上の直鎖または分岐脂肪酸のエステルが好ましく、C3以上のトリオールとしては、グリセリン、トリメチロールプロパン、ピリドキシン等が挙げられ、C8以上の直鎖または分岐脂肪酸としては、カプリル酸、オクタン酸、2−エチルヘキサン酸、ノナン酸、イソノナン酸、カプリン酸、ジメチルオクタン酸、ミリスチン酸、パルミチン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、アジピン酸、グルタミン酸、セバシン酸等が挙げられる。 The triol diester is preferably an ester of a C3 or higher triol and a C8 or higher linear or branched fatty acid, and the C3 or higher triol includes glycerin, trimethylolpropane, pyridoxine, etc., and a C8 or higher linear or branched fatty acid. As caprylic acid, octanoic acid, 2-ethylhexanoic acid, nonanoic acid, isononanoic acid, capric acid, dimethyloctanoic acid, myristic acid, palmitic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, adipic acid, glutamic acid And sebacic acid.
トリオールトリエステルとしては、C3以上のトリオールとC8以上の直鎖または分岐脂肪酸のエステルが好ましく、C3以上のトリオールとしては、グリセリン、トリメチロールプロパン、ピリドキシン等が挙げられ、C8以上の直鎖または分岐脂肪酸としては、カプリル酸、オクタン酸、2−エチルヘキサン酸、ノナン酸、イソノナン酸、カプリン酸、ジメチルオクタン酸、ミリスチン酸、パルミチン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、アジピン酸、グルタミン酸、セバシン酸等が挙げられる。
具体的には、トリ−2−エチルヘキサン酸トリメチロールプロパン、トリイソステアリン酸トリメチロールプロパン、トリ2−エチルヘキサン酸グリセリル、トリオクタン酸グリセリン、トリパルミチン酸グリセリル、トリイソパルミチン酸グリセリン、トリミリスチン酸グリセリン、トリイソステアリン酸グリセリル、トリオレイン酸グリセリル、トリカプリル酸グリセリル、トリ(カプリル・カプリン酸)グリセリル、トリ−2−ヘプチルウンデカン酸グリセリン、トリ2−ヘキシルデカン酸ピリドキシン、トリカプリル酸ピリドキシン、トリパルミチン酸ピリドキシン等が挙げられる。
The triol triester is preferably an ester of a C3 or higher triol and a C8 or higher straight chain or branched fatty acid, and the C3 or higher triol includes glycerin, trimethylolpropane, pyridoxine, etc., and a C8 or higher straight chain or branched chain. As fatty acids, caprylic acid, octanoic acid, 2-ethylhexanoic acid, nonanoic acid, isononanoic acid, capric acid, dimethyloctanoic acid, myristic acid, palmitic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, adipic acid, Examples thereof include glutamic acid and sebacic acid.
Specifically, tri-2-ethylhexanoic acid trimethylolpropane, triisostearic acid trimethylolpropane, tri-2-ethylhexanoic acid glyceryl, trioctanoic acid glyceryl, tripalmitic acid glycerin, triisopalmitic acid glycerin, trimyristic acid glycerin Glyceryl triisostearate, glyceryl trioleate, glyceryl tricaprylate, glyceryl tri (capryl / capric acid), glyceryl tri-2-heptylundecanoate, pyridoxine tri-2-hexyldecanoate, pyridoxine tricaprylate, pyridoxine tripalmitate, etc. Can be mentioned.
テトラオールトリエステルとしては、C4以上のテトラオールとC8以上の直鎖または分岐脂肪酸のエステルが好ましく、C4以上のテトラオールとしては、ペンタエリスリトール、アスコルビン酸、ジグリセリルなどが挙げられ、C8以上の直鎖または分岐脂肪酸としては、カプリル酸、オクタン酸、2−エチルヘキサン酸、ノナン酸、イソノナン酸、カプリン酸、ジメチルオクタン酸、ミリスチン酸、パルミチン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、アジピン酸、グルタミン酸、セバシン酸等が挙げられる。
具体的には、トリイソステアリン酸ジグリセリルなどが挙げられる。
The tetraol triester is preferably an ester of C4 or higher and a linear or branched fatty acid of C8 or higher. Examples of the C4 or higher tetraol include pentaerythritol, ascorbic acid, diglyceryl, etc. As linear or branched fatty acids, caprylic acid, octanoic acid, 2-ethylhexanoic acid, nonanoic acid, isononanoic acid, capric acid, dimethyloctanoic acid, myristic acid, palmitic acid, stearic acid, isostearic acid, oleic acid, linoleic acid , Adipic acid, glutamic acid, sebacic acid and the like.
Specific examples include diglyceryl triisostearate.
テトラオールテトラエステルとしては、C4以上のテトラオールとC8以上の直鎖または分岐脂肪酸のエステルが好ましく、C4以上のテトラオールとしては、ペンタエリスリトール、アスコルビン酸、ジグリセリル、ポリグリセリルなどが挙げられ、C8以上の直鎖または分岐脂肪酸としては、カプリル酸、オクタン酸、2−エチルヘキサン酸、ノナン酸、イソノナン酸、カプリン酸、ジメチルオクタン酸、ミリスチン酸、パルミチン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、アジピン酸、グルタミン酸、セバシン酸等が挙げられる。
具体的には、テトラ2−エチルヘキサン酸ペンタエリスリトール、テトライソステアリン酸ポリグリセリル、テトラ2−ヘキシルデカン酸アスコルビル等が挙げられる。
The tetraol tetraester is preferably an ester of a C4 or higher tetraol and a C8 or higher linear or branched fatty acid, and the C4 or higher tetraol includes pentaerythritol, ascorbic acid, diglyceryl, polyglyceryl, etc. As the above linear or branched fatty acids, caprylic acid, octanoic acid, 2-ethylhexanoic acid, nonanoic acid, isononanoic acid, capric acid, dimethyloctanoic acid, myristic acid, palmitic acid, stearic acid, isostearic acid, oleic acid, Linoleic acid, adipic acid, glutamic acid, sebacic acid and the like can be mentioned.
Specific examples include pentaerythritol tetra-2-ethylhexanoate, polyglyceryl tetraisostearate, ascorbyl tetra-2-hexyldecanoate, and the like.
これらの液状エステル油は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。さらに、液状エステル油のアルコールの価数が異なるもの(例えば、モノアルコールモノエステルとジオールジエステル)を組み合わせて使用すると、より安定性が高くなるため特に好ましい。 These liquid ester oils can be used alone or in any combination of two or more. Furthermore, it is particularly preferable to use a combination of liquid ester oils having different alcohol valences (for example, monoalcohol monoester and diol diester) because the stability becomes higher.
本発明で用いる液状エステル油の配合量は、本発明の効果を奏すれば特に制限されないが、皮膚外用剤全体として通常0.01〜80%、好ましくは0.1〜60重量%、特に好ましくは1〜50重量%であれば良い。0.01重量%より少ないと製剤化が困難もしくは充分な効果が得られず、80重量%を超えると安定性が低下する傾向が強くなるため好ましくない。 The blending amount of the liquid ester oil used in the present invention is not particularly limited as long as the effects of the present invention are obtained, but is generally 0.01 to 80%, preferably 0.1 to 60% by weight, particularly preferably 1 to 50% as a whole skin external preparation. It is sufficient if it is weight%. If it is less than 0.01% by weight, it is difficult to formulate or a sufficient effect cannot be obtained, and if it exceeds 80% by weight, the stability tends to decrease, which is not preferable.
本発明においてグリコールエーテルとは、グリコールの水酸基の片方または両方がエーテル化した化合物であれば特に制限されず、グリコールは単一のオリゴマー、またはポリマーであっても2種以上のオリゴマーであっても良い。例えば、エチレングリコールモノエーテル、エチレングリコールジエーテル、ジエチレングリコールモノエーテル、ジエチレングリコールジエーテル、トリエチレングリコールモノエーテル、トリエチレングリコールジエーテル、テトラエチレングリコールモノエーテル、テトラエチレングリコールジエーテル、ポリエチレングリコールモノエーテル、プロピレングリコールモノエーテル、プロピレングリコールジエーテル、ジプロピレングリコールモノエーテル、ジプロピレングリコールジエーテル、トリプロピレングリコールモノエーテル、トリプロピレングリコールジエーテル、ポリプロピレングリコールモノエーテル、ブチレングリコールモノエーテル、ブチレングリコールジエーテル、アルキレングリコールアセタート等が挙げられる。また、エーテルとしてはアルキルエーテル、アルコキシエーテル、芳香族エーテル、アリルエーテルなどが例示でき、具体的にはエチルエーテル、メチルエーテル、n-プロピルエーテル、イソプロピルエーテル、n-ブチルエーテル、イソブチルエーテル、t-ブチルエーテル、n-ペンチルエーテル、n-ヘキシルエーテル、フェニルエーテル、ビニルエーテル等が挙げられる。 In the present invention, the glycol ether is not particularly limited as long as one or both of the hydroxyl groups of glycol are etherified. The glycol may be a single oligomer, a polymer, or two or more oligomers. good. For example, ethylene glycol monoether, ethylene glycol diether, diethylene glycol monoether, diethylene glycol diether, triethylene glycol monoether, triethylene glycol diether, tetraethylene glycol monoether, tetraethylene glycol diether, polyethylene glycol monoether, propylene Glycol monoether, propylene glycol diether, dipropylene glycol monoether, dipropylene glycol diether, tripropylene glycol monoether, tripropylene glycol diether, polypropylene glycol monoether, butylene glycol monoether, butylene glycol diether, alkylene glycol Such as acetate That. Examples of ethers include alkyl ethers, alkoxy ethers, aromatic ethers, and allyl ethers. Specifically, ethyl ether, methyl ether, n-propyl ether, isopropyl ether, n-butyl ether, isobutyl ether, t-butyl ether. N-pentyl ether, n-hexyl ether, phenyl ether, vinyl ether and the like.
グリコールエーテルの具体例としては、エチレングリコールモノビニルエーテル、エチレングリコールモノエチルエーテル、エチレングリコールモノ-n-プロピルエーテル、エチレングリコールモノイソプロピルエーテル、エチレングリコールモノ-n-ブチルエーテル、エチレングリコールモノイソブチルエーテル、エチレングリコールモノ-t-ブチルエーテル、エチレングリコールモノ-2-メチルペンチルエーテル、エチレングリコールモノ-n-ヘキシルエーテル、エチレングリコールモノ-24-ヘキサジエンエーテル、エチレングリコールモノ-2,6,8-トリメチル-4-ノニルエーテル、エチレングリコールモノフェニルエーテル、及びエチレングリコールモノメチルフェニルエーテル等のエチレングリコールモノエーテル;エチレングリコールジメチルエーテル、及びエチレングリコールジエチルエーテル等のエチレングリコールジエーテル;ジエチレングリコールモノメチルエーテル、ジエチレングリコールモノエチルエーテル(以下エトキシジグリコールとも言う)、ジエチレングリコールモノ-n-プロピルエーテル、ジエチレングリコールモノ-n-ブチルエーテル、ジエチレングリコールモノイソブチルエーテル、ジエチレングリコールモノ-n-ヘキシルエーテル、及びジエチレングリコールモノメチルフェニルエーテル等のジエチレングリコールモノエーテル; ジエチレングリコールジメチルエーテル、ジエチレングリコールジビニルエーテル等のジエチレングリコールジエーテル;トリエチレングリコールモノメチルエーテル、トリエチレングリコールモノエチルエーテル、トリエチレングリコールモノ-n-ブチルエーテル及びトリエチレングリコールモノビニルエチルエーテル等のトリエチレングリコールモノエーテル;トリエチレングリコールジメチルエーテル、トリエチレングリコールジビニルエーテル等のトリエチレングリコールジエーテル;テトラエチレングリコールモノフェニルエーテル等のテトラエチレングリコールモノエーテル;テトラエチレングリコールジエチルエーテル等のテトラエチレングリコールジエーテル;ポリエチレングリコールモノメチルエーテル等のポリエチレングリコールモノエーテル;プロピレングリコールモノメチルエーテル、プロピレングリコールモノエチルエーテル、プロピレングリコール-n-モノプロピルエーテル、プロピレングリコールモノイソプロピルエーテル、プロピレングリコールモノ-n-ブチルエーテル、プロピレングリコールモノイソブチルエーテル、プロピレングリコールモノアリルエーテル、プロピレングリコールモノフェニルエーテル等のプロピレングリコールモノエーテル;プロピレングリコールジメチルエーテル、プロピレングリコールジエチルエーテル、プロピレングリコール-n-ジプロピルエーテル、プロピレングリコールジイソプロピルエーテル、プロピレングリコールジn-ブチルエーテル、プロピレングリコールジイソブチルエーテル、プロピレングリコールジアリルエーテル、プロピレングリコールジフェニルエーテル等のプロピレングリコールジエーテル;ジプロピレングリコールモノエチルエーテル、及びジプロピレングリコールモノ-n-ブチルエーテル、ジプロピレングリコールモノイソブチルエーテル、ジプロピレングリコールアリルエーテル等のジプロピレングリコールモノエーテル;ジプロピレングリコールジエチルエーテル、及びジプロピレングリコールジn-ブチルエーテル、ジプロピレングリコールジイソブチルエーテル、ジプロピレングリコールアリルエーテル等のジプロピレングリコールジエーテル;トリプロピレングリコールモノメチルエーテル、トリプロピレングリコールモノエチルエーテル、及びトリプロピレングリコールモノ-n-ブチルエーテル、トリプロピレングリコールモノイソブチルエーテル、トリプロピレングリコールモノアリルエーテル等のトリプロピレングリコールモノエーテル;トリプロピレングリコールジメチルエーテル、トリプロピレングリコールジエチルエーテル、及びトリプロピレングリコールジn-ブチルエーテル、トリプロピレングリコールジイソブチルエーテル、トリプロピレングリコールジアリルエーテル等のトリプロピレングリコールジエーテル;ポリプロピレングリコールモノブチルエーテル等のポリプロピレングリコールモノエーテル;ブチレングリコールモノメチルエーテル、ブチレングリコールモノエチルエーテル、及びブチレングリコールモノ-n-ブチルエーテル等のブチレングリコールモノエーテル;ブチレングリコールジメチルエーテル、ブチレングリコールジエチルエーテル、及びブチレングリコールジn-ブチルエーテル等のブチレングリコールジエーテル;エチレングリコールモノメチルエーテルアセタート、エチレングリコールモノエチルエーテルアセタート、エチレングリコールモノ-n-ブチルエーテルアセタート、ジエチレングリコールモノエチルエーテルアセタート、ジエチレングリコールモノ-n-ブチルエーテルアセタート、プロピレングリコールモノメチルエーテルアセテート等のアルキレングリコールアセタート;等が挙げられる。 Specific examples of glycol ethers include ethylene glycol monovinyl ether, ethylene glycol monoethyl ether, ethylene glycol mono-n-propyl ether, ethylene glycol monoisopropyl ether, ethylene glycol mono-n-butyl ether, ethylene glycol monoisobutyl ether, ethylene glycol Mono-t-butyl ether, ethylene glycol mono-2-methylpentyl ether, ethylene glycol mono-n-hexyl ether, ethylene glycol mono-24-hexadiene ether, ethylene glycol mono-2,6,8-trimethyl-4-nonyl ether Ethylene glycol monoethers such as ethylene glycol monophenyl ether and ethylene glycol monomethyl phenyl ether; And ethylene glycol diethers such as ethylene glycol diethyl ether; diethylene glycol monomethyl ether, diethylene glycol monoethyl ether (hereinafter also referred to as ethoxy diglycol), diethylene glycol mono-n-propyl ether, diethylene glycol mono-n-butyl ether, diethylene glycol monoisobutyl ether Diethylene glycol monoethers such as diethylene glycol mono-n-hexyl ether and diethylene glycol monomethyl phenyl ether; diethylene glycol diethers such as diethylene glycol dimethyl ether and diethylene glycol divinyl ether; triethylene glycol monomethyl ether, triethylene glycol monoethyl ether, triethylene glycol Triethylene glycol monoethers such as mono-n-butyl ether and triethylene glycol monovinyl ethyl ether; Triethylene glycol diethers such as triethylene glycol dimethyl ether and triethylene glycol divinyl ether; Tetraethylene glycol mono ethers such as tetraethylene glycol monophenyl ether Ether; Tetraethylene glycol diether such as tetraethylene glycol diethyl ether; Polyethylene glycol monoether such as polyethylene glycol monomethyl ether; Propylene glycol monomethyl ether, Propylene glycol monoethyl ether, Propylene glycol-n-monopropyl ether, Propylene glycol monoisopropyl Ether, propylene glycol Propylene glycol monoethers such as mono-n-butyl ether, propylene glycol monoisobutyl ether, propylene glycol monoallyl ether, propylene glycol monophenyl ether; propylene glycol dimethyl ether, propylene glycol diethyl ether, propylene glycol-n-dipropyl ether, propylene glycol Propylene glycol diethers such as diisopropyl ether, propylene glycol di n-butyl ether, propylene glycol diisobutyl ether, propylene glycol diallyl ether, propylene glycol diphenyl ether; dipropylene glycol monoethyl ether, and dipropylene glycol mono-n-butyl ether, dipropylene glycol Monoisobutyl Dipropylene glycol monoethers such as ether, dipropylene glycol allyl ether; dipropylene glycol diethers such as dipropylene glycol diethyl ether, dipropylene glycol di n-butyl ether, dipropylene glycol diisobutyl ether, dipropylene glycol allyl ether; Propylene glycol monomethyl ether, tripropylene glycol monoethyl ether, and tripropylene glycol mono-ether such as tripropylene glycol mono-n-butyl ether, tripropylene glycol monoisobutyl ether, tripropylene glycol monoallyl ether; tripropylene glycol dimethyl ether, tripropylene Glycol diethyl ether and tripropylene glycol Tripropylene glycol diethers such as polypropylene n-butyl ether, tripropylene glycol diisobutyl ether, tripropylene glycol diallyl ether; polypropylene glycol monoethers such as polypropylene glycol monobutyl ether; butylene glycol monomethyl ether, butylene glycol monoethyl ether, and butylene glycol mono -Butylene glycol monoethers such as n-butyl ether; butylene glycol diethers such as butylene glycol dimethyl ether, butylene glycol diethyl ether, and butylene glycol di n-butyl ether; ethylene glycol monomethyl ether acetate, ethylene glycol monoethyl ether acetate, ethylene Glycol mono-n-butyl ether And alkylene glycol acetates such as acetate, diethylene glycol monoethyl ether acetate, diethylene glycol mono-n-butyl ether acetate, and propylene glycol monomethyl ether acetate.
グリコールエーテルとして好ましくは、エチレングリコールモノエーテル、エチレングリコールジエーテル、ジエチレングリコールモノエーテル、ジエチレングリコールジエーテル、トリエチレングリコールモノエーテル、テトラエチレングリコールモノエーテル、テトラエチレングリコールジエーテル、ポリエチレングリコールモノエーテル、プロピレングリコールモノエーテル、プロピレングリコールジエーテル、ジプロピレングリコールモノエーテル、ジプロピレングリコールジエーテル、トリプロピレングリコールモノエーテルであり、具体的にはエチレングリコールモノビニルエーテル、エチレングリコールモノエチルエーテル、エチレングリコールモノ-n-プロピルエーテル、エチレングリコールモノイソプロピルエーテル、エチレングリコールモノ-n-ブチルエーテル、エチレングリコールモノイソブチルエーテル、エチレングリコールモノ-t-ブチルエーテル、エチレングリコールモノ-2-メチルペンチルエーテル、エチレングリコールジメチルエーテル、エチレングリコールジエチルエーテル、ジエチレングリコールモノメチルエーテル、ジエチレングリコールモノエチルエーテル、ジエチレングリコールモノ-n-プロピルエーテル、ジエチレングリコールモノ-n-ブチルエーテル、ジエチレングリコールモノイソブチルエーテル、ジエチレングリコールモノ-n-ヘキシルエーテル、ジエチレングリコールモノメチルフェニルエーテル、ジエチレングリコールジメチルエーテル、ジエチレングリコールジビニルエーテル、ジエチレングリコールエチルビニルエーテル、トリエチレングリコールモノメチルエーテル、トリエチレングリコールモノエチルエーテル、トリエチレングリコールモノ-n-ブチルエーテル、トリエチレングリコールモノビニルエチルエーテル、テトラエチレングリコールモノフェニルエーテル、テトラエチレングリコールジエチルエーテル、ポリエチレングリコールメチルモノエーテル、プロピレングリコールモノメチルエーテル、プロピレングリコールモノエチルエーテル、プロピレングリコール-n-モノプロピルエーテル、プロピレングリコールモノイソプロピルエーテル、プロピレングリコールモノ-n-ブチルエーテル、プロピレングリコールフェニルエーテル、プロピレングリコールモノメチルエーテル、プロピレングリコールジメチルエーテル、プロピレングリコールジエチルエーテル、プロピレングリコール-n-ジプロピルエーテル、プロピレングリコールジイソプロピルエーテル、プロピレングリコールジn-ブチルエーテル、プロピレングリコールジイソブチルエーテル、プロピレングリコールジアリルエーテル、プロピレングリコールジフェニルエーテル、ジプロピレングリコールモノエチルエーテル、ジプロピレングリコールモノ-n-ブチルエーテル、ジプロピレングリコールジエチルエーテル、及びジプロピレングリコールジn-ブチルエーテル、ジプロピレングリコールジイソブチルエーテル、ジプロピレングリコールアリルエーテル、トリプロピレングリコールモノメチルエーテル、トリプロピレングリコールモノエチルエーテル、およびトリプロピレングリコールモノ-n-ブチルエーテルである。 Preferred glycol ethers are ethylene glycol monoether, ethylene glycol diether, diethylene glycol monoether, diethylene glycol diether, triethylene glycol monoether, tetraethylene glycol monoether, tetraethylene glycol diether, polyethylene glycol monoether, propylene glycol mono Ether, propylene glycol diether, dipropylene glycol monoether, dipropylene glycol diether, tripropylene glycol monoether, specifically ethylene glycol monovinyl ether, ethylene glycol monoethyl ether, ethylene glycol mono-n-propyl ether , Ethylene glycol monoisopropyl ether, ethyl Glycol mono-n-butyl ether, ethylene glycol monoisobutyl ether, ethylene glycol mono-t-butyl ether, ethylene glycol mono-2-methylpentyl ether, ethylene glycol dimethyl ether, ethylene glycol diethyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, Diethylene glycol mono-n-propyl ether, diethylene glycol mono-n-butyl ether, diethylene glycol monoisobutyl ether, diethylene glycol mono-n-hexyl ether, diethylene glycol monomethyl phenyl ether, diethylene glycol dimethyl ether, diethylene glycol divinyl ether, diethylene glycol ethyl vinyl ether, triethyl Glycol monomethyl ether, triethylene glycol monoethyl ether, triethylene glycol mono-n-butyl ether, triethylene glycol monovinyl ethyl ether, tetraethylene glycol monophenyl ether, tetraethylene glycol diethyl ether, polyethylene glycol methyl mono ether, propylene glycol monomethyl Ether, propylene glycol monoethyl ether, propylene glycol-n-monopropyl ether, propylene glycol monoisopropyl ether, propylene glycol mono-n-butyl ether, propylene glycol phenyl ether, propylene glycol monomethyl ether, propylene glycol dimethyl ether, propylene glycol diethyl ether, Professional Pyrene glycol-n-dipropyl ether, propylene glycol diisopropyl ether, propylene glycol di n-butyl ether, propylene glycol diisobutyl ether, propylene glycol diallyl ether, propylene glycol diphenyl ether, dipropylene glycol monoethyl ether, dipropylene glycol mono-n-butyl ether , Dipropylene glycol diethyl ether, and dipropylene glycol di n-butyl ether, dipropylene glycol diisobutyl ether, dipropylene glycol allyl ether, tripropylene glycol monomethyl ether, tripropylene glycol monoethyl ether, and tripropylene glycol mono-n-butyl ether It is.
グリコールエーテルとしてさらに好ましくは、エチレングリコールモノエーテル、プロピレングリコールモノエーテル、ジプロピレングリコールモノエーテルであり、具体的にはエチレングリコールモノメチルエーテル、エチレングリコールモノエチルエーテル、エチレングリコールモノプロピルエーテル、ジエチレングリコールモノメチルエーテル、ジエチレングリコールモノエチルエーテル、ジエチレングリコールモノプロピルエーテル、プロピレングリコールモノエチルエーテル、プロピレングリコールモノプロピルエーテル、ジプロピレングリコールモノエチルエーテル、ジプロピレングリコールモノプロピルエーテルである。 More preferably, the glycol ether is ethylene glycol monoether, propylene glycol monoether, dipropylene glycol monoether, specifically ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monopropyl ether, diethylene glycol monomethyl ether, Diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, propylene glycol monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol monoethyl ether, dipropylene glycol monopropyl ether.
本発明で用いるグリコールエーテルの配合量は、本発明の効果を奏すれば特に制限されず、皮膚への使用感や効果を考慮して適宜選択して用いることができるが、皮膚外用剤全体として、通常1〜60重量%、より好ましくは3〜50重量%、さらに好ましくは5〜40重量%、特に好ましくは5〜30重量%であれば良い。 The blending amount of the glycol ether used in the present invention is not particularly limited as long as the effects of the present invention are exhibited, and can be appropriately selected and used in consideration of the feeling of use and effects on the skin. Usually, 1 to 60% by weight, more preferably 3 to 50% by weight, still more preferably 5 to 40% by weight, and particularly preferably 5 to 30% by weight.
本発明の皮膚外用剤において、さらに炭化水素またはシリコーンを含有させると安定性が高くなるため、より好ましい。これらの炭化水素またはシリコーンは30℃で液状であるとさらに好ましい。
液状炭化水素としては、スクワラン、植物性スクワラン、スクワレン、流動パラフィン、流動イソパラフィン、軽質流動パラフィン、軽質イソパラフィン、軽質流動イソパラフィン、α―オレフィンオリゴマー、好ましくは、スクワラン、植物性スクワラン、流動パラフィン、軽質流動パラフィン等が挙げられる。
液状シリコーンとしては、ジフェニルポリシロキサン、メチルポリシロキサン、ジメチルポリシロキサン、アルキル変性ジメチルポリシロキサン、メチルフェニルポリシロキサン、メチルハイドロジェンポリシロキサン、トリメチルシロキシケイ酸、メチルシクロポリシロキサン、ステアロキシメチルポリシロキサン、セトキシメチルポリシロキサン、セチルジメチコン、セチルジメチコンコポリオール、ラウリルメチコンコポリオール、ステアリルジメチコンコポリオール等が挙げられ、好ましくは遊離の水酸基を有しないシリコーンであり、具体的にはジフェニルポリシロキサン、ジメチルポリシロキサン、アルキル変性ジメチルポリシロキサン、メチルフェニルポリシロキサン、メチルポリシロキサンである。
In the external preparation for skin of the present invention, it is more preferable to further contain a hydrocarbon or silicone, since the stability becomes high. More preferably, these hydrocarbons or silicones are liquid at 30 ° C.
Liquid hydrocarbons include squalane, vegetable squalane, squalene, liquid paraffin, liquid isoparaffin, light liquid paraffin, light isoparaffin, light liquid isoparaffin, α-olefin oligomer, preferably squalane, vegetable squalane, liquid paraffin, light fluid. Paraffin etc. are mentioned.
Liquid silicones include diphenylpolysiloxane, methylpolysiloxane, dimethylpolysiloxane, alkyl-modified dimethylpolysiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane, trimethylsiloxysilicic acid, methylcyclopolysiloxane, stearoxymethylpolysiloxane, Examples thereof include cetoxymethyl polysiloxane, cetyl dimethicone, cetyl dimethicone copolyol, lauryl methicone copolyol, stearyl dimethicone copolyol, and the like, preferably silicone having no free hydroxyl group, specifically diphenylpolysiloxane, dimethylpolysiloxane. Siloxane, alkyl-modified dimethylpolysiloxane, methylphenylpolysiloxane, and methylpolysiloxane.
本発明で用いる炭化水素またはシリコーンの配合量は、本発明の効果を奏すれば特に制限されないが、皮膚外用剤全体として通常0.1〜20重量%、好ましくは1〜15重量%、特に好ましくは3〜10重量%であれば良い。1重量%より少ないと安定化の効果が減少し、20重量%を超えても安定化効果は増大しないため好ましくない。 The blending amount of the hydrocarbon or silicone used in the present invention is not particularly limited as long as the effects of the present invention are exhibited, but is generally 0.1 to 20% by weight, preferably 1 to 15% by weight, particularly preferably as a whole skin external preparation. May be 3 to 10% by weight. If the amount is less than 1% by weight, the stabilizing effect decreases, and if it exceeds 20% by weight, the stabilizing effect does not increase, which is not preferable.
本発明の皮膚外用剤の調製方法は、特に制限されず、通常の皮膚外用剤を調製するのに必要な各種成分などを適宜選択、配合して、常法により調製することができる。また、本発明の皮膚外用剤の外皮への適用量や用法は特に制限されず、通常、一日数回、適量を皮膚等の外皮に塗布するなどして用いることができる。 The method for preparing the external preparation for skin of the present invention is not particularly limited, and can be prepared by a conventional method by appropriately selecting and blending various components necessary for preparing an ordinary external preparation for skin. Moreover, the application amount and usage of the external preparation for skin of the present invention to the outer skin are not particularly limited, and it can be used usually by applying an appropriate amount to the outer skin such as skin several times a day.
本発明の皮膚外用剤は、種々の形態に調製することができる。例えば、軟膏剤、クリーム剤、液剤(油状、ローション状、乳液状、エアゾール状を含む)、ゲル剤(液晶、マイクロエマルジョンを含む)、貼付剤(パック状を含む)、固形剤(スティック状を含む)などの剤型が挙げられ、特に液剤(ローション状、油状、乳液状を含む)、ゲル剤(液晶、マイクロエマルジョンを含む)に適用すると有用である。なかでも高温における製剤の安定化効果から、本発明の実施形態としては液晶、マイクロエマルジョンが特に好ましい。 The external preparation for skin of the present invention can be prepared in various forms. For example, ointments, creams, liquids (including oils, lotions, emulsions, aerosols), gels (including liquid crystals and microemulsions), patches (including packs), solids (sticks) And the like, and is particularly useful when applied to liquid agents (including lotions, oils, and emulsions) and gel agents (including liquid crystals and microemulsions). Among these, liquid crystal and microemulsion are particularly preferable as an embodiment of the present invention because of the effect of stabilizing the preparation at high temperature.
液晶とは、一般的に構成分子中に長い配向性を有する高度の結晶性を持ち、固体と液体の中間的な流動性および粘稠性のある液体であり、光学的異方性を示すことが多い。液晶は六方晶層やラメラ層を形成しており、この構造によって白色光では色づいた縞模様や偏光による屈折・反射が起こるため、顕微鏡下での複屈折や目視で液晶の形成を容易に識別することができる。
液晶は生体二重膜や細胞間脂質と構造が類似しているため、皮膚になじみやすく、また有用な成分の経皮吸収を促進できるという利点がある。
A liquid crystal is a liquid with a high degree of crystallinity, generally having a long orientation in the constituent molecules, a fluidity and viscosity that is intermediate between solid and liquid, and exhibits optical anisotropy. There are many. The liquid crystal forms a hexagonal layer and a lamellar layer, and this structure causes refraction and reflection due to colored stripes and polarized light in white light, so it is easy to identify birefringence under the microscope and visual observation of liquid crystal formation. can do.
Since liquid crystals are similar in structure to biological bilayer membranes and intercellular lipids, they have the advantage that they are easy to adapt to the skin and can promote percutaneous absorption of useful components.
マイクロエマルジョンとは、一般的に油−水−両親媒性物質からなる透明あるいは半透明な一液相で、膨潤した大きなミセルが分散した系であると定義され、本質的に可溶化系と同様であると言われている。マイクロエマルジョンの平均粒子径は、光学的透明性から0.5μm以下であると好ましい。
マイクロエマルジョンは、光学的な透明性を有するほど分散しているミセルが小さいため、通常のエマルジョンよりも製剤が角質層から皮膚に吸収されやすいという利点を持つ。
A microemulsion is generally defined as a transparent or translucent one-liquid phase consisting of an oil-water-amphiphile, and a system in which large swollen micelles are dispersed. It is said that. The average particle size of the microemulsion is preferably 0.5 μm or less from the viewpoint of optical transparency.
Microemulsions have the advantage that the formulation is more easily absorbed into the skin from the stratum corneum than normal emulsions because the micelles dispersed are small enough to have optical transparency.
本発明の皮膚外用剤が液晶型皮膚外用剤である場合、グリセリンまたはグリコールとグリコールエーテルの混合溶液に天然界面活性剤、水溶性化合物、少量の水などを投入・撹拌し、油分および油溶性化合物などを適宜投入・撹拌して調製することができる。また、本発明の液晶型皮膚外用剤は、少量の水を配合することができるが、水を別途配合せずに実質的に無水の製剤としても調製することができる。 When the skin external preparation of the present invention is a liquid crystal type skin external preparation, a natural surfactant, a water-soluble compound, a small amount of water, etc. are added to and stirred in a mixed solution of glycerin or glycol and glycol ether, and the oil and oil-soluble compound Or the like can be appropriately added and stirred. Moreover, although the liquid crystal type skin external preparation of this invention can mix | blend a small amount of water, it can prepare also as a substantially anhydrous formulation, without mix | blending water separately.
本発明の皮膚外用剤がマイクロエマルジョン型皮膚外用剤である場合、グリセリンまたはグリコールとグリコールエーテルの混合溶液に天然界面活性剤などを投入・撹拌し、油分および油溶性化合物などを適宜投入・撹拌した後、水溶性化合物、水を加えて高圧ホモミキサーを使用して乳化、調製することができる。 When the skin external preparation of the present invention is a microemulsion type skin external preparation, a natural surfactant or the like is added to and stirred in a mixed solution of glycerin or glycol and glycol ether, and an oil and an oil-soluble compound are appropriately added and stirred. Thereafter, a water-soluble compound and water can be added and emulsified and prepared using a high-pressure homomixer.
本発明の皮膚外用剤はさらに水を含有していてもよく、水分量は本発明の効果を奏すれば特に制限されないが、皮膚外用剤全体として通常0.001〜97重量%、好ましくは0.01〜95重量%、特に好ましくは0.1〜90重量%であれば良い。 The skin external preparation of the present invention may further contain water, and the amount of water is not particularly limited as long as the effect of the present invention is exerted, but is generally 0.001 to 97% by weight, preferably 0, as the whole skin external preparation. It may be 0.01 to 95% by weight, particularly preferably 0.1 to 90% by weight.
さらに、本発明の皮膚外用剤は、天然界面活性剤以外の界面活性剤を別途配合せずに、実質的に天然界面活性剤以外の界面活性剤を含有しない製剤としても調製することができる。 Furthermore, the external preparation for skin of the present invention can be prepared as a preparation substantially containing no surfactant other than the natural surfactant without separately adding a surfactant other than the natural surfactant.
本発明の皮膚外用剤は、医薬品又は医薬部外品、化粧品のいずれの範疇に属するものであってもよいため、様々な用途に用いることができる。本発明の皮膚外用剤の用途としては、例えば、湿疹、かぶれ、乾燥性そう痒症、乾皮症、しもやけ、あせも等痒みや炎症を治療するための皮膚炎治療剤又は鎮痒剤、切傷、擦傷、靴擦れ、かき傷、さし傷、火傷、化膿性創傷、痔、ひび、あかぎれ等の治療促進や悪化防止のための殺菌消毒剤や損傷治癒剤、水虫、ニキビ等を治療するための感染性皮膚疾患治療剤又は抗菌剤、口唇炎、口角炎、口唇のひびわれ、ただれなどを治療するための口唇用治療剤、手指のあれ、ひじ・ひざ・かかと・くるぶし等の角化症、さめ肌を治療するための角質軟化剤、消炎鎮痛剤などの医薬品、手荒れ、肌荒れ、唇の荒れ、日焼け後のほてり、しわ・たるみ、肌を整える、唇のきめを整える、皮膚・唇をすこやかに保つ、皮膚・唇にうるおいを与える、皮膚・唇を保護する、皮膚の乾燥・しもやけ・ひび・あかぎれ・かぶれ等の予防、腋臭抑制などに用いる医薬部外品、保湿、美白、角質軟化、クレンジングなどに用いる化粧品等が好適な用途として例示できるが、特にこれらに制限されない。 Since the external preparation for skin of the present invention may belong to any category of pharmaceuticals, quasi-drugs, and cosmetics, it can be used for various applications. Examples of the use of the external preparation for skin of the present invention include eczema, rash, dry pruritus, xerosis, moisturized skin, bruise and other dermatitis therapeutic agents or antipruritics, cuts, scratches, etc. Infectivity to treat antiseptics, wound healing agents, athlete's foot, acne, etc. to promote and prevent deterioration of shoes, scratches, scratches, scissors, burns, purulent wounds, wrinkles, cracks, scratches, etc. Treatment for skin diseases or antibacterial agents, cheilitis, keratitis, lip cracks, sores, etc. Treatment for lips, finger contact, keratosis such as elbows, knees, heels, and ankles, shark skin Drugs such as keratin softeners and anti-inflammatory analgesics to treat, rough hands, rough skin, rough lips, hot flashes after sunburn, wrinkles / sag, smooth skin, smooth lips, keep skin / lips smooth, Gives moisture to skin and lips, skin Examples of suitable applications include quasi-drugs used to protect skin, prevent dryness, frostiness, cracks, red spots, rashes, etc., odor control, etc., and cosmetics used for moisturizing, whitening, keratin softening, cleansing, etc. However, it is not particularly limited to these.
本発明の皮膚外用剤は、必要に応じて種々の成分(薬理活性成分や生理活性成分を含む)を組み合わせることができる。このような成分の種類は特に制限されず、例えば、ステロイド剤、局所麻酔剤、鎮痒剤、抗炎症剤、ビタミン剤、抗菌剤、抗ウイルス剤、角質軟化剤、鎮痛剤、保湿剤、美白剤、収斂剤、抗酸化剤、発毛抑制剤、抗シワ剤などが挙げられ、油溶性成分であるとより好ましい。
本発明において好適な成分としては例えば、次のような成分が例示できる。
The skin external preparation of the present invention can be combined with various components (including pharmacologically active components and physiologically active components) as necessary. The type of such ingredients is not particularly limited, and examples thereof include steroids, local anesthetics, antipruritics, anti-inflammatory agents, vitamins, antibacterial agents, antiviral agents, keratin softeners, analgesics, moisturizers, and whitening agents. Astringents, antioxidants, hair growth inhibitors, anti-wrinkle agents, and the like, and oil-soluble components are more preferred.
Examples of suitable components in the present invention include the following components.
ステロイド剤:吉草酸酢酸デキサメタゾン、デキサメタゾン、吉草酸酢酸プレドニゾロン、酪酸ヒドロコルチゾン、酢酸プレドニゾロン、プレドニゾロン、酢酸ヒドロコルチゾン、ヒドロコルチゾン、酢酸コルチゾン、ベタメタゾン、酪酸クロベタゾン、トリアムシノロンアセトニドなど。 Steroid agents: Dexamethasone acetate dexamethasone, dexamethasone acetate, prednisolone acetate valerate, hydrocortisone butyrate, prednisolone acetate, prednisolone acetate, hydrocortisone acetate, hydrocortisone, cortisone acetate, betamethasone, clobetasone butyrate, triamcinolone acetonide, etc.
局所麻酔剤:リドカイン、塩酸リドカイン、ジブカイン、塩酸ジブカイン、アミノ安息香酸エチル、ユーカリ油、オイゲノール、メントール、カンフル、ハッカ油など。 Local anesthetics: lidocaine, lidocaine hydrochloride, dibucaine, dibucaine hydrochloride, ethyl aminobenzoate, eucalyptus oil, eugenol, menthol, camphor, mint oil, etc.
鎮痒剤:クロタミトン、クロルフェニラミン、マレイン酸クロルフェニラミン、ジフェンヒドラミン、ノニル酸ワニリルアミド、サリチル酸、サリチル酸メチル、サリチル酸グリコール、カプサイシン、塩酸ジフェンヒドラミン、カンフル、チモール、メントール、オイゲノール、ヒノキチオール、ポリオキシエチレンラウリルエーテル、コンフリーエキス、シソエキス、セージエキス、ボタンピエキス、ボダイジュエキスなど。 Antipruritics: crotamiton, chlorpheniramine, chlorpheniramine maleate, diphenhydramine, nonylic acid vanillylamide, salicylic acid, methyl salicylate, glycolic salicylate, capsaicin, diphenhydramine hydrochloride, camphor, thymol, menthol, eugenol, hinokitiol, polyoxyethylene lauryl ether, Comfrey extract, perilla extract, sage extract, button pi extract, bodaiju extract, etc.
抗炎症剤:アラントイン又はその誘導体、インドメタシン、イブプロフェン、イブプロフェンピコノール、ブフェキサマク、フルフェナム酸ブチル、ベンダザック、ピロキシカム、ケトプロフェン、フェルビナク、サリチル酸メチル又はサリチル酸グリコール等のサリチル酸誘導体など。 Anti-inflammatory agents: Allantoin or derivatives thereof, salicylic acid derivatives such as indomethacin, ibuprofen, ibuprofen piconol, bufexamac, flufenamic acid butyl, bendazac, piroxicam, ketoprofen, felbinac, methyl salicylate or glycol salicylate.
ビタミン剤:レチノール、酢酸レチノール等のレチノール誘導体(ビタミンA類)、レチナール、レチノイン酸、レチノイン酸メチル、レチノイン酸エチル、レチノイン酸レチノール、ビタミンA油、ビタミンA脂肪酸エステル等のビタミンA類、β−カロチン、α−カロチン、γ−カロチン、δ−カロチン、リコピン、ゼアキサンチン、クリプトキサンチン、エキネノン等のプロビタミンA類、コハク酸dl−α−トコフェロール、コハク酸dl−α−トコフェロールカルシウム等のビタミンE類、リボフラビン、フラビンモノヌクレオチド、フラビンアデニンジヌクレオチド、リボフラビン酪酸エステル、リボフラビンテトラ酪酸エステル、リボフラビン5’−リン酸エステルナトリウム、リボフラビンテトラニコチン酸エステル等のビタミンB2類、ニコチン酸メチル等のニコチン酸類、アスコルビン酸ステアリン酸エステル、ジパルミチン酸L−アスコルビルなどのビタミンC類、メチルヘスペリジン、エルゴカルシフェロール、コレカルシフェロールなどのビタミンD類、フィロキノン、ファルノキノン等のビタミンK類、γ−オリザノール、ジベンゾイルチアミン、ジベンゾイルチアミン塩酸塩、チアミン塩酸塩、チアミンセチル塩酸塩、チアミンチオシアン酸塩、チアミンラウリル塩酸塩、チアミン硝酸塩、チアミンモノリン酸塩、チアミンリジン塩、チアミントリリン酸塩、チアミンモノリン酸エステルリン酸塩、チアミンモノリン酸エステル、チアミンジリン酸エステル、チアミンジリン酸エステル塩酸塩、チアミントリリン酸エステル、チアミントリリン酸エステルモノリン酸塩等のビタミンB1類、塩酸ピリドキシン、酢酸ピリドキシン、塩酸ピリドキサール、5’−リン酸ピリドキサール、塩酸ピリドキサミン等のビタミンB6類、シアノコバラミン、ヒドロキソコバラミン、デオキシアデノシルコバラミン等のビタミンB12類、葉酸、プテロイルグルタミン酸等の葉酸類、ニコチン酸、ニコチン酸アミドなどのニコチン酸類、パントテン酸、パントテン酸カルシウム、パントテニルアルコール(パンテノール)、D−パンテサイン、D−パンテチン、補酵素A、パントテニルエチルエーテル等のパントテン酸類、ビオチン、ビオチシン等のビオチン類、アスコルビン酸、アスコルビン酸ナトリウム、デヒドロアスコルビン酸、アスコルビン酸リン酸エステルナトリウム、アスコルビン酸リン酸エステルマグネシウム等のアスコルビン酸誘導体であるビタミンC類、そのほか、カルニチン、フェルラ酸、α−リポ酸、オロット酸等のビタミン様作用因子など。 Vitamin preparations: Retinol derivatives such as retinol and retinol acetate (vitamins A), retinal, retinoic acid, methyl retinoic acid, ethyl retinoic acid, retinoic acid retinol, vitamin A oil, vitamin A fatty acid ester, etc., β- Provitamin A such as carotene, α-carotene, γ-carotene, δ-carotene, lycopene, zeaxanthin, cryptoxanthine, echinenone, vitamin E such as dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate , Such as riboflavin, flavin mononucleotide, flavin adenine dinucleotide, riboflavin butyrate, riboflavin tetrabutyrate, sodium riboflavin 5'-phosphate, riboflavin tetranicotinate B2, nicotinic acids such as methyl nicotinate, ascorbic acid stearate, vitamin C such as L-ascorbyl dipalmitate, vitamin Ds such as methyl hesperidin, ergocalciferol, cholecalciferol, phylloquinone, farnoquinone, etc. Vitamin Ks, γ-oryzanol, dibenzoyl thiamine, dibenzoyl thiamine hydrochloride, thiamine hydrochloride, thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine Triphosphate, thiamine monophosphate, thiamine monophosphate, thiamine diphosphate, thiamine diphosphate hydrochloride, thiamine triphosphate, thiamine triphosphate Vitamin B1 such as monophosphate, vitamin B6 such as pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, 5'-phosphate pyridoxal, pyridoxamine hydrochloride, vitamin B12 such as cyanocobalamin, hydroxocobalamin, deoxyadenosylcobalamin, folic acid, Folates such as pteroylglutamic acid, nicotinic acids such as nicotinic acid and nicotinamide, pantothenic acid, calcium pantothenate, pantothenyl alcohol (panthenol), D-panthecin, D-panthetin, coenzyme A, pantothenylethyl Pantothenic acids such as ether, biotins such as biotin and biotin, ascorbic acid, sodium ascorbate, dehydroascorbic acid, sodium ascorbate phosphate ester, ascorbate phosphate ester Vitamin C is ascorbic acid derivatives such as Le magnesium, other, carnitine, ferulic acid, alpha-lipoic acid, and vitamin-like agents such as orotic acid.
抗菌剤:イソプロピルメチルフェノール、グルコン酸クロルヘキシジン、塩酸クロルヘキシジン、塩化ベンザルコニウム、塩化ベンゼトニウム、臭化セチルトリメチルアンモニウム、塩化デカリニウム、トリクロサン、トリクロロカルバニリドなど。
抗ウイルス剤:アシクロビル、ペンシクロビルなど。
Antibacterial agents: isopropylmethylphenol, chlorhexidine gluconate, chlorhexidine hydrochloride, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium bromide, decalinium chloride, triclosan, trichlorocarbanilide and the like.
Antiviral agents: acyclovir, penciclovir, etc.
角質軟化剤:エチルアルコール、イソプロピルアルコール、プロパノール、ブタノール、ポリエチレングリコール、ベンジルアルコール、フェニルエチルアルコール、炭酸プロピレン、ヘキシルドデカノール、アラントイン、ジメチルスルホキシド、ジメチルアセトアミド、ジメチルホルムアミド、トリエタノールアミン、ジイソプロピルアジペート、エチルラウリレート、ラノリン、脂肪酸ジアルキロールアミド、サリチル酸、サリチル酸誘導体、尿素、イオウ、レゾルシン、グリコール酸、フィチン酸、乳酸、乳酸塩、水酸化ナトリウム、水酸化カリウムなど。 Keratin softener: ethyl alcohol, isopropyl alcohol, propanol, butanol, polyethylene glycol, benzyl alcohol, phenylethyl alcohol, propylene carbonate, hexyl decanol, allantoin, dimethyl sulfoxide, dimethylacetamide, dimethylformamide, triethanolamine, diisopropyl adipate, ethyl Laurylate, lanolin, fatty acid dialkyrolamide, salicylic acid, salicylic acid derivative, urea, sulfur, resorcin, glycolic acid, phytic acid, lactic acid, lactate, sodium hydroxide, potassium hydroxide and the like.
鎮痛剤:メフェナム酸、フルフェナム酸、インドメタシン、サリチル酸メチル、サリチル酸グリコール、ジクロフェナク、ジクロフェナクナトリウム、フェルビナク、アルクロフェナク、ブフェキサマク、アスピリン、アセトアミノフェン、イブプロフェン、ケトプロフェン、プラノプロフェン、フェノプロフェン、フェングロフェン、フルルビプロフェン、ザルトプロフェン、ナプロキセン、フルビプロフェン、フルルビプロフェンアキセチル、フェンブフェン、リシプフェン、ピロキシカム、アンピロキシカム、テノキシカム、オキシフェンブタゾン、フェニルブタゾン、クロフェゾン、スリンダック、クリンダック、ベンザダック、L−メントール、カンファー、スルピリン、塩酸チアラミド、オルセノン、フェンチアザック、ベンタゾシン、メピリゾールなど。 Painkillers: mefenamic acid, flufenamic acid, indomethacin, methyl salicylate, glycol salicylate, diclofenac, diclofenac sodium, felbinac, alclofenac, bufexamac, aspirin, acetaminophen, ibuprofen, ketoprofen, pranoprofen, fenoprofen, fenglofen, Flurbiprofen, zaltoprofen, naproxen, flurbiprofen, flurbiprofen axetil, fenbufen, ricipfen, piroxicam, ampiroxicam, tenoxicam, oxyphenbutazone, phenylbutazone, clofesone, sulindac, clindac, benzaduck, L -Menthol, camphor, sulpyrine, thiaramide hydrochloride, orsenone, fenthiazac, benta Shin, such as Mepirizoru.
保湿剤:ポリエチレングリコール、ジグリセリントレハロース、ヒアルロン酸ナトリウム、ヘパリン類似物質、コンドロイチン硫酸ナトリウム、コラーゲン、エラスチン、ケラチン、キチン、キトサンなどの高分子化合物、グリシン、アスパラギン酸、アルギニン等のアミノ酸、乳酸ナトリウム、尿素、ピロリドンカルボン酸ナトリウム等の天然保湿因子、カミツレエキス、アロエエキス、アロエベラエキス、ハマメリスエキス、ローズマリーエキス、タイムエキス、チャエキス、シソエキスなどの植物抽出エキスなど。 Moisturizer: polyethylene glycol, diglycerin trehalose, sodium hyaluronate, heparin analog, chondroitin sulfate sodium, collagen, elastin, keratin, chitin, chitosan and other high molecular compounds, glycine, aspartic acid, arginine and other amino acids, sodium lactate, Natural moisturizing factors such as urea and sodium pyrrolidonecarboxylate, plant extract extracts such as chamomile extract, aloe extract, aloe vera extract, hamamelis extract, rosemary extract, thyme extract, tea extract and perilla extract.
美白剤:ビタミンA又はその誘導体、ビタミンC又はその誘導体、ビタミンE又はその誘導体、パントテン酸又はその誘導体等のビタミン類、プラセンタ;アルブチン;コウジ酸;システイン;フィチン酸;イリス(アイリス)、アーモンド、アロエ、イチョウ、ウーロン茶、エイジツ、オウゴン、オウレン、オトギリソウ、オドリコソウ、海藻、カッコン、カンゾウ、クチナシ、クジン、コムギ、コメ、コメハイガ、オリザノール、コメヌカ、シソ、シャクヤク、センキュウ、ソウハクヒ、ダイズ、茶、トウキ、トウキンセンカ、ハマメリス、ベニバナ、ボタンピ、ヨクイニン、トウキ、エノキ、カキ(Diospyros kaki)、チョウジ等の植物に由来する成分、エキス及び精油など。 Whitening agents: vitamins A or derivatives thereof, vitamins C or derivatives thereof, vitamins E or derivatives thereof, vitamins such as pantothenic acid or derivatives thereof, placenta; arbutin; kojic acid; cysteine; phytic acid; iris (iris), almond, Aloe, Ginkgo, Oolong tea, Ages, Ogon, Ouren, Hypericum, Olysam, Seaweed, Cascon, Licorice, Gardenia, Kujin, Wheat, Rice, Rice haiga, Oryzanol, Rice bran, Perilla, Peonies, Senkyu, Sakuhachi, Saki, Tea, Soy Ingredients, extracts and essential oils derived from plants such as eucalyptus, hamamelis, safflower, button pi, yokuinin, touki, enoki, oyster (Diospyros kaki), clove.
収斂剤:クエン酸、酒石酸、乳酸、塩化アルミニウム、硫酸アルミニウム、アラントインクロルヒドロキシアルミニウム、アラントインジヒドロキシアルミニウム、アルミニウムフェノールスルホン酸、パラフェノールスルホン酸亜鉛、硫酸亜鉛、乳酸亜鉛、アルミニウムクロロヒドロオキシドなど。
抗酸化剤:ジブチルヒドロキシトルエン、ブチルヒドロキシアニソール、アスコルビン酸、エリソルビン酸、dl−α−トコフェロール、エチレンジアミン四酢酸二ナトリウム・二水和物(以下、エデト酸ナトリウムとも言う)、ソルビン酸、亜硫酸ナトリウム、L−システイン塩酸塩など。
Astringent: citric acid, tartaric acid, lactic acid, aluminum chloride, aluminum sulfate, allantoinchlorohydroxyaluminum, allantoindihydroxyaluminum, aluminum phenolsulfonic acid, zinc paraphenolsulfonic acid, zinc sulfate, zinc lactate, aluminum chlorohydroxide and the like.
Antioxidants: dibutylhydroxytoluene, butylhydroxyanisole, ascorbic acid, erythorbic acid, dl-α-tocopherol, disodium ethylenediaminetetraacetate dihydrate (hereinafter also referred to as sodium edetate), sorbic acid, sodium sulfite, L-cysteine hydrochloride and the like.
発毛抑制剤:イソフラボン、ヒオウギエキス、ドクダミエキス、イリス根エキス、パパイン酵素など。
抗シワ剤:ビタミンA及びその誘導体、グリコール酸、アシル化グルコサミン、カイネチン、ビタミンC、ビタミンE、アロエ、コラーゲン、ヒアルロン酸、トリペプチド、海藻エキス、マロニエエキス、ローズマリーエキス、ヤグルマソウエキスなど。
Hair growth inhibitor: isoflavone, cypress extract, docami extract, iris root extract, papain enzyme, etc.
Anti-wrinkle agent: Vitamin A and its derivatives, glycolic acid, acylated glucosamine, kinetin, vitamin C, vitamin E, aloe, collagen, hyaluronic acid, tripeptide, seaweed extract, maronier extract, rosemary extract, cornflower extract and the like.
これらの成分は1種または2種以上を組み合わせて用いることができる。またそれらの配合量は、本発明の効果を奏すれば特に制限されないが、望ましくは薬事法上許容される上限配合量を限度に適宜選択使用することができる。具体的には、皮膚外用剤100重量部あたり通常0.001〜20重量部、好ましくは0.001〜10重量部、より好ましくは0.001〜5重量部の範囲から目的に応じて調製することができる。 These components can be used alone or in combination of two or more. Moreover, those compounding amounts are not particularly limited as long as the effects of the present invention are obtained, but can be suitably selected and used as long as the upper limit compounding amount allowed by the Pharmaceutical Affairs Law is desirable. Specifically, it is prepared according to the purpose from the range of usually 0.001 to 20 parts by weight, preferably 0.001 to 10 parts by weight, more preferably 0.001 to 5 parts by weight per 100 parts by weight of the external preparation for skin. be able to.
本発明の皮膚外用剤は、保存安定性や粘度等の品質を損なわず、また本発明の効果を損なわない量的及び質的範囲内で、必要に応じて医薬品、医薬部外品または化粧品分野において一般的に用いられる各種の成分、例えば基剤、界面活性剤、増粘剤、保存剤、pH調整剤、安定化剤、刺激軽減剤、防腐剤、着色剤、分散剤、香料等を配合することができる。なお、これらの成分は1種単独で、または2種以上を任意に組み合わせて配合することができる。 The external preparation for skin of the present invention does not impair quality such as storage stability and viscosity, and within the quantitative and qualitative range that does not impair the effects of the present invention, as necessary, in the pharmaceutical, quasi-drug or cosmetic field. Ingredients commonly used in the formulation, such as bases, surfactants, thickeners, preservatives, pH adjusters, stabilizers, irritation reducers, preservatives, colorants, dispersants, fragrances, etc. can do. In addition, these components can be mix | blended individually by 1 type or in combination of 2 or more types.
基剤:パラフィン、ゲル化炭化水素、オゾケライト、セレシン、ワセリン、ハードファット、マイクロクリスタリンワックス等の炭化水素、ラウリン酸、ミリスチン酸、パルミチン酸、ステアリン酸、ベヘニン酸、イソステアリン酸、オレイン酸、リノール酸等の脂肪酸、高重合メチルポリシロキサン、ジメチルシロキサン・メチル(ポリオキシエチレン)シロキサン・メチル(ポリオキシプロピレン)シロキサン共重合体、ジメチルシロキサン・メチル(ポリオキシエチレン)シロキサン共重合体、ジメチルシロキサン・メチル(ポリオキシプロピレン)シロキサン共重合体、ポリオキシエチレン・メチルポリシロキサン共重合体、ポリ(オキシエチレン・オキシプロピレン)・メチルポリシロキサン共重合体、ジメチルシロキサン・メチルセチルオキシシロキサン共重合体、ジメチルシロキサン・メチルステアロキシシロキサン共重合体、アクリル酸アルキル共重合体メチルポリシロキサンエステル、架橋型メチルポリシロキサン、架橋型メチルフェニルポリシロキサン、架橋型ポリエーテル変性シリコーン、架橋型アルキルポリエーテル変性シリコーン、架橋型アルキル変性シリコーン等の重合型シリコーン、エチレングリコールモノアセタート、エチレングリコールジアセタート、トリエチレングリコールジアセタート、ヘキシレングリコールジアセタート、及び2-メチル-2-プロペン-1,1-ジオールジアセタート等のグリコールアセタート、トリエチレングリコールジバレラート、2,2,4-トリメチル-1,3-ペンタンジオールモノイソブチラート、2,2,4-トリメチル-1,3-ペンタンジオールジイソブチラート等のグリコールエステル、エチレングリコールジアクリラート、ジエチレングリコールジアクリラート、プロピレングリコールモノアクリラート、2,2-ジメチル-トリメチレングリコールジアクリラート、及び1,3-ブチレングリコールジアクリラート等のグリコールアクリラート、エチレングリコールジニトラート、ジエチレングリコールジニトラート、トリエチレングリコールジニトラート、及びプロピレングリコールジニトラート等のグリコールジニトラート、2,2′-[1,4-フェニレンジオキシ]ジエタノール、ジオキサン、ブチレングリコールアジピン酸ポリエステルなど。 Base: hydrocarbons such as paraffin, gelled hydrocarbon, ozokerite, ceresin, petrolatum, hard fat, microcrystalline wax, lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, isostearic acid, oleic acid, linoleic acid Fatty acids such as, highly polymerized methylpolysiloxane, dimethylsiloxane methyl (polyoxyethylene) siloxane methyl (polyoxypropylene) siloxane copolymer, dimethylsiloxane methyl (polyoxyethylene) siloxane copolymer, dimethylsiloxane methyl (Polyoxypropylene) siloxane copolymer, polyoxyethylene / methylpolysiloxane copolymer, poly (oxyethylene / oxypropylene) / methylpolysiloxane copolymer, dimethylsiloxane / methyl Cetyloxysiloxane copolymer, dimethylsiloxane / methylstearoxysiloxane copolymer, alkyl acrylate copolymer methylpolysiloxane ester, crosslinked methylpolysiloxane, crosslinked methylphenylpolysiloxane, crosslinked polyether-modified silicone, crosslinked Type alkyl polyether-modified silicone, polymerization type silicone such as cross-linked alkyl-modified silicone, ethylene glycol monoacetate, ethylene glycol diacetate, triethylene glycol diacetate, hexylene glycol diacetate, and 2-methyl-2 -Glycol acetates such as propene-1,1-diol diacetate, triethylene glycol divalerate, 2,2,4-trimethyl-1,3-pentanediol monoisobutyrate, 2,2,4-trimethyl 1,3-pentanediol Glycol esters such as diisobutyrate, ethylene glycol diacrylate, diethylene glycol diacrylate, propylene glycol monoacrylate, 2,2-dimethyl-trimethylene glycol diacrylate, and 1,3-butylene glycol diacrylate Glycol dinitrates such as glycol acrylate, ethylene glycol dinitrate, diethylene glycol dinitrate, triethylene glycol dinitrate, and propylene glycol dinitrate, 2,2 '-[1,4-phenylenedioxy] diethanol, dioxane, butylene glycol Adipic acid polyester and so on.
界面活性剤:ソルビタンモノイソステアレート、ソルビタンモノラウレート、ソルビタンモノパルミテート、ソルビタンモノステアレート、ペンタ−2−エチルヘキシル酸ジグリセロールソルビタン、テトラ−2−エチルヘキシル酸ジグリセロールソルビタン等のソルビタン脂肪酸エステル類、モノステアリン酸グリセリル、モノステアリン酸グリセリンリンゴ酸等のグリセリン脂肪酸類、モノイソステアリン酸ポリグリセリル、ジイソステアリン酸ポリグリセリル等のポリグリセリン脂肪酸類、モノステアリン酸プロピレングリコール等のプロピレングリコール脂肪酸エステル類、ポリオキシエチレン硬化ヒマシ油40、ポリオキシエチレン硬化ヒマシ油60、ポリオキシエチレン硬化ヒマシ油80などの硬化ヒマシ油誘導体、モノラウリル酸ポリオキシエチレン(20)ソルビタン(ポリソルベート20)、モノステアリン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート60)、モノオレイン酸ポリオキシエチレン(20)ソルビタン(ポリソルベート80)などのポリオキシエチレンソルビタン脂肪酸エステル類、ポリオキシエチレンモノヤシ油脂肪酸グリセリル、グリセリンアルキルエーテル、アルキルグルコシド、ポリオキシエチレンセチルエーテルなど。 Surfactants: Sorbitan fatty acid esters such as sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexylate, diglycerol sorbitan tetra-2-ethylhexylate Glyceryl fatty acids such as glyceryl monostearate and glyceryl monostearate malic acid, polyglyceryl fatty acids such as polyglyceryl monoisostearate and polyglyceryl diisostearate, propylene glycol fatty acid esters such as propylene glycol monostearate, polyoxyethylene cured Hardened castor oil derivatives such as castor oil 40, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene hydrogenated castor oil 80, monolauri Polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene (20) sorbitan (polysorbate 20), polyoxyethylene (20) sorbitan monostearate (polysorbate 60), polyoxyethylene (20) sorbitan monooleate (polysorbate 80) , Polyoxyethylene monococonut oil fatty acid glyceryl, glycerin alkyl ether, alkyl glucoside, polyoxyethylene cetyl ether and the like.
増粘剤:グアーガム、ローカストビーンガム、カラギーナン、キサンタンガム、デキストラン、メチルセルロース、エチルセルロース、カルボキシメチルセルロース、ヒドロキシエチルセルロース、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、アルギン酸ナトリウム、アルギン酸プロピレングリコールエステル、ポリビニルアルコール、ポリビニルピロリドン、ポリビニルメチルエーテル、カルボキシビニルポリマー、アクリル酸メタクリル酸アルキル共重合体、ポリアクリル酸ナトリウム、ポリエチレングリコール、ベントナイト、デキストリン脂肪酸エステル、ペクチンなど。 Thickener: Guar gum, locust bean gum, carrageenan, xanthan gum, dextran, methylcellulose, ethylcellulose, carboxymethylcellulose, hydroxyethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, sodium alginate, propylene glycol alginate, polyvinyl alcohol, polyvinylpyrrolidone , Polyvinyl methyl ether, carboxyvinyl polymer, alkyl methacrylate copolymer, sodium polyacrylate, polyethylene glycol, bentonite, dextrin fatty acid ester, pectin and the like.
保存剤:安息香酸、安息香酸ナトリウム、デヒドロ酢酸、デヒドロ酢酸ナトリウム、パラオキシ安息香酸イソブチル、パラオキシ安息香酸イソプロピル、パラオキシ安息香酸ブチル、パラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、パラオキシ安息香酸ベンジル、パラオキシ安息香酸メチル、フェノキシエタノールなど。 Preservatives: Benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, benzyl paraoxybenzoate, paraoxybenzoic acid Methyl, phenoxyethanol, etc.
pH調整剤:無機酸(塩酸、硫酸、リン酸、ポリリン酸、ホウ酸など)、有機酸(乳酸、酢酸、クエン酸、酒石酸、リンゴ酸、コハク酸、コハク酸ナトリウム、シュウ酸、グルコン酸、フマル酸、プロピオン酸、酢酸、アスパラギン酸、イプシロン−アミノカプロン酸、グルタミン酸、アミノエチルスルホン酸など)、グルコノラクトン、酢酸アンモニウム、無機塩基(炭酸水素ナトリウム、炭酸ナトリウム、水酸化カリウム、水酸化ナトリウム、水酸化カルシウム、水酸化マグネシウムなど)、有機塩基(モノエタノールアミン、トリエタノールアミン、ジイソプロパノールアミン、トリイソプロパノールアミン、リジンなど)など。 pH adjusters: inorganic acids (hydrochloric acid, sulfuric acid, phosphoric acid, polyphosphoric acid, boric acid, etc.), organic acids (lactic acid, acetic acid, citric acid, tartaric acid, malic acid, succinic acid, sodium succinate, oxalic acid, gluconic acid, Fumaric acid, propionic acid, acetic acid, aspartic acid, epsilon-aminocaproic acid, glutamic acid, aminoethylsulfonic acid, etc.), gluconolactone, ammonium acetate, inorganic base (sodium bicarbonate, sodium carbonate, potassium hydroxide, sodium hydroxide, Calcium hydroxide, magnesium hydroxide, etc.), organic bases (monoethanolamine, triethanolamine, diisopropanolamine, triisopropanolamine, lysine, etc.).
これらの成分は1種または2種以上を組み合わせて用いることができる。またそれらの配合量は、本発明の効果を奏すれば特に制限されないが、望ましくは薬事法上許容される上限配合量を限度に適宜選択使用することができる。具体的には、皮膚外用剤100重量部あたり通常0.001〜20重量部、好ましくは0.
001〜10重量部、より好ましくは0.001〜5重量部の範囲から目的に応じて調製することができる。
These components can be used alone or in combination of two or more. Moreover, those compounding amounts are not particularly limited as long as the effects of the present invention are obtained, but can be suitably selected and used as long as the upper limit compounding amount allowed by the Pharmaceutical Affairs Law is desirable. Specifically, the amount is usually 0.001 to 20 parts by weight, preferably 0.
It can be prepared according to the purpose from the range of 001 to 10 parts by weight, more preferably 0.001 to 5 parts by weight.
さらに本発明は、皮膚外用剤の安定性を向上させる方法をも包含する。本発明の方法において、天然界面活性剤、グリコールまたはグリセリン、および液状油を含有する皮膚外用剤の安定化は、グリコールエーテルをも配合することによって達成できる。
本発明の方法において、天然界面活性剤、グリコール、グリセリン、グリコールエーテル、およびこれらの配合量、配合比については、前記皮膚外用剤で用いたものと同様である。
本発明の方法において、液状油とは30℃で液状である油であれば特に限定されず、例えば液状エステル油、液状炭化水素、液状シリコンなどが挙げられる。液状エステル油、液状炭化水素、液状シリコンおよびこれらの配合量、配合比については、前記皮膚外用剤で用いたものと同様である。
本方法を使用して得られた組成物は、その製剤形態に応じて、1日あたり1回から数回に分けて、公知あるいは慣用されている方法にて用法・用量にて使用することができる。
Furthermore, this invention also includes the method of improving the stability of a skin external preparation. In the method of the present invention, stabilization of a skin external preparation containing a natural surfactant, glycol or glycerin, and liquid oil can be achieved by blending with glycol ether.
In the method of the present invention, the natural surfactant, glycol, glycerin, glycol ether, and the blending amount and blending ratio thereof are the same as those used in the external preparation for skin.
In the method of the present invention, the liquid oil is not particularly limited as long as it is liquid at 30 ° C., and examples thereof include liquid ester oil, liquid hydrocarbon, and liquid silicon. About liquid ester oil, liquid hydrocarbon, liquid silicon, and these compounding quantity and compounding ratio, it is the same as that used with the said skin external preparation.
The composition obtained by using this method can be used in a dosage or administration by a known or commonly used method, divided into 1 to several times per day according to the formulation form. it can.
以下に実施例を挙げて本発明を具体的に説明するが、これらの実施例は何ら本発明の範囲を限定するものではない。なお、配合量等は精製水または特に単位の記載のないものについては、すべて重量%を表す。 EXAMPLES The present invention will be specifically described below with reference to examples, but these examples do not limit the scope of the present invention. In addition, a compounding quantity etc. represent weight% altogether about purified water or a thing without the description of a unit.
試験例 製剤安定性
表1、2に示す処方に従い、グリセリンおよびエトキシジグリコールの混合溶液中にレシチンを投入して十分撹拌した後、油分を加えて調製した製剤について、調製直後の相状態および湿度75%、40℃の恒温室に1ヶ月保存した後の外観変化を評価した。
結果を表1、2に示す。
Test example Preparation stability According to the formulations shown in Tables 1 and 2, for the preparation prepared by adding lecithin into a mixed solution of glycerin and ethoxydiglycol and thoroughly stirring, and then adding oil, the phase state and humidity immediately after preparation Appearance change after 1 month storage in a constant temperature room of 75% and 40 ° C. was evaluated.
The results are shown in Tables 1 and 2.
比較例1〜3から、エトキシジグリコールなしでは、ともに製剤を安定に保つことができないことがわかった。一方、実施例1〜4は、いずれも安定性の高いことが確認された。 From Comparative Examples 1 to 3, it was found that both the preparations could not be kept stable without ethoxydiglycol. On the other hand, it was confirmed that Examples 1-4 were all highly stable.
実施例5〜11では、液晶、乳化、均一透明のいずれの製剤も高温安定性が良好であることが示されている。また、実施例7では配合する液状エステル油量が製剤全体の35重量%と高くなっていても液晶を保持しており、本発明の有用性の高さを示している。さらに実施例10はマイクロエマルジョンを形成しており、液状エステル油含量が高い状態で高温安定性が維持できている。 In Examples 5 to 11, it is shown that any liquid crystal, emulsified, and uniformly transparent preparation has good high-temperature stability. Further, in Example 7, the liquid crystal was retained even when the amount of liquid ester oil to be blended was as high as 35% by weight of the whole preparation, indicating the high usefulness of the present invention. Further, Example 10 forms a microemulsion, and the high temperature stability can be maintained with a high liquid ester oil content.
表1、2の実施例1〜10は液晶またはマイクロエマルジョンを形成しつつ、高温で安定であるため、これらの製剤が本来有している皮膚へのなじみやすさ、経皮吸収の促進などの機能から、上記実施例にさらに油溶性有用成分を加えることで、有用成分の肌への効率的な浸透を期待することができる。中でも、上記実施例中に配合しているテトラ2−ヘキシルデカン酸アスコルビルは、生体内で活性体のアスコルビン酸に変化することが知られている油溶性有用成分の一つであり、本実施例をそのまま使用しても薬理効果を十分に期待することができることから、特に有用である。 Examples 1 to 10 in Tables 1 and 2 are stable at high temperatures while forming liquid crystals or microemulsions, so that these preparations are inherently compatible with the skin and promote percutaneous absorption. From the functions, it is possible to expect efficient penetration of the useful components into the skin by adding the oil-soluble useful components to the above examples. Among them, ascorbyl tetra-2-hexyldecanoate blended in the above examples is one of the oil-soluble useful components known to change into active ascorbic acid in vivo. Even if it is used as it is, it is particularly useful because a pharmacological effect can be sufficiently expected.
以下に製剤実施例を挙げる。なお、以下の実施例中の配合量は、精製水または特に単位の記載のないものについてはすべて重量%を表す。 The formulation examples are given below. In addition, the compounding quantity in a following example represents weight% altogether about purified water or the thing without the description of a unit especially.
実施例12 白色水溶性ゲル
水素添加大豆レシチン 0.5
グリチルリチン酸二カリウム 0.1
グリセリン 10.0
エトキシジグリコール 7.0
ジカプリン酸プロピレングリコール 1.0
2−エチルヘキサン酸セチル 1.0
メチルフェニルポリシロキサン 3.0
スクワラン 1.0
酢酸トコフェロール 0.5
アラントイン 0.1
ポリオキシエチレン硬化ヒマシ油60 0.5
ヒドロキシエチルセルロース 0.2
アクリル酸・メタクリル酸アルキル共重合体 0.4
トリエタノールアミン 0.25
エデト酸ナトリウム 0.05
精製水 残量
100%
Example 12 White water-soluble gel Hydrogenated soybean lecithin 0.5
Dipotassium glycyrrhizinate 0.1
Glycerin 10.0
Ethoxydiglycol 7.0
Propylene glycol dicaprate 1.0
Cetyl 2-ethylhexanoate 1.0
Methylphenylpolysiloxane 3.0
Squalane 1.0
Tocopherol acetate 0.5
Allantoin 0.1
Polyoxyethylene hydrogenated castor oil 60 0.5
Hydroxyethyl cellulose 0.2
Acrylic acid / alkyl methacrylate copolymer 0.4
Triethanolamine 0.25
Sodium edetate 0.05
Purified water remaining
100%
実施例13 透明水溶性ゲル
卵黄レシチン 0.2
グリセリン 15.0
エトキシジグリコール 8.0
ジカプリル酸プロピレングリコール 0.1
アロエベラエキス 1.0
カミツレエキス 0.5
無水エタノール 8.0
ポリオキシエチレン硬化ヒマシ油40 4.0
トリエタノールアミン 0.75
カルボキシビニルポリマー 0.5
キサンタンガム 0.5
アルギン酸ナトリウム 0.3
エデト酸ナトリウム 0.05
精製水 残量
100%
Example 13 Transparent water-soluble gel egg yolk lecithin 0.2
Glycerin 15.0
Ethoxydiglycol 8.0
Propylene glycol dicaprylate 0.1
Aloe vera extract 1.0
Chamomile extract 0.5
Absolute ethanol 8.0
Polyoxyethylene hydrogenated castor oil 40 4.0
Triethanolamine 0.75
Carboxyvinyl polymer 0.5
Xanthan gum 0.5
Sodium alginate 0.3
Sodium edetate 0.05
Purified water remaining
100%
実施例14 ローション
ヒアルロン酸ナトリウム 0.02
グリセリン 20.0
1,3‐ブチレングリコール 5.0
エトキシジグリコール 5.0
トリ2−エチルヘキサン酸トリメチロールプロパン 0.01
ポリオキシエチレン硬化ヒマシ油80 0.6
ポリエチレングリコール1500 0.5
コハク酸 0.4
コラーゲン加水分解物 0.1
コハク酸ナトリウム 0.06
精製水 残量
100%
Example 14 Lotion Sodium Hyaluronate 0.02
Glycerin 20.0
1,3-butylene glycol 5.0
Ethoxydiglycol 5.0
Trimethylolpropane tri-2-ethylhexanoate 0.01
Polyoxyethylene hydrogenated castor oil 80 0.6
Polyethylene glycol 1500 0.5
Succinic acid 0.4
Collagen hydrolyzate 0.1
Sodium succinate 0.06
Purified water remaining
100%
実施例15 クレンジング
水素添加レシチン 0.5
テトラ2−エチルヘキサン酸ペンタエリスリトール 5.0
トリ(カプリル・カプリン酸)グリセリル 5.0
グリセリン 20.0
エトキシジグリコール 9.0
軽質流動パラフィン 10.0
アルキルグルコシド 10.0
ポリオキシエチレン硬化ヒマシ油40 1.0
ポリオキシエチレンモノヤシ油脂肪酸グリセリル 1.0
カルボキシビニルポリマー 0.5
トリエタノールアミン 0.1
精製水 残量
100%
Example 15 Cleansing Hydrogenated Lecithin 0.5
Tetra-2-ethylhexanoic acid pentaerythritol 5.0
Tri (capryl / capric acid) glyceryl 5.0
Glycerin 20.0
Ethoxydiglycol 9.0
Light liquid paraffin 10.0
Alkyl glucoside 10.0
Polyoxyethylene hydrogenated castor oil 40 1.0
Polyoxyethylene monococonut oil fatty acid glyceryl 1.0
Carboxyvinyl polymer 0.5
Triethanolamine 0.1
Purified water remaining
100%
実施例16 クリーム
大豆レシチン 0.1
ジプロピレングリコール 5.0
エトキシジグリコール 15.0
トリイソステアリン酸トリメチロールプロパン 0.5
トリ2−エチルヘキサン酸グリセリル 5.0
白色ワセリン 10.0
ポリオキシエチレン硬化ヒマシ油40 1.9
ステアリルアルコール 1.3
モノステアリン酸グリセリル 1.1
γ−オリザノール 1.0
カルボキシビニルポリマー 0.3
トリエタノールアミン 0.22
エデト酸ナトリウム 0.05
精製水 残量
100%
Example 16 Cream Soy Lecithin 0.1
Dipropylene glycol 5.0
Ethoxydiglycol 15.0
Trimethylolpropane triisostearate 0.5
Glyceryl tri-2-ethylhexanoate 5.0
White petrolatum 10.0
Polyoxyethylene hydrogenated castor oil 40 1.9
Stearyl alcohol 1.3
Glyceryl monostearate 1.1
γ-oryzanol 1.0
Carboxyvinyl polymer 0.3
Triethanolamine 0.22
Sodium edetate 0.05
Purified water remaining
100%
実施例17 クリーム
コンドロイチン硫酸ナトリウム 0.1
グリセリン 5.0
エトキシジグリコール 8.0
トリ2−エチルヘキサン酸トリメチロールプロパン 5.0
ジカプリル酸プロピレングリコール 0.5
グリチルリチン酸ジカリウム 0.1
白色ワセリン 10.0
セタノール 2.0
ポリオキシエチレン硬化ヒマシ油40 1.9
モノステアリン酸グリセリル 1.1
アスコルビン酸リン酸エステルナトリウム 0.5
カルボキシビニルポリマー 0.3
トリエタノールアミン 0.22
エデト酸ナトリウム 0.05
精製水 残量
100%
Example 17 Cream Sodium chondroitin sulfate 0.1
Glycerin 5.0
Ethoxydiglycol 8.0
Trimethylolpropane tri-2-ethylhexanoate 5.0
Propylene glycol dicaprylate 0.5
Dipotassium glycyrrhizinate 0.1
White petrolatum 10.0
Cetanol 2.0
Polyoxyethylene hydrogenated castor oil 40 1.9
Glyceryl monostearate 1.1
Sodium ascorbate phosphate 0.5
Carboxyvinyl polymer 0.3
Triethanolamine 0.22
Sodium edetate 0.05
Purified water remaining
100%
実施例18 クリーム
セラミド3 0.05
グリセリン 3.0
1,3‐ブチレングリコール 2.0
エトキシジグリコール 5.0
2−エチルヘキサン酸セチル 15.0
トリ2−エチルヘキサン酸トリメチロールプロパン 0.5
塩酸ピリドキシン 0.1
モノステアリン酸グリセリル 3.5
ポリオキシエチレンセチルエーテル 3.5
カルボキシビニルポリマー 0.8
トリエタノールアミン 0.22
エデト酸ナトリウム 0.05
精製水 残量
100%
Example 18 Cream Ceramide 3 0.05
Glycerin 3.0
1,3-butylene glycol 2.0
Ethoxydiglycol 5.0
Cetyl 2-ethylhexanoate 15.0
Tri-2-ethylhexanoic acid trimethylolpropane 0.5
Pyridoxine hydrochloride 0.1
Glyceryl monostearate 3.5
Polyoxyethylene cetyl ether 3.5
Carboxyvinyl polymer 0.8
Triethanolamine 0.22
Sodium edetate 0.05
Purified water remaining
100%
実施例19 非水型液晶ゲル
水素添加大豆レシチン 2.0
エトキシジグリコール 10.0
テトラ2−ヘキシルデカン酸アスコルビル 40.0
トリ(カプリル・カプリン酸)グリセリル 5.0
スクワラン 3.0
エデト酸ナトリウム 0.05
グリセリン 残量
100%
Example 19 Nonaqueous Liquid Crystal Gel Hydrogenated Soybean Lecithin 2.0
Ethoxydiglycol 10.0
Ascorbyl tetra-2-hexyldecanoate 40.0
Tri (capryl / capric acid) glyceryl 5.0
Squalane 3.0
Sodium edetate 0.05
Glycerin remaining
100%
実施例20 非水型液晶ゲル
水素添加大豆レシチン 1.0
プロピレングリコール 3.0
エトキシジグリコール 10.0
トリ2−イソステアリン酸トリメチロールプロパン 20.0
トリ(カプリル・カプリン酸)グリセリル 1.0
パルミチン酸レチノール 0.01
メチルフェニルポリシロキサン 5.0
エデト酸ナトリウム 0.05
グリセリン 残量
100%
Example 20 Nonaqueous Liquid Crystal Gel Hydrogenated Soybean Lecithin 1.0
Propylene glycol 3.0
Ethoxydiglycol 10.0
Tri-2-isostearic acid trimethylolpropane 20.0
Tri (capryl / capric acid) glyceryl 1.0
Retinol palmitate 0.01
Methylphenylpolysiloxane 5.0
Sodium edetate 0.05
Glycerin remaining
100%
実施例21 マイクロエマルジョン
水素添加大豆レシチン 2.0
エトキシジグリコール 10.0
テトラ2−エチルヘキサン酸ペンタエリスリトール 25.0
ジカプリン酸プロピレングリコール 5.0
精製水 5.0
エデト酸ナトリウム 0.05
グリセリン 残量
100%
Example 21 Microemulsion Hydrogenated Soy Lecithin 2.0
Ethoxydiglycol 10.0
Tetra-2-ethylhexanoic acid pentaerythritol 25.0
Propylene glycol dicaprate 5.0
Purified water 5.0
Sodium edetate 0.05
Glycerin remaining
100%
実施例22 マイクロエマルジョン
水素添加大豆レシチン 2.0
エトキシジグリコール 10.0
テトラ2−ヘキシルデカン酸アスコルビル 10.0
δ−トコレチナート 0.1
トリ(カプリル・カプリン酸)グリセリル 5.0
精製水 5.0
エデト酸ナトリウム 0.05
グリセリン 残量
100%
Example 22 Microemulsion Hydrogenated Soy Lecithin 2.0
Ethoxydiglycol 10.0
Ascorbyl tetra-2-hexyldecanoate 10.0
δ-tocolatinate 0.1
Tri (capryl / capric acid) glyceryl 5.0
Purified water 5.0
Sodium edetate 0.05
Glycerin remaining
100%
実施例22 マイクロエマルジョン
水素添加大豆レシチン 2.0
エトキシジグリコール 10.0
テトラ2−ヘキシルデカン酸アスコルビル 10.0
酢酸トコフェロール 5.0
テトラ2−エチルヘキサン酸ペンタエリスリトール 5.0
精製水 5.0
エデト酸ナトリウム 0.05
グリセリン 残量
100%
Example 22 Microemulsion Hydrogenated Soy Lecithin 2.0
Ethoxydiglycol 10.0
Ascorbyl tetra-2-hexyldecanoate 10.0
Tocopherol acetate 5.0
Tetra-2-ethylhexanoic acid pentaerythritol 5.0
Purified water 5.0
Sodium edetate 0.05
Glycerin remaining
100%
実施例22 非水型液晶ゲル
水素添加大豆レシチン 4.0
エトキシジグリコール 10.0
テトラ2−ヘキシルデカン酸アスコルビル 20.0
メチルフェニルポリシロキサン 5.0
テトラ2−エチルヘキサン酸ペンタエリスリトール 5.0
グリセリン 残量
100%
Example 22 Nonaqueous Liquid Crystal Gel Hydrogenated Soybean Lecithin 4.0
Ethoxydiglycol 10.0
Ascorbyl tetra-2-hexyldecanoate 20.0
Methylphenylpolysiloxane 5.0
Tetra-2-ethylhexanoic acid pentaerythritol 5.0
Glycerin remaining
100%
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Cited By (11)
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JP2007001965A (en) * | 2005-06-22 | 2007-01-11 | Sunstar Inc | Emulsion composition and cosmetic containing the same |
JP2008050273A (en) * | 2006-08-22 | 2008-03-06 | Shiseido Co Ltd | Skin care composition for external use |
JP2008063280A (en) * | 2006-09-07 | 2008-03-21 | Cedarcos Japan Co Ltd | Skin cosmetic |
JP2008184414A (en) * | 2007-01-29 | 2008-08-14 | Kao Corp | Cleansing composition |
JP2008195712A (en) * | 2007-01-16 | 2008-08-28 | Rohto Pharmaceut Co Ltd | External emulsion formulation |
JP2009511561A (en) * | 2005-10-14 | 2009-03-19 | レキット ベンキサー (ユーケイ) リミテッド | Microemulsion and shaving device containing microemulsion |
JP2010524988A (en) * | 2007-04-26 | 2010-07-22 | コグニス・アイピー・マネージメント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | Esters of hexyldecanol and short chain fatty acids |
WO2012011214A1 (en) * | 2010-07-23 | 2012-01-26 | 宮鍋 征克 | Method for obtaining sphingolipid and sphingolipid |
JP2012126910A (en) * | 2010-07-23 | 2012-07-05 | Miyanabe Masakatsu | Sphingolipid derived from fermentation lees |
JP2017165683A (en) * | 2016-03-16 | 2017-09-21 | 株式会社マンダム | Skin Cosmetic |
JP2020002059A (en) * | 2018-06-28 | 2020-01-09 | 小林製薬株式会社 | External composition |
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Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2007001965A (en) * | 2005-06-22 | 2007-01-11 | Sunstar Inc | Emulsion composition and cosmetic containing the same |
JP2009511561A (en) * | 2005-10-14 | 2009-03-19 | レキット ベンキサー (ユーケイ) リミテッド | Microemulsion and shaving device containing microemulsion |
JP2008050273A (en) * | 2006-08-22 | 2008-03-06 | Shiseido Co Ltd | Skin care composition for external use |
JP2008063280A (en) * | 2006-09-07 | 2008-03-21 | Cedarcos Japan Co Ltd | Skin cosmetic |
JP2008195712A (en) * | 2007-01-16 | 2008-08-28 | Rohto Pharmaceut Co Ltd | External emulsion formulation |
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JP2012041518A (en) * | 2010-07-23 | 2012-03-01 | Miyanabe Masakatsu | Sphingolipid and method for obtaining sphingolipid |
JP2012126910A (en) * | 2010-07-23 | 2012-07-05 | Miyanabe Masakatsu | Sphingolipid derived from fermentation lees |
JP2017165683A (en) * | 2016-03-16 | 2017-09-21 | 株式会社マンダム | Skin Cosmetic |
JP2020002059A (en) * | 2018-06-28 | 2020-01-09 | 小林製薬株式会社 | External composition |
JP7321679B2 (en) | 2018-06-28 | 2023-08-07 | 小林製薬株式会社 | external composition |
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